MPCST SPONSORED National Seminar DRUG DISCOVERY THROUGH REVERSE PHARMACOLOGY & ITS TRANSFORMATION INTO MODERN THERAPEUTICS CURRENT STATUS, CHALLENGES & OPPORTUNITIES
27th March 2017
ABSTRACT BOOK
Organized By Acropolis Institute of Pharmaceutical Education and Research www.aiper.ac.in
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
ABOUT THE INSTITUTE
Acropolis Institute of Pharmaceutical Education & Research (AIPER) is nurtured by Teach for India Education & Research Society having objective of creating state of art, world class and high quality technical education facilities at Indore. Towards fulfilment of its objective society established AIPER in the year 2008. AIPER is a philanthropic organization sprawled in an area of around 2 acres and is committed to the service of humanity through technological advancement. The institute offers Masters degree in Pharmaceutics and Bachelor’s degree in Pharmacy. The institute is approved by AICTE, New Delhi, PCI & CPCSEA and is affiliated to Rajiv Gandhi Technical University (RGPV), Bhopal.
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
GROUP CHAIRMAN’S MESSAGE
I am feeling immense pleasure to know that Acropolis Institute of Pharmaceutical Education & Research is going to organize MPCST Sponsored National Seminar on “Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities” on 27th March 2017.
The seminars, conferences act as a platform for academicians, industrialist, research scholars and students for sharing knowledge of drug discovery in the area of Pharmaceuticals, Cosmetics, Neutraceuticals and Allied segments.
I send my greetings and best wishes to the local organizing committee and all the participants for the grand success of seminar and also the deliberations. I also extend my best wishes for all the academic lectures and the scientific session.
Mr. Ashish Sojatia Group Chairman Acropolis Indore (M.P.)
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PRINCIPAL’S MESSAGE
It gives me immense pleasure in welcoming all the dignitaries, speakers and delegates to the MPCST Sponsored National Seminar on “Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities” on behalf of Acropolis Institute of Pharmaceutical Education & Research.
There could have not been any more relevant theme for National seminar in Pharmaceutical sciences to know the proper utilization of traditional knowledge, modern tools in discovering novel lead molecules from plants by employing Reverse Pharmacology techniques.
I hope this seminar will open up the discussion to help up the entire participant in the field of recent development in drug discovery. The seminar will definitely help and open a new area of research to the researchers by utilizing traditional medicinal knowledge. I wish the seminar to be a thought provoking, intellectually stimulating event, igniting the minds of participants for drug discovery and development through Reverse Pharmacology.
I also take this opportunity in thanking MPCST for sponsoring this event.
Dr. G.N. Darwhekar Principal AIPER Indore (M.P.)
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
ABOUT SEMINAR
Reverse pharmacology is the science of integrating documented clinical experiences and experiential observations into leads by transdisciplinary exploratory studies and further developing these into drug candidates or formulations through robust preclinical and clinical research. In recent years the revived scientific interest in plant-derived natural product-based drug discovery has been observed due to scientific and technological advances in the relevant research fields. The present seminar will highlight issues related to the proper utilization of traditional knowledge, modern tools in discovering novel lead molecules from plants by employing reverse pharmacology techniques. The seminar will definitely help and open a new area of research to the researchers by utilizing traditional medicinal knowledge.
OBJECTIVES OF THE SEMINAR
The objective of the proposed seminar is to understand the role of medicinal plants in discovery of new drugs which will provide a new area of research to understand and explore the plethora of medicinal plants and traditional knowledge for its transformation into modern therapeutics to achieve the goal of “Health For All”.
TOPICS TO BE DISCUSSED
Drug Discovery status in India Country’s contribution in the drug development Detailed process of drug discovery from lab to market including the time and cost involved at each stages Challenges involved in the plant origin drug discovery and its regulatory status including the patentability Country’s Scope and opportunity in the current scenario. etc
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
CHIEF GUEST
Dr. Shailendra Saraf Vice- President, Pharmacy Council of India
GUEST OF HONOURS & INVITED SPEAKERS
Mr. Sanjay Tiwari Vice President, Sun Pharmaceutical Industries Ltd.
Dr. Swarnalata Saraf Professor, University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur (C.G.) Vice- President, Association of Pharmacy Teachers in India
Dr. Manish Wanjari Scientist 2, Regional Ayurveda Research Institute for Drug Development, Gwalior, CCRAS, Ministry of AYUSH, Government of India
Dr. Adnan Naim Department of Bioscience and Biomedical Engineering, IIT Indore
Dr. C Karthikeyan Assistant Professor, School of Pharmaceutical Sciences, RGPV Bhopal
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
ORGANIZING COMMITTEE
CHIEF PATRONS Shri Ashok Sojatia Shri Ashish Sojatia
PATRONS Prof. M.K. Dube Dr. Shamsher Singh
TECHNICAL ADVISOR Dr. D.K. Jain Director, COP, IPS Academy
ORGANIZING CHAIRMAN Dr. G.N. Darwhekar
CONVENER Mr. Praveen Sharma
CO- CONVENER Mr. Ashish Gupta
REGISTRATION SCIENTIFIC WEB & MEDIA COMITTEE COMMITTEE Dr. Kunjbihari Sulakhiya Mr. Vikas Jain Ms. Lata Sharma Ms. Priyanka Joshi Ms. Ankita Mane Ms. Ritu Soudawat Ms. Priyanka Mishra Ms. Archana Patidar Ms. Akanksha Dwivedi Ms. Rakhi Khabiya
STAGE HOSPITALITY COMMITTEE COMMITTEE Mr. Mukul Sharma Mr. Ravi Sharma Ms. Anamika Singh Mr. Anupam Mishra
Organizing Institute Acropolis Institute of Pharmaceutical Education & Research, Indore
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
SEMINAR PROCEEDINGS
Acropolis Institute of Pharmaceutical Education & Research, Indore
MPCST SPONSORED
National Seminar on Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
TIME EVENT
8:30AM-9:30AM REGISTRATION & BREAKFAST
9:30AM-10:30AM PREINAUGRAL SESSION
10:30AM-11:30AM INAUGURAL CEREMONY
11:30AM-12:30PM SCIENTIFIC SESSION I
12:30PM- 1:30PM SCIENTIFIC SESSION II
1:30PM-2:00PM LUNCH
2:00PM-3:00PM SCIENTIFIC SESSION III
3:00PM-4:00PM POSTER PRESENTATION
4:00PM-5:00PM VALEDICTORY
5:00PM-5:30PM HIGH TEA
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
Acropolis Institute of Pharmaceutical Education & Research, Indore
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
INDEX
ABSTRACT TITLE PRESENTING NO. AUTHOR PREDICTION OF SITE OF METABOLISM FOR CYTOCHROME Dr. Elangovan PP-01 P450 1A2 LIGANDS AND VIRTUAL SCREENING MODELS Manivannan DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 3-(2- PP-02 OXO-2-ARYLETHYLIDENE)INDOLIN-2-ONES AS POTENTIAL Dr. C. Karthikeyan ANTI-BREAST CANCER AGENTS RATIONALIZATION OF MOLECULAR DESCRIPTORS OF PP-03 CYCLIC-UREA DERIVATIVES AS HIV PROTEASE INHIBITORS: Dr. M.C.Sharma A QSAR STUDIES EFFECT OF ACACIA NILOTICA L. ON DRUG INDUCED SEXUAL PP-04 Dr. Neelesh Malviya DYSFUNCTION IN MALE RATS. STRUCTURE-BASED VIRTUAL SCREENING AND IN-SILICO ADMET PROFILING ON PTP1B RECEPTOR FOR Mr. Neelesh PP-05 IDENTIFICATION OF POTENTIAL CELL PERMEABLE Maheshwari INHIBITORS OF NOVEL ANTI DIABETIC AGENT 3D-QSAR STUDIES OF 3-[4-(1H-IMIDAZOL-1-YL) PHENYL] PP-06 Ms. Ritu Soudawat PROP-2-EN-1-ONES AS ANTILEISHMANIAL AGENTS FORMULATION AND EVALUATION OF PLURONIC LECITHIN PP-07 Ms. Prerana Mishra ORGANOGEL OF LORNOXICAM FOR TOPICAL DELIVERY. SPECTROPHOTOMETRIC ESTIMATION OF TOTAL TANNIN PP-08 Dr. Vishal Soni CONTENT IN SOME AYURVEDIC EYE DROPS IN-VITRO ANTIUROLITHIATIC ACTIVITY OF ALCOHOLIC AND PP-09 HYDROALCOHOLIC EXTRACTS OF KALANCHOE PINNATA Dr. Priyanka Soni LEAVES IN VITRO SCREENING OF ETOPOSIDE HYDROGEL FOR ITS PP-10 PROPERTY AGAINST MELANOMA (B16F10) & LUNG (L-132) Mr. Anupam Mishra CANCER CELL LINES HIGH POTENTIAL ACTION OF AGOMELATINE FOR THE Dr. Shaily PP-11 TREATMENT OF OBSESSIVE COMPULSIVE DISORDER Chaudhary ANTI INFLAMMATORY & ANTI ULCER ACTIVITY OF JASMINUM PP-12 Mr. Anupam Mishra SAMBAC IN WISTAR RATS. REVERSE PHARMACOLOGY: A NEW APPROACH TO DRUG Mr. Vikas Kumar PP-13 DISCOVERY AND DEVELOPMENT AND ALSO AMELIORATES Jain PROCESS. APPROACHES IN THE DEVELOPMENT OF QUALITY PP-14 PARAMETERS OF MEDICINAL PLANTS WITH REFERENCE TO Dr. Sumeet Dwivedi ENDANGERED MEDICINAL PLANTS MODELING OF CARBONIC ANHYDRASE INHIBITOR-I (CA-I) PP-15 Ms. Sarla Biloniya, WITH LOG KI (NANOMOLAR AFFINITY)
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 1
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP-16 DRUG DISCOVERY: JOURNEY FROM CONCEPT TO MARKET Ms. Saloni Kakkar FORMULATION & EVALUATION OF BERBERINE PP-17 NANOPARTICLES FOR ADMINISTRATION THROUGH NASAL Ms. Ankita Mane ROUTE PP-18 NETWORK P[HARMACOLOGY Ms. Anamika Singh SOLID DISPERSION: A REVIEW Mr. Abhishek PP-19 Yaduvanshi ANTIDEPRESSANT ACTIVITY OF HYDROALCOHOLIC Ms. Aashruti PP-20 EXTRACT OF BUCHANANIA LANZAN Agrawal HERBAL PLANTS CONTAINING CHOLINESTERASE PP-21 Mr Aman Mourya INHIBITORS ACTIVITY APPROACH FOR MEMORY ENHANCING PP-22 A REVIEW: ON MEDICATED TAPE Mr. Ankit Gupta PP-23 CARBON NANOTUBES : A REVIEW Mr. Avinash Sharma ANTIPARASITIC ACTIVITY OF NYCTANTHES ARBOR-TRISTIS PP-24 Mr. A. Nigam LINN. IN MALARIA: "REVERSE PHARMACOLOGY" A REVIEW : ON FAST DISINTEGRATING TABLETS Mr. Beerendra PP-25 Vishwakarma HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY PP-26 Mr. Farhan Qureshi PROCESS AND FUTURE ASPECTS ANTI-ANEMIC ACTIVITY OF HYDRO-ALCOHOLIC LEAF Ms. Deepanshu PP-27 EXTRACT OF TAMARINDUS INDICA IN PHENYLHYDRAZINE Gupta INDUCED ANEMIC RATS WNT/Β-CATENIN PATHWAY AS NOVEL TARGET FOR PP-28 Mr. Abhishek Rai ANTICANCER DRUG DISCOVERY IDENTIFICATION OF NOVEL ANTI-INFLAMMATORY AGENTS PP-29 FOR PREVENTION OF CHRONIC DISEASES: "REVERSE Ms. H.Sayyed PHARMACOLOGY" ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF HYDRO- PP-30 Mr. Someshver Sirvi ALCOHOLIC EXTRACT OF JUGLANS CINEREA DEVELOPING AN ANTI-MALARIAL PHYTOMEDICINE THROUGH Ms. Manobhi PP-31 REVERSE PHARMACOLOGY Maltare TARGETING THE MDM2-P53 PROTEIN-PROTEIN INTERACTION PP-32 Ms. Neha Trivedi FOR NEW CANCER THERAPEUTICS AN ARCHETYPE SHIFT FOR MODERN DRUG DEVELOPMENT: PP-33 AN APPROACH FOR CLINICAL CANDIDATE USING REVERSE Ms. Varnika Pagare PHARMACOLOGY. COMBINATORIAL CHEMISTRY: “A NOVEL AND EFFICIENT PP-34 Mr. Palash Prajapati APPROACH IN DRUG DISCOVERY” DIURETIC ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF PP-35 Mr. Pawan Goud NYCTANTHES ARBORTRISTIS IN ALBINO RATS PP-36 SUBLINGUAL TABLETS : AN OVERVIEW Ms. Sheetal Sem PP-37 NEW ECO-FRIENDLY TITRIMETRIC ANALYSIS OF ASPIRIN Ms. Smriti Mishra
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 2
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
TABLETS USING MIXED HYDROTROPIC SOLUBILISATION TREATMENT OF TUBERCULOSIS FROM DRUG DEVELOPED PP-38 Ms. Soniya Pillai THROUGH SOIL BACTERIA PP-39 PILOT PLANT DEVELOMENT OF MARIJUANA TAMPONS Ms. Sunayna Joshi DESIGN AND DEVELOPMENT OF MICROEMULSION DRUG PP-40 DELIVERY SYSTEM OF FELODIPINE FOR IMPROVEMENT OF Ms. Rinku Verma ORAL BIOAVAILABILITY’’ NEW ECO-FRIENDLY APPLICATION OF MIXED HYDROTROPIC PP-41 SOLUBILISATION FOR TITRIMETRIC ANALYSIS OF Mr. Sunil Goyal ACECLOFENAC TABLETS MEMORY ENHANCING ACTIVITY OF BUCHANANIA LANZAN BY Mr. Priyanshu PP-42 SCOPOLAMINE INDUCED AMNESIA IN RATS Shekar A REVIEW: ON GASTRORESISTENT MICROPARTICLES PP-43 CONTAINING SODIUM-PANTOPRAZOLE: STABILITY STUDIES Ms. Priyanka Yadav AND IN-VIVO ANTIULCER ACTIVITY 5 ACETIC ACID PEPTIDE HYBRID DERIVATIVES AS POTENT PP-44 Mr. R. Sharma ANTIDIABETIC AGENTS "REVERSE PHARMACOLOGY" NOVEL CARBAZOLE TETHERED PYRROLE DERIVATIVES AS PP-45 POTENT INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS Mr. R. Adhav "REVERSE PHARMACOLOGY" ANTI-DIABETIC EFFECT OF MAHANIMBINE FROM MURRAYA Ms. Supriya PP-46 KOENIGII: REVERSE PHARMACOLOGY Shidhaye NATURAL GUMS AS SUPERDISINTEGRANTS IN PP-47 Mr. Sovran S Thakur FORMULATION OF MOUTH DISSOLVING TABLETS- A REVIEW ADR IN HERBAL MEDICATION WITH MAINSTREAM MEDICAL PP-48 Ms. Garima Sharma THERAPIES ISOLATION OF AMYLASE PRODUCING BACTERIA FROM SOIL AND ITS OPTIMIZATION OF PP-49 Ms. Nidhi Nair PRODUCTION PARAMETERS BY SHAKE FLASK CULTURE METHOD CUTTING EDGE IN DRUG DISCOVERY AND DEVELOPMENT – Ms. Mehazabeen PP-50 REVERSE PHARMACOLOGY Kachchawala INHIBITION OF MATRIX METALLOPROTEINASE – 2 (MMP) IN DMH INDUCED COLON CANCER IN SD RATS IN THE PP-51 PRESENCE OF DIETARY SUPPLEMENTS AND Mr. Taha Hakimi CHEMOTHERAPY: A MECHANISM AND PROBLEMS BASED APPROACH
PP-52 IN VITRO ANTI OXIDANT ACTIVITY OF HYDRO-ALCOHOLIC Ms. Sweta S Koka EXTRACT OF CAESALPINIA BONDUC
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 3
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 01
PREDICTION OF SITE OF METABOLISM FOR CYTOCHROME P450 1A2 LIGANDS AND VIRTUAL SCREENING MODELS Elangovan Manivannan*and N.S. Hari Narayanan Moorthy School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore-452001 (M.P.) Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak-484887 [email protected]
ABSTRACT
Cytochrome P450 (CYP) 3A4, 2D6, 2C9, 2C19, and 1A2 are the most important drug-metabolizing enzymes. Understanding of which parts of a drug molecule are subject to metabolic reactions catalyzed by these enzymes is crucial for drug design. With the availability of large number of high resolution crystal structures of human cytochrome P450 enzymes made possible the utility of structure-based molecular modeling tools to study cytochrome P450. In the present study we explore the possibilities of employing docking and scoring functions on cytochrome P450 1A2. An Attempt has been made to address the issues like prediction of binding orientations and conformations for various substrates, a virtual screening with satisfactory enrichment rates. The results show that docking and scoring can be used successfully to address the issues. Results of the structure-based modeling were compared to experimental data. The possibilities and limitations of using structure-based drug design tools for cytochrome P450 1A2 are discussed in detail. Keywords: Cytochrome P450 (CYP), metabolism, ligands, screening models.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 4
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 02
DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 3-(2-OXO-2-ARYLETHYLIDENE) INDOLIN-2-ONES AS POTENTIAL ANTI-BREAST CANCER AGENTS C. Karthikeyan1*, H. Lee2, M. R. Mustafa3 and P. Trivedi1 1Schoool of Pharmaceutical Sciences,Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal-462033, India. 2Advanced Medical Research Institute of Canada, Sudbury, Ontario P3E 5J1, Canada. 3Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia. [email protected]
ABSTRACT
Breast cancer is one of the most commonly diagnosed cancers among women and it is the second leading cause of cancer deaths in women worldwide. The present study describes discovery of a novel series of 3-(2-oxo-2-arylethylidene) indolin-2-ones as potential antibreast cancer agents. Fourteen 3-(2- oxo-2-phenylethylidene) indolin-2-ones designed employing molecular hybridization approach were synthesized and evaluated for growth inhibitory activity against three breast cancer cell lines (MDA- MB231, MDA-MB468 and MCF-7) and one non-cancer breast epithelial cell line (184B5) using SRB protocol. The results indicated that most of the compounds showed promising anticancer activity (<20 µM) against the studied cancer cell lines. Compound 3m bearing a 5- chloro substituent in the benzo ring of the Isatin moiety and 3, 4-dimethoxy substitution in the phenyl ring was found to be the most active in the series with IC50 values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF-7 cells, respectively. The mechanism of cytotoxicity of 3m was studied in MCF-7 cells and the results revealed that 3m induces intracellular ROS generation, which causes DNA damage, increased membrane permeability and activation of a mitochondria-dependent caspase cascade resulting in apoptosis. Overall, the findings of the mechanistic studies highlight 3m as a potential new lead molecule for the development of novel anticancer agents with potential therapeutic benefits in breast cancer. Keywords: Breast cancer, molecular hybridization, anticancer, apoptosis.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 5
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 03
RATIONALIZATION OF MOLECULAR DESCRIPTORS OF CYCLIC-UREA DERIVATIVES AS HIV PROTEASE INHIBITORS: A QSAR STUDIES Sharma M.C.* *School of Pharmacy, Devi Ahilya University, Khandwa Road, Indore (M.P) - 452 001, India [email protected]
ABSTRACT
Herein described is quantitative structure activity analysis of a series of cyclic-urea derivatives were taken as HIV protease inhibitors with inhibitory HIV were developed. The best quantitative structure activity relationship model was selected having a correlation coefficient (r2) of 0.7562, cross-validated correlation coefficient (q2) of 0.7218. The model selected emphasized the importance of Highest Occupied Molecular Orbital, and lowest unoccupied molecular orbital energy suggest that a good percentage of the total variance in biological activity. Based on the findings of the QSAR study, novel compounds for HIV protease inhibitors can be synthesized. Keywords: QSAR, multiple linear regressions, cyclic-urea, Chem‐Office 8.0, HIV protease inhibitors
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 6
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 04
EFFECT OF ACACIA NILOTICA L. ON DRUG INDUCED SEXUAL DYSFUNCTION IN MALE RATS
Neelesh Malviya* Department of Pharmacognosy Smriti College of Pharmaceutical Education, Indore, M.P. [email protected]
ABSTRACT
Acacia nilotica L. commonly known as babool is one of the most widely used medicinal plants in Indian system of medicine and traditionally used as antiplasmodial, anti-inflammatory, analgesic and antipyretic. It has been reported to have antidiabetic, antioxidant and considerable inhibitory effects against HIV-1 protease. In traditional system of medicines, stem of Acacia nilotica is often recommended for the management and treatment of Male sexual dysfunctions. However, convincing scientific data to support the aforesaid claim is lacking. Thus in the absence of any scientific evidence, in the present study an attempt was taken to investigate the effect of alcoholic extract of Acacia nilotica L. stem on male rat sexual behavior and its effects on androgenic hormones in paroxetine induced reproductive dysfunction in experimental male rat model. Alcoholic extract of stem of Acacia nilotica at the dose of 500mg/kg body weight was administered in male rats and mount frequency, intromission frequency, ejaculatory frequency, mount latency, intromission latency, ejaculatory latency and post-ejaculatory interval, sperm profile, testes weight, testicular index, hormones level and histoarchitecture of reproductive organs were the parameters observed and compared during the study. Results observed from the study revealed that the alcoholic extract of stem of Acacia nilotica at the dose of 500mg/kg body weight, significantly restore the sexual behaviour in paroxetine induced reproductive dysfunction in experimental male rat model. Keywords: Indian system of medicine, Male Sexual Dysfunction, Acacia nilotica, Paroxetine, Medicinal Plant
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 7
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 05
STRUCTURE-BASED VIRTUAL SCREENING AND IN-SILICO ADMET PROFILING ON PTP1B RECEPTOR FOR IDENTIFICATION OF POTENTIAL CELL PERMEABLE INHIBITORS OF NOVEL ANTI DIABETIC AGENT Maheshwari Neelesh#1, Karthikeyan Chandrabose1, Trivedi Piyush1 Moorthy N. S. Hari Narayana2 1 School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal, Madhya Pradesh. 2Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh [email protected]
ABSTRACT
Abstract: Protein tyrosine phosphatases (PTPs) and protein tyrosine kinases (PTKs) maintain a balance of protein activity through the dephosphorylation and phosphorylation of proteins in a signalling pathway and regulate virtually all aspects of cellular functions. An imbalance of PTP and PTK activities can lead to abnormalities which causes of human diseases, such as cancers, diabetes and obesity. PTP1B is an important member of PTP family which has been implicated as key regulators of intracellular signalling cascades and involved in various important pathways related with diabetes and obesity. Hence, it has been acknowledged as an outstanding therapeutic target for the treatment of cancer, diabetes along with obesity. The aim of this study was to screen a library of small molecules In-silico for discovery of some inhibitors of PTP1B with increased cell permeability. The molecular docking based virtual screening results showed that compounds possessed good docking score and interacted well with the active site residues as well as secondary aryl phosphate binding site of PTP1B enzyme. In-silico ADME prediction studies on these hits were also found to be promising. Non-charged compounds identified as hits may act as novel leads for PTP1B inhibitors. Keywords: PTP1B, Diabetes and obesity, Docking, ADME prediction
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 8
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 06
3D-QSAR STUDIES OF 3-[4-(1H-IMIDAZOL-1-YL) PHENYL] PROP-2-EN-1-ONES AS ANTILEISHMANIAL AGENTS
Soudawat Ritu 1, Kaskhedikar, S.G. 2 1Acropolis Institute of Pharmaceutical Education and Research, Indore, M.P. 2 Department of Pharmacy, Shri G. S. Institute of Technology & Science, Indore. [email protected]
ABSTARCT
Leishmaniasis, a disease caused by obligate intracellular protozoa of the genus Leishmania, is an old but largely unknown disease that afflicts the world’s large populations. WHO estimates the worldwide prevalence to be approximately 12 million cases, with annual mortality of about 60 000. The size of the population at risk is about 350 million. Currently the drugs used for the treatment of Leishmaniasis are limited and are very expensive and highly toxic. The recently reported series of 3-[4-(1H-Imidazol-1-yl) Phenyl] Prop-2-en-1-ones have activity in the range of 0.63 to 1.11 µg against Leishmania major promastigotes and may rise another class of therapeutic agents. The molecular modeling study was performed using P-IV processor CS Chemoffice version 8.0 and regression analysis were carried out on VALSTAT. The various statistical parameters of the selected model are: The correlation coefficient (r) =0.865, R-squared the coefficient of determination (r2) = 0.788, Fisher test value F=82.72, the standard
2 2 2 deviation of regression (SD) - 0.148, bootstrapping r (r bs) - 0.798 & Q -0.624.
Keywords: Leishmaniasis, QSAR, Antileishmanial Agents, molecular modeling.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 9
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 07
FORMULATION AND EVALUATION OF PLURONIC LECITHIN ORGANOGEL OF LORNOXICAM FOR TOPICAL DELIVERY. Prerana Mishra*, D P Chatterjee Mittal Institute of Pharmacy, Bhopal (M. P.) [email protected]
ABSTRACT
Pluronic Lecithin Organogels (PLO gels) are commonly used as transdermal vehicles in compounding pharmacies to provide customized medication for pain management as well as for other therapies. The purpose of this research is to formulate and evaluate the suitability of pluronic lecithin organogels containing lornoxicam for topical application. Eleven formulations were developed using lornoxicam, soya-lecithin, Pluronic F127, isopropyl myristate, PEG-400, sorbic acid and potassium sorbate were coded as F-1to F-11. Concentration of Pluronic F127 and soya-lecithin was varied in these formulations. The optimized organogels were evaluated for appearance and feel rheologically, in vitro diffusion study, drug content, viscosity and pH. Release of lornoxicam from all formulations was monitored via dialysis membrane-70 and Wistar rat skin as a semipermeable membrane into phosphate buffer saline (0.2 M, pH 7.4) using Keshary-Chien diffusion cell. The viscosities of different formulations were determined by using Brookfield Viscometer at 25°. An attempt has been made to explore the potential of pluronic lecithin organogels for topical delivery of lornoxicam.
Keywords: Pluronic Lecithin Organogels, transdermal.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 10
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 08
SPECTROPHOTOMETRIC ESTIMATION OF TOTAL TANNIN CONTENT IN SOME AYURVEDIC EYE DROPS
Soni Vishal*, Soni Priyanka, Mali Tarun
Department of Herbal Drug Research, B.R. Nahata College of Pharmacy, Research Centre, Mhow Neemuch Road, Mandsaur 458001, India
ABSTRACT
Ayurvedic eye drops preparation contains aqueous extracts of different herbs. Ethnobotanical survey shows that plants used in Ayurvedic eye drops formulation are rich source of tannin and tannin like compounds. Tannins are responsible for antimicrobial and antioxidant properties of Ayurvedic eye drops. The present study was designed with the aim to determine the tannin content in two different brands of Ayurvedic eye drops, by colorimetric method using Folin-denis reagent. The tannin content of both the brands was found to be A-725.23 and B-556.00 μg/ml. The results obtained are reproducible with coefficient of variation less than 0.99 %. The present approach can be used as one of the parameters for the standardization of Ayurvedic eye drop preparations.
Keywords: Tannin estimation, antimicrobial activity, Ayurvedic eye drops, standardization etc
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 11
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 09
IN-VITRO ANTIUROLITHIATIC ACTIVITY OF ALCOHOLIC AND HYDROALCOHOLIC EXTRACTS OF KALANCHOE PINNATA LEAVES
Soni Priyanka, , Soni Vishal, Chhipa Abu Sufiyan
Department of Herbal Drug Research, B.R. Nahata College of Pharmacy and Research Centre
Mhow Neemuch Road, Mandsaur 458 001, India
ABSTRACT
The objective of this research was to find the efficiency of alcoholic and hydroalcoholic extracts of Kalanchoe pinnata leaves in dissolution of calcium oxalate crystals by using in-vitro dissolution model. in-vitro dissolution model was prepared by using semi permeable membranes obtained from eggs that served as dissolution bags for the investigation. Dissolution bags containing calcium oxalate and different extracts were suspended in conical flasks containing TRIS buffer. Percentage dissolution of calcium oxalate by different extracts was evaluated by titrimetry. Hydroalcoholic extract of leaves of Kalanchoe pinnata showed more dissolution of calcium oxalate as compared to alcoholic extract. Although the dissolution of calcium oxalate by hydroalcoholic extract was less than that of standard drug. Results obtained from this research work indicated promising effects of Kalanchoe pinnata leaves in dissolution of calcium oxalate. Extracts of Kalanchoe pinnata leaves can be used for the effective treatment of urolithiasis.
Keywords: Kalanchoe pinnata, antiurolithiatic activity, calcium oxalate, hydroalcoholic, alcoholic, cystone.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 12
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 10
IN VITRO SCREENING OF ETOPOSIDE HYDROGEL FOR ITS PROPERTY AGAINST MELANOMA (B16F10) & LUNG (L-132) CANCER CELL LINES
Mishra Anupam*1, N Ganesh2, Soni Govind2, Yadav Khushwant S2., Dhote Vipin V2
1Acropolis institute of pharmaceutical education and research, Indore
2VNS faculty of pharmacy, Bhopal
ABSTRACT
The present study was designed to investigate the in vitro screening of the Etoposide Hydrogel for its property against Melanoma (B16F10) and Lung (L-132) Cancer Cell Lines.
Viability of cancer cell lines is determined by trypan blue exclusion method, in this method 10µl of cell line & 10µl of 0.4% trypan blue stain was added thoroughly and allows staining for 5 min and to observing under microscope. Cytotoxicity study of cancer cell lines against hydrogels of etoposide and other anticancer drugs was determined by M.T.T assay. Cells were seeded into 96-well plate and subjected on hydrogel treatments. 24 h before the end of experiment, 30μl of M.T.T was added and cells were incubated at 37°C. Then medium was removed and the residue was dissolved in DMSO. The absorbance of each well was read at 490 nm with ELISA reader. Thermosensitive Hydrogel of Etoposide showed Anticancer activity and was found to be statistically very significant when compared to normal control with a p value of <0.05 and <0.001 on treatment with lung cancer (L132) and Melanoma (B16F10) cell lines respectively. The present study is a comparative study between old conventional therapeutic regimen and modern approach of sustain release of drug i.e. hydrogels. It demonstrates that the hydrogel of etoposide have effectively approach the cancerous cells to inhibit its potentiality. Such drug delivery is in demand in the field of oncomedicine where the conventional drug causes huge number of cellular as well as organ toxicity. The present study will not only approach the cancerous cells but could be able to protect normal cell cellularity & morphology.
Keywords: Lung cancer, Melanoma, Thermosensitive Hydrogels of Etoposide, Cell lines, M.T.T assay.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 13
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 11
HIGH POTENTIAL ACTION OF AGOMELATINE FOR THE TREATMENT OF OBSESSIVE COMPULSIVE DISORDER
Shaily Chaudhary*1,Khuswant Singh Yadav1 and Nikunjana Patel2
1Smriti College of Pharmaceutical Education, 4/1, Pipliya Kumar Kakkad, MR-11, Indore, Madhya Pradesh, India. 2Faculty of Pharmacy, Shree S. K. Patel College of Pharmaceutical Education &Research, Ganpat University,Ganpat Vidyanagar, Gujarat, India.
ABSTRACT
In the present work, a randomized, double-blind, placebo-controlled trial was performed to check the efficacy of agomelatine in treatment of anxiety disorder, prompting its therapeutic potential in treatment of obsessive compulsive disorder (OCD). The effect of acute and chronic administration of agomelatine on the marble burying behavior (MBB) of mice, which is reported to be an index of anticompulsive behavior, was performed. In addition, to rule out the role of enhanced serotonergic neurotransmission, studies were carried out in p-chlorophenylamine (PCPA). Results indicated a potent and dose dependent influence of agomelatine on MBB of mice. However, the higher doses were found to be locomotor depressant. In conclusion, agomelatine administration reduces the MBB in mice, which should be explored for its potential use in the treatment of OCD.
Keywords: Agomelatine, obsessive compulsive disorder (OCD), marble-burying behavior (MBB), melatonin.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 14
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 12
ANTI INFLAMMATORY & ANTI ULCER ACTIVITY OF JASMINUM SAMBAC IN WISTAR RATS.
Mishra Anupam1*, Dangi Uma2, Sheikh Saima2, Kawadkar Manisha2, Dhote Vipin V2.
1Acropolis institute of pharmaceutical education and research, Indore
2VNS faculty of pharmacy, Bhopal
ABSTRACT
The present study was designed to investigate the Antiulcer activity following indomethacin induced ulceration & Anti-inflammatory activity following histamine induced paw edema of Jasminum sambac in rats.Adult wistar rats (180-250gm) were exposed to inflammation by using Histamine induced paw edema. Rat received histamine (0.1ml) in saline solution for 7 days in sub-planater region of left hind paw. Ethenolic extract of jasminum sambac leaf (400mg/kg, p.o.) given & following parameter were estimated like percentage inhibition paw volume and Antioxidant parameters like S.O.D & L.P.O. Jasminum sambac was evaluated for Anti-ulcer activity; ulcer was induced using indomethacin induced model. Animal were treated with indomethacin (5mg/kg, p.o.) for 5 days for induction. Aqueous extract of jasminum sambac stem (500mg/kg, p.o.) was administered & ulceration was evaluated by estimating ulcer index and percentage (%) ulcer inhibition. Jasminum sambac leaf extract showed significant (*P<0.05) Reduction in paw volume percentage inhibition, SOD activity (P<0.001) were significantly enhanced while LPO levels (P<0.001) significantly reduced with treatment of jasminum sambac. Jasminum sambac stem extract showed significant reduction (*P<0.05) in ulcer index & percentage ulcer inhibition as compare to control group. Jasminum sambac showed potent Anti-ulcer & Anti-inflammatory activity which could be mediated by antioxidant, analgesic & antispasmodic. These activities could be attributed to the presence of glycosides like sambicin, jasminin and flavonoides. The optimum dose of Jasminum sambac which produced gastro protective activity was found to be 500mg/kg & anti-inflammatory activity was found to be 400mg/kg in this experimental study.
Keywords: Anti-inflammatory, anti-ulcer.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 15
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 13
REVERSE PHARMACOLOGY: A NEW APPROACH TO DRUG DISCOVERY AND DEVELOPMENT AND ALSO AMELIORATES PROCESS.
Jain Vikas Kumar*, Darwhekar G N
Acropolis institute of pharmaceutical education and research, Indore
ABSTRACT
“Historically modern drug therapy has developed from the herbal and folklore medicine of the past with its mixture of magic, empirical pharmacology and faith of the patient in the doctor.” Natural products of ayurveda offer a vast potential for novel phytomolecules with clinical activity. In India, ayurveda is availed of by more than 70% of the population. There has been a renaissance in scientific exploration of medicinal plants with therapeutic activity. New methods have been proposed and developed for such exploration. Ayurvedic pharmacoepidemiology, observational therapeutics and reverse Pharmacology paths have led to significant hits, leads and drug candidates for several diseases. The active phyto- molecules will also provide novel scaffolds for medicinal chemists to enhance efficacy and reduce toxicity. In case of conventional R & D expenses have risen enormously in last decade but surprisingly it has not led to a corresponding increase in the number and efficacy of new drugs. Alternatively, reverse pharmacology also known as target base drug discovery is now becoming a popular option in the field of drug discovery and development from bedside observations on drug effects to bench-side experiments. This approach generates evidence of safety and efficacy at different levels of biological organization, ranging from cell to community. Eventually the innovative integration of research methods will be translated back to the bedside as a new drug. The article also discusses the Reverse Pharmacology approach for natural products used for treatment of various diseases.
Keywords: Reverse Pharmacology, Ayurveda, Drug discovery and development, R&D
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 16
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 14
APPROACHES IN THE DEVELOPMENT OF QUALITY PARAMETERS OF MEDICINAL PLANTS WITH REFERENCE TO ENDANGERED MEDICINAL PLANTS
Shriwas Shweta, Dwivedi Sumeet*, Dubey Raghvendra
College of Pharmacy, Dr. APJ Abdul Kalam University, Indore, (M.P.), India
ABSTRACT
India is among the important mega biodiversity centers of the world with nearly 45,000 known plant species. This diversity coupled with a rich heritage of traditional knowledge in Ayurveda, Siddha and Unani. Herbal medicines, however, are associated with a number of shortcomings including uniform efficacy and lack of appropriate quality control measures at various stages of product development. The present paper intends to outline the importance of development of quality parameters towards standardization and manufacturing of botanicals especially endangered medicinal plants. The previous finding highlights that there have been constant efforts for developing state of the art technologies in the field of herbal research. Sincere efforts were to be taken to ensure safety, purity and efficacy of herbal medicines by the Govt. authorities and researcher.
Keywords: India, quality control, regulations, standardization, traditional medicine
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 17
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 15
MODELING OF CARBONIC ANHYDRASE INHIBITOR-I (CA-I) WITH LOG KI (NANOMOLAR AFFINITY)
Biloniya Sarla, Verma R.G., Solanki Aruna
Government Science College, Dewas
ABSTRACT
This paper deals with a QSAR study on a large set of carbonic anhydrase inhibitor-I using a combination of topological descriptor. The regression analysis has been carried out assuming linear relationship between LogKi nd topological descriptor. The analysis of the data has indicated that an excellent model is obtained. The obtained model is further supported through cross validation.
Keywords: QSAR/ topological descriptor/ carbonic anhydrase inhibitor-I/LogKi
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 18
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 16
DRUG DISCOVERY: JOURNEY FROM CONCEPT TO MARKET
Kakkar Saloni 1*, Tahlan Sumit 1
1Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana
ABSTRACT
Drug development takes around 10-15 years and is an expensive, long and high-risk business. Before a drug is deemed suitable for patients, it has to go through rigorous testing and cost-effectiveness analyses. The need for new drugs is because of medical reasons, disease prevalence and the likelihood of success. Before any drug can be administered to humans, it involves refining the molecular properties until a compound is suitable. The major sources for the development of drug candidate have always been natural compounds from plants, fungi or marine animals but nowadays focus has shifted to genetics and proteins to create new molecules using computers. Any drug candidate has to undergo extensive range of in vitro and in vivo test procedures prior to its administration to humans. One of the regulatory requirements is that the drug is to be administered to animals as well to assess its safety which is known as Pre-clinical trial. Clinical trials includes phase I in which healthy volunteers participate to assess primarily pharmacokinetics, safety and toleration, phase II involves the patients with the target disease to establish efficacy and dose-response relationship and large-scale phase III studies to confirm safety and efficacy. Each drug is required to outweigh its benefits over its risks before it will be approved by the regulatory agencies. The pre -clinical and clinical trials as well as the manufacturing of pharmaceutical products are required to follow the regulatory standards. The assessment of the new medicinal product’s safety continues beyond the initial drug approval through post-marketing monitoring of adverse events.
Keywords: Drug discovery, Pre-clinical trial, Clinical trial, Safety and efficacy.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 19
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 17
FORMULATION & EVALUATION OF BERBERINE NANOPARTICLES FOR ADMINISTRATION THROUGH NASAL ROUTE
Mane Ankita, Darwhekar G.N, Gupta Ashish
Acropolis Institute of Pharmaceutical Education & Research, Indore
ABSTRACT
Berberine is a protoberberine type, isoquinoline alkaloid, derived from medicinal plants such as Hydrastis Canadensis L, Coptis rhizome & barberry plants (Berberis vulgaris). Berberine is used in indian & chinese medicines as an antimicrobial, stomachic & in treatment of cancer, diabetes mellitus & neurodegenerative diseases. Literature review shows that berberine distributes readily in various tissues and hence very low amount of berberine reach to the systemic circulation which accounts for its low bioavailability (0.68 %). Bioavailability of berberine can be improved by formulating it as nanoparticles.
Present study aims to prepare & evaluate nanoparticles containing berberine using chitosan as polymer and administration of this nanoparticle preparation through nasal route so as to improve its bioavailability. The nanoparticles were prepared by ionic gelation method and evaluated for particle size, zeta potential, entrapment efficiency, In-vitro drug release & drug release kinetics.
The formulation A5 showed particle size – 104.52 nm, zeta potential – 32.40 mV and entrapment efficiency – 30.05 %. In-vitro release studies showed improved bioavailability of 80.23 %. The drug release kinetic studies showed that berberine nanoparticle formulation followed Higuchi & Korsmeyer- peppas model of drug release.
Keywords: Nanoparticle, antimicrobial, bioavailability, nasal route.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 20
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 18
NETWORK PHARMACOLOGY: A NOVEL APPROACH FOR DRUG DEVELOPMENT
Singh Anamika*, Darwhekar G. N.
Acropolis Institute of Pharmaceutical Education and Research, Indore
ABSTRACT
Network pharmacology is a distinctive new approach to drug discovery. It involves application of network analysis to determine the set of proteins most critical in any disease, and then chemical biology to identify molecules capable of targeting that set of proteins. It is a novel approach which works on the principle of “multiple targets, multiple effects, complex disease” instead of the conventional principle of “one gene, one target, one disease”. System biology is a recent trend in bioscience research which focuses on the complex interactions in biological systems from a holistic perspective rather than altering the single molecular component. The process of network pharmacology research includes data collection and validation followed by network analysis and visualization. Network pharmacology can make an impact at two main approaches in the drug development process. One is to establish a pragmatic network model and predict the drug target based on public databases or available data of earlier researches. Subsequently, the mechanism of functional drug should be explored for the network equilibrium principle. The advantage of network pharmacology includes regulation of the signaling pathway with multiple channels, increase in drug efficacy, reduction of side effects, increase in the success rates of clinical trials and decrease in the costs of drug discovery. The advancements in systems biology and bioinformatics and the concept of network pharmacology will undoubtedly bring about a conceptual move in drug discovery.
Keywords: Network Pharmacology, Drug Discovery, System Biology
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 21
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 19
SOLID DISPERSION: A REVEW
Yaduvanshi Abhishek*, Darwhekar G.N., Gupta Ashish, Sharma Ravi
Acropolis institute of pharmaceutical education and research, Indore
ABSTRACT
Upto 40 percent of new chemical entities are poorly water soluble or lipid soluble. Drugs that followes dissolution rate limited gastrointestinal absorption results in better dissolution and good bio availability due to decressed particle size. However reduction of particle size of drug may cause aggregation and agglomeration those results in poor wettability. Development of solid dispersion is an effective approach to improve bioavailability of poorly water soluble drugs by overcoming the limitations of other approaches like formation of salt, reduction of particle size. Solid Dispersion is a novel phenomenon to overcome these problems and to enhance the dissolution by making the solid dispersion of water soluble carriers with poorly water soluble drugs. The overall review emphasis on bioavailablity enhancement of poorly aqueous soluble drugs by solid dispersion technolgy which utilizes to develop various dosage forms in convinent way.
Keywords: Solid Dispersion, Bioavailablity, Solubility, Techniques
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 22
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 20
ANTIDEPRESSANT ACTIVITY OF HYDROALCOHOLIC EXTRACT OF BUCHANANIA LANZAN
Agrawal Aashruti*, Joshi Ankur, Malviya Sapna, & Kharia Anil
Modern institute of Pharmaceutical Sciences, Indore
(Shri Prabhat Chandra Kharia Research and Educational Society)
Alwasa, Behind Rewti Range, Sanwer Road, Dist Indore (MP) Pin 453111
ABSTRACT
The present study was design to evaluate the effect of Buchanania lanzan hydro-alcoholic extract as well as its interaction with conventional anxiolytic and antidepressant drugs using tail suspension test and forced swim test (FST) and to evaluate the possible mechanisms involved in its actions. The rhizomes of Buchanania lanzan were collected and authenticated. Extraction of dried rhizomes was carried out using soxhlet apparatus to obtain its Hydro alcoholic extract. The extract of Buchanania lanzan showed the significant antidepressant activity comparable to the standard drug. The oral administration of Buchanania lanzan extract at 150 mg/ kg and 300 mg/kg respectively as compared to the control treated group showed an antidepressant activity comparable to that of standard drug. The antidepressant effects of Buchanania lanzan extract seem to be mainly associated with the activation of dopamineergic system and possess potential anxiolytic and antidepressant activities.
Keywords: Antidepressant activity, Buchanania lanzan, forced swimming test, tail suspension test.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 23
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 21
HERBAL PLANTS CONTAINING CHOLINESTERASE INHIBITORS ACTIVITY APPROACH FOR MEMORY ENHANCING
Mourya Aman*, Joshi Ankur, Malviya Sapna, & Kharia Anil
Modern institute of Pharmaceutical Sciences, Indore
(Shri Prabhat Chandra Kharia Research and Educational Society)
Alwasa, Behind Rewti Range, Sanwer Road, Dist Indore (MP) Pin 453111
ABSTRACT
Learning is the process of acquisition of information and skills, while subsequent retention of that information is called memory. Learning and memory together called as cognition. Also, memory is a process involving encoding, storing, and recalling information. Thus, memory records various facts and events, make it available for further use, and hence can be considered as most valuable health asset. To elucidate the biochemical and molecular mechanisms underlying learning and memory could be considered as one of the challenging tasks for neuroscientists. Poor memory, lower retention, and slow recall are common problems in today’s stressful and competitive world, especially with associated ageing process. Neurotransmitter modification is an important method for the treatment of memory loss or amnesia. Inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is considered as a promising strategy for the treatment of neurological disorder Amnesia. A potential source of AChE inhibitors is certainly provided by the abundance of plants in nature. This article aims to provide f plants having AChE inhibitory activity. Numerous phytoconstituents and promising plant species as AChE inhibitors are described in this.
Keywords: Acetylcholinesterase, Phytoconstituents, Amnesia
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 24
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 22
A REVIEW: ON MEDICATED TAPE
Gupta Ankit*, Darwhekar G.N.
Acropolis institute of pharmaceutical education and research, Indore
ABSTRACT
Medicated tape (bandage) is the popular for its self-application property. Due to its adhesive property, dose at the site will adhere longer. Medicated tape is widely uses for the wound healing and as a analgesics. The medicated tape is the topical drug delivery system which improves the bioavailability of drug with the help of hydration of skin. Medicated tape has advantage over the non-conscious patients and its self-applicability. Several advantages are their related to medicated tape easy to application, self- application and long duration of action are major advantages. Removal of medicated tape from skin is painful it is a major disadvantage of medicated tape. Medicated tape with controlled amount of drug in each medicated tape is helpful to cure the disease. Medicated tape with lignocaine will reduce the stinging and burning topically which happens by some other drugs.
Keywords: Medicated tape, Medicated tape containing lignocaine, Bandage of lignocaine, Lignocaine
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 25
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 23
CARBON NANOTUBES: A REVIEW
Sharma Avinash*, Sharma Praveen, Darwhekar G.N.
Acropolis Institute of Pharmaceutical Education and Research, Indore
ABSTRACT
The Carbon nanotubes (CNT) are one of the most unique in the field of nanotechnology during last decade. The cylindrical carbon molecules possess novel properties that make them quite useful for many applications in nanotechnology. Carbon nanotubes lie between fullerenes and graphite as a quite new member of allotropes. These allotropes of carbon derived from graphene sheet which exhibit unusual mechanical strength i.e. toughness, elasticity. Nanotubes are classified as single-walled nanotubes and multiple nanotubes. Generally CNTs rolled graphene with SP2 Hybridization. CNTs applied in many field of nanotechnology, nanomedicies, nanoelectronics and biotechnology. Not only in the field of Therapeutics but as well as these CNTs are feasible to the diagnosis purposes. There are various technologies recently developed to synthesize CNTs including Chemical vaporize deposition (CVD), the laser ablation method and sol gel method. Overall CNTs have shown a wide glimpse in the future of nanotechnology and other fields of material science.
Keywords: Carbon nanotubes, synthesis, Single and multiple walled nanotubes.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 26
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 24
ANTIPARASITIC ACTIVITY OF NYCTANTHES ARBOR-TRISTIS LINN. IN MALARIA: "REVERSE PHARMACOLOGY"
A. Nigam*, M. Zaveri, G. Jain, N. Kawathekar
Dept. of Pharmacy, Shri G.S. Institute of Technology and Science,
23-Park Road, Indore (M.P)-452003, India
ABSTRACT
An unceasing threat of drug resistance continuously poses demand for new antimalarial drugs. A scientific assessment of traditionally used antimalarial plants through reverse pharmacology is crucial for a fast track drug discovery. Herbal plant Nyctanthes arbor-tristis Linn. (Parijat) is being used in clinical practice and had shown antimalarial activity, with a parasite clearance in 76.6% of 120 patients, in an earlier clinical study. The objective of this study is to further explore antimalarial potential of the plant through additional objective markers.
Keywords: Malaria, anti-parasitic activity, drug resistance.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 27
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 25
A REVIEW: ON FAST DISINTEGRATING TABLETS
Vishwakarma Beerendra*, Sharma Ravi, Darwhekar G.N.
Acropolis institute of Pharmaceutical Education And Research, Indore
ABSTRACT
Tablet is the most popular among all dosage existing today because of its convenience of self administration, compactness easy administration and manufacturing and fast onset of action is required for conventional therapy. Pharmaceutical research is focused on designing a fast disintegrating tablet is a novel drug delivery system with improved patient compliance and increase bioavailability of poorly water soluble drug. FDTs is solid unit dosage forms which disintegrate or dissolve in saliva within a few second when put on tongue of without need of water. FDTs provide advantages particularly for bedridden, psychiatric, pediatric and geriatric patient. Dysphagia is the most common disadvantages of conventional tablets. The review describe the various formulation aspects superdisintegrants, conventional technology, new patented technology, evaluation test, marketed formulation, suitability of drug candidates and future prospects.
Keywords: Fast disintegrating tablet, conventional technique, superdisintegrants.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 28
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 26
HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY PROCESS AND FUTURE ASPECTS
Qureshi Farhan*, Mule Preeti, Malviya Sapna, Kharia Anil
Modern Institute of Pharmaceutical Sciences, Indore
ABSTRACT
High Throughput Screening (HTS) is a drug-discovery process widely used in the pharmaceutical industry. It leverages automation to quickly assay the biological or biochemical activity of a large number of drug-like compounds. It is a useful for discovering ligands for receptors, enzymes, ion-channels or other pharmacological targets, or pharmacologically profiling a cellular or biochemical pathway of interest. Typically, HTS assays are performed in "automation-friendly". It is a way of rapidly assessing a large number of candidate compounds or genetic modulators to identify active compounds, antibodies or genes which modulate a particular biomolecular pathway. An HTS system generally includes robotic microplate and labware handling systems, liquid handling systems, colony pickers and laboratory instrument control software. The wells in the microplates are filled via the liquid handling systems, and sensors are used to evaluate the samples in the microplate, often after a period of incubation. Laboratory automation software choreographs the entire process, ensuring accuracy within the process and repeatability between processes. High-throughput screening (HTS) allows researchers to quickly and cost-effectively process thousands and even hundreds of thousands (ultra-high-throughput screening, or uHTS) of compounds, which in turn enables them to zero in on hits (compounds that display the desired characteristic) to be advanced into the next stages of drug discovery and development. Ultra-high- throughput screening (uHTS) is an automated methodology for conducting hundreds of thousands of biological or chemical screening tests per day. The cut-off between high-throughput screening (HTS) and uHTS is somewhat arbitrary. The advent of automated plate-handling and reading instrumentation, and the replacement of radiolabeling assays with luminescence- and fluorescence-based screens, created the opportunity for the several-hundredfold improvement in throughput represented by uHTS.
Keywords: HTS, uHTS, Microplate, fluorescence
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 29
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 27
ANTI-ANEMIC ACTIVITY OF HYDRO-ALCOHOLIC LEAF EXTRACT OF TAMARINDUS INDICA IN PHENYLHYDRAZINE INDUCED ANEMIC RATS
Gupta Deepanshu*, Joshi Ankur, Malviya Sapna, & Kharia Anil
Modern institute of Pharmaceutical Sciences, Indore
(Shri Prabhat Chandra Kharia Research and Educational Society)
Alwasa, Behind Rewti Range, Sanwer Road, Dist Indore (MP) Pin 453111
ABSTRACT
The aim of the present study is to evaluate the anti-anemic activity of hydro-alcoholic leaf extract of Tamarindus indica against phenylhydrazine induced hemolytic anemia in rats. Phenylhydrazine (60mg/kg) was administered intraperitoneally for 2 days to induce anemia in rats. The animals were divided in to four groups of 6 animals each. Group I served as normal control, group II as anemic control, group III as reference control administered with Vitamin B12 and group IV animals were treated with 200mg/kg, of hydro-alcoholic leaf extract of Tamarindus indica. All the test drugs were administered once daily for 28 days through oral route. On 29th day blood was withdrawn, through tail puncture under phenobarbitone anesthesia and subjected to the estimation of RBC, Hb and percentage Hematocrit. Both the hydro-alcoholic leaf extract of Tamarindus indica and Vitamin B12 significantly increased the RBC, Hb and Hematocrit levels which conclude that, Tamarindus indica leaf extract exhibits anti-anemic activity.
Keywords: Anemia, Anti-anemic activity, Tamarindus indica and Vitamin B12.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 30
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 28
WNT/Β-CATENIN PATHWAY AS NOVEL TARGET FOR ANTICANCER DRUG DISCOVERY
Rai Abhishek*, Karthikeyan C., Jain Deepti
School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Bhopal.
ABSTRACT
The Wnt/β-catenin pathway plays crucial role in regulating several features of cell cycle progression, apoptosis and the EMT process in many types of cancer cells. Deregulation of Wnt/β-catenin pathway has clear implications in the process of tumorigenesis, CSC, tumor cell invasion and metastasis hence aberrant Wnt/ β-catenin signaling has been implicated in different cancers including familial adenomatous polyposis, sporadic colorectal cancer, hepatocellular carcinomas, pancreatic cancer, prostate cancer, medulloblastoma, hematologic malignancies, breast and pancreatic cancer and sarcomas. Implication of Wnt/β-catenin pathway in such a broad spectrum of cancers defines its importance in anticancer drug discovery. The intricate regulation of β-catenin provides alternative points for therapeutic interventions. Wnt/β-catenin pathway has been targeted at different levels including extracellular and cell membrane level, cytoplasmic level, and nuclear levels. Targeting Wnt/β-catenin pathway for anticancer activity has armed us with some very potent and effective molecules including LGK974, IPWs, NSC668036, OMP- 18R5, IWR1, JW55, JW74, XAV939, IWRs, PKF222-815, iCRT5, ICG-001, AVI-4126, and CCI-779 out of which some are in clinical trials and others have shown promising activities in animal trials and cell line studies.
Keywords: Wnt/β-catenin pathway, Cancer, embryonic pathway, Cancer stem cells.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 31
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 29
IDENTIFICATION OF NOVEL ANTI-INFLAMMATORY AGENTS FOR PREVENTION OF CHRONIC DISEASES: "REVERSE PHARMACOLOGY"
H.Sayyed*, M. Zaveri, G. Jain, N. Kawathekar
Dept. of Pharmacy, Shri G.S. Institute of Technology and Science,
23-Park Road, Indore (M.P)-452003, India
ABSTRACT
Inflammation, although first characterized by Cornelius Celsus, Extensive research within last three decades has confirmed these observations and identified the molecular basis for most chronic diseases and for the associated inflammation. The transcription factor, Nuclear Factor-kappaB (NF-kappaB) that controls over 500 different gene products, has emerged as major mediator of inflammation. Thus agents that can inhibit NF-kappaB and diminish chronic inflammation have potential to prevent or delay the onset of the chronic diseases and further even treat them. In an attempt to identify novel anti-inflammatory agents which are safe and effective, in contrast to high throughput screen, we have turned to "reverse pharmacology" approach. We found that, a science of long life, can serve as a "goldmine" for novel anti- inflammatory agents used for centuries to treat chronic diseases. The current review is an attempt to provide description of various Herbal plants currently used for treatment, their active chemical components, and the inflammatory pathways that they inhibit.
Keywords: Inflammation, transcription factor, reverse pharmacology.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 32
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 30
ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF JUGLANS CINEREA
Sirvi Someshver*, Joshi Ankur, Pathak Vishwas, Malviya Sapna, & Kharia Anil
Modern institute of Pharmaceutical Sciences, Indore
(Shri Prabhat Chandra Kharia Research and Educational Society)
Alwasa, Behind Rewti Range, Sanwer Road, Dist Indore (MP) Pin 453111
ABSTRACT
Analgesic and antipyretic effects of hydroalcholic extract of fruits of Juglans cinerea (Juglandaceae) were investigated at doses 150mg/kg b.w. and 300mg/kg b.w. using acetic-acid induced writhing, hot- plate, tail-clip, formalin and yeast-induced pyrexia tests. Oral administration Juglans cinerea hydro-alcholic extract produced significant (P<0.0001) reduction in no. of writhes induced by acetic-acid. Moreover, in hot-plate test, Juglans cinerea hydro-alcholic extract significantly (P<0.0001) raised the pain threshold at different time of observation (0-60min) in comparison with control. In tail-clip test also the extract caused a significant (P<0.0001) inhibition of pain at both the doses used. There was a significant dose-dependent inhibition of both phases of the formalin induced pain response in mice. Tested on yeast-induced pyrexia in rats, Juglans cinerea hydro-alcholic extract significantly (P<0.0001) reversed hyperthermia at either dose. The results of pharmacological tests performed in the present study suggest that Juglans cinerea hydro-alcholic extract possesses potent analgesic and antipyretic effects.
Keywords: Juglans cinerea, Analgesic activity, Antipyretic activity.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 33
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 31
DEVELOPING AN ANTI-MALARIAL PHYTOMEDICINE THROUGH REVERSE PHARMACOLOGY
Maltare Manobh*, Singh Anamika, Darwhekar G.N.
Acropolis institute of pharmaceutical education and research, Indore
ABSTRACT
Reverse pharmacology is the science of integrating documented clinical/experimental hits into leads by transdisciplinary exploratory studies and further developing these into drug candidates by experimental and clinical research. MALARIA elimination efforts will lead to much wider use of the few currently effective anti-malarial drugs such as artesunate .There is already discussion about intermittent treatment of infants, pregnant women. Resistances already exist to amodiaquine and sp, and will probably increase as a result of increase drug pressure. In this cortex it is important to maximize the lifespan of anti-malarial and for its development the Anti-malarial Phytomedicines are used. A reverse pharmacology approach to developing an anti-malarial phytomedicine was designed and implemented in Mali, resulting in new standardized herbal anti-malarial after six years of research. The first step was to select a remedy for development, through a retrospective treatment-outcome study. The second step was dose escalating clinical trial that showed a dose-response phenomenon and helped select and most efficacious dose. The third step was randomized controlled trial to compare the phytomedicine to standard first-line treatment. The last step was to identify active compounds which can be used as markers for standardization and quality control. This example of reverse pharmacology for an anti-malarial phytomedicine is developed faster, long term and more cheaply than conventional drugs.
Keywords: Reverse pharmacology, Anti-malarial, phytomedicine.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 34
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 32
TARGETING THE MDM2-P53 PROTEIN-PROTEIN INTERACTION FOR NEW CANCER THERAPEUTICS
Trivedi Neha, Karthikeyan Chandrabose, Trivedi Piyush, Maheshwari Neelesh
School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal, Madhya Pradesh.
ABSTRACT
The p53 tumor suppressor protein is a transcriptional factor that plays a key role in regulation of several cellular processes, including the cell cycle, apoptosis, DNA repair, and angiogenesis. The murine double minute 2 (MDM2) protein is the primary cellular inhibitor of p53, functioning through direct interaction with p53. Design of non-peptide, small-molecule inhibitors that block the MDM2-p53 interaction has been sought as an attractive strategy to activate p53 for the treatment of cancer and other human diseases. Major advances have been made in the design of small-molecule inhibitors of the MDM2-p53 interaction in recent years, and several compounds have moved into advanced preclinical development or clinical trials.
Keywords: HDM2 • Inhibitors • MDM2 • Protein-protein interactions.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 35
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 33
AN ARCHETYPE SHIFT FOR MODERN DRUG DEVELOPMENT: AN APPROACH FOR CLINICAL CANDIDATE USING REVERSE PHARMACOLOGY.
Pagare Varnika*, Soni Priyanka, Patidar Archana, Darwhekar G. N.
Acropolis Institute of pharmaceutical Education and Research, Indore.
ABSTRACT
A trans-disciplinary endeavor in the field of drug discovery called reverse pharmacology, also known as target-based drug discovery (TDD), is a hypothesis that involves modulation of the activity of a specific protein target. The approach leverages on chemical and biological information about ligands and/or biological targets to identify and optimize new drugs. This has been made possible by increase identification of molecular targets, elucidation of the 3D structures by X- ray crystallography and nuclear magnetic resonance (NMR), availability of commercial, private or public data bases (of biological targets and ligands) and availability of computer-aided drug design software. Targeting the protein and involvement of CADD is highly beneficial starting point for drug discovery. CADD employs the use of in silico filters to identify hits (active drug candidates), eliminate compounds with undesirable properties (poor activity and/or poor Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET), selects the most promising candidates for further evaluation, and optimizes these leads i.e. transform biologically active compounds into suitable drugs by improving their physicochemical, pharmaceutical, ADMET/PK (pharmacokinetic) properties. It involves Screening of chemical libraries of small molecules which is used to identify compounds that bind with high affinity to the target. The hits from these screens are then used as starting points for desired clinical candidate. Differently than the classical (forward) pharmacology, with the reverse pharmacology approach in vivo efficacy of identified active (lead) compounds is usually performed in the final drug discovery stages.
Keywords: Reverse pharmacology, X- ray crystallography, CADD, data bases.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 36
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 34
COMBINATORIAL CHEMISTRY: “A NOVEL AND EFFICIENT APPROACH IN DRUG DISCOVERY”
PrajapatiPalash*, Muley Preeti, MalviyaSapna, Kharia Anil
Modern Institute of Pharmaceutical Sciences, Indore
ABSTRACT
Combinatorial Chemistry is defined as the systematic and repetitive covalent connection of a set of different ‘building blocks’ of varying structures to each other to yield a large array of diverse molecular entities (libraries) simultaneously. Combinatorial chemistry involves the rapid synthesis or the computer simulation of a large number of different but often structurally related molecules or materials. Combinatorial chemistry is especially common in CADD (Computer Added Drug Design).The logical development of receptor technology is closely connected with the changes in strategy of chemical synthesis. High Throughput Screening provides the most promising substances. The vast number of chemical compounds produced by Combinatorial Chemistry and the possibility of testing many compounds, including natural products, in a short period of time by HTS attracted attention of many workers. It has become possible to use solid- or solution-phase syntheses with different chemistries and scaffolds to produce libraries tailor-made for finding or optimizing a lead directed at almost any class of target. Various detection techniques like Fluorescence resonance energy transfer (FRET), Homogeneous time resolved fluorescence (HTRF), etc are available, and the screening of more than 100,000 samples is per day possible. With the introduction of robotics, automation and miniaturization techniques, it has become feasible to screen 50,000 compounds a day with complex work-stations. Today, Cell-based assays are used in more than half of all High throughput drug screening for target validation and ADMET (Absorption, Distribution, Metabolism, Elimination and Toxicity) in the early stage of drug discovery.
Keywords: Combinatorial chemistry, HTS (High throughput screening), Libraries, Cell-based assays, Miniaturization
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 37
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 35
DIURETIC ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF NYCTANTHES ARBORTRISTIS IN ALBINO RATS
Goud Pawan*, Joshi Ankur, Malviya Sapna, & Kharia Anil
Modern institute of Pharmaceutical Sciences, Indore
ABSTRACT
In the present study hydro-alcoholic extract of Nyctanthes arbortristis was prepared using soxhlets apparatus. Albino rats were divided into 5 groups of 6 rats each. Group-I (Control) received distilled water 25ml/kg orally. Group-II (Standard). received Furosemide 20mg/kg orally. Group-III received hydro-alcoholic extract of Nyctanthes arbortristis 100 mg/kg, Group-IV received hydro-alcoholic extract of Nyctanthes arbortristis 200 mg/kg and Group-V received hydro-alcoholic extract of Nyctanthes arbortristis 400 mg/kg. The urine samples were collected for all the groups upto 5 hours after dosing and urine volume was measured. Urine was analysed for electrolytes (Na+, K+ and Cl-). ANOVA, Dunnet’ s test and p-values were measured and data was analysed. hydro-alcoholic extract of Nyctanthes arbortristis exhibited significant diuretic activity by increasing urine volume and also by enhancing elimination of Sodium (Na+), Potassium (K+) and Chloride (Cl-) at doses of 100 and 200mg/kg. hydro-alcoholic extract of Nyctanthes arbortristis possesses significant diuretic activity.
Keywords: Diuretics, Nyctanthes arbortristi, Furosemide,
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 38
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 36
SUBLINGUAL TABLETS: AN OVERVIEW
Sem Sheetal, Gupta Ashish, Darwhekar G.N.
Acropolis Institute of Pharmaceutical Education and Research, Indore
ABSTRACT
The Demand of Sublingual tablets are growing rapidly now a days for geriatric and pediatric patients suffering from dysphagia. Sublingual administration is most convenient providing ease of administration, painless, enhancing bioavailability. Drug delivery via sublingual route is one of the most promising alternatives that is useful for rapid onset of action with better patient compliance than orally ingested. Sublingual means “under the tongue”, which refers that administering drug through mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. The mechanism involved in drug transfer across the oral mucosa is majorly passive diffusion. Then the drug further diffuses into venous capillary and eventually reaches to the systemic circulation via the jugular vein. In permeability concept, most preferable is sublingual area which is more permeable than buccal and palatal area. The portion of drug which is absorbed through sublingual route avoid hepatic first pass metabolism and enhance the bioavailability of drug. Several techniques can be used to formulate sublingual tablets. The review emphasize on sublingual tablets, factors affecting sublingual absorption, advantages and various evaluation parameters with available marketed formulations.
Keywords: Sublingual tablets, Oral cavity, Enhanced bioavailability, Dysphagia.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 39
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 37
NEW ECO-FRIENDLY TITRIMETRIC ANALYSIS OF ASPIRIN TABLETS USING MIXED HYDROTROPIC SOLUBILISATION
Mishra Smriti *, Maheshwari R.K., Likhar Sumit
Department of Pharmacy, Shri G.S. Institute of Technology and Science, Indore-452003, India
ABSTRACT
In the present study, a blend of 15% w/v sodium salicylate, 5%w/vniacinamide, 5%w/vsodium acetate and 5% w/v sodium citrate is prepared to carry out estimation of aspirin tablets. The solubility of aspirin in distilled water at room temperature was found to be 1.31 mg/ml. The solubility of aspirin was significant in this mixed hydrotropic blend (133.9 mg/ml). The crushed powder of tablets of aspirin were extracted using this blend. The analysis of the drug was done by titrimetric analysis in 0.5M hydrochloric acid. Various organic solvents like methanol, chloroform, dimethyl formamide and ethanol have been employed for solubilisation of poorly water soluble drugs to conduct their titrimetric analysis. This proposed method for analysis is recommended because it eliminates the use of toxic solvents and it is a novel, rapid, accurate and reproducible method that is economic as well. Statistical data proved accuracy, precision and reproducibility of the proposed analytical method.
The proposed method uses the concept of mixed hydrotropy and provides an alternative method of analysis where the toxicity of solvents can be eliminated. Keywords: Mixed hydrotropy, titrimetry, aspirin, sodium salicylate, niacinamide, sodium acetate, sodium citrate.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 40
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 38
TREATMENT OF TUBERCULOSIS FROM DRUG DEVELOPED THROUGH SOIL BACTERIA
Pillai Soniya*, Mishra Priya, Dwivedi Akanksha, Khabiya Rakhi, Darwhekar GN
Acropolis Institute of Pharmaceutical Education and Research, Indore
ABSTRACT
Tuberculosis is very deadly and severely spreading infectious disease, caused by Mycobacterium tuberculosis. In 2015 an estimated 4,80,000 cases were unresponsive to the two major drugs used to treat tuberculosis. It is estimated more than 2,50,000 tuberculosis deaths were from drug resistant infection. Mycobacterium tuberculosis is becoming increasingly resistant to current therapies, indicating an urgent need to develop new and effective tuberculosis drugs.
The review describes the rapid synthesis of analogues of the sansanmycin uridylpeptide natural product. The sansanmycin are produced by the soil bacterium streptomyces species and has a number of interesting structural features that are unique to uridylpeptide natural product family. These natural product analogues disrupt the activity of mycobacterium tuberculosis phospho-MurNAc pentapeptide translocase, the integral membrane enzyme responsible for the biosynthesis of Lipid-I, a key intermediate in mycobacterial peptidoglycan synthesis. These analogs inhibit the action of a key protein needed to build a protective cell wall around the bacterium. Without the cell wall, the bacterium dies. This wall – building protein is not targeted by currently available tuberculosis drugs. Thus through soil bacteria economic and effective treatment of tuberculosis is achievable.
Keywords: Tuberculosis, soil bacteria, sansanmycin uridylpeptide.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 41
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 39
PILOT PLANT DEVELOMENT OF MARIJUANA TAMPONS
Joshi Sunayna *, Dwivedi Akanksha, Darwhekar G.N.
Acropolis Institute of Pharmaceutical Education & Research, Indore. Madhya Pradesh, India.
ABSTRACT
Marijuana is progressively more recognized as an effective medicinal product by both the common public and medical professionals. This abstract is about development of pilot plant of marijuana tampons. They aren’t typically considered as tampons, but they can be used as modified tampons inserted in the form of suppositories. Women who suffer from painful menstrual cramps sympathize with the debilitating discomfort that arrives monthly like clockwork. However, now there’s apparently a new remedy for cramps marijuana tampons Makers of marijuana-infused personal lubricant, created “relief suppositories” made out of Marijuana .these suppositories “maximize the muscle relaxing and pain relieving properties of cannabis without inducing a psychotropic ‘high’. Primary focus is on relieving pain, with an intention to “share the powerful medicinal properties of this plant while utilizing modern extraction techniques to standardize purity and potency.” Creating a tampon, rather than a pill, helps deliver the medicine directly to where it is needed most. These tampons, which cost $44 for a 4-pack, are made with only three ingredients: cocoa butter, distilled THC Oil and CBD Isolate (99.99%) from organically-grown hemp. CBD Isolate is one of “two key active cannabinoid compounds found in cannabis,” the other being THC. Reviewer of the suppositories claims that the pill “smells like cookie dough and cocoa butter.”There’s a catch though—the tampons are only available in for residents of Colorado and for residents of California with a medical marijuana card or physician’s recommendation letter. Manufacturing of marijuana tampons can be achieved at laboratory scale and by feting local entrepreneurs and organizing awareness camps about the effectiveness of these tampons could be briefed. Marketing and selling of marijuana tampons could be started which would ultimately lead a good starter in local markets of India
Keywords: Marijuana tampons, Pain-killing activity, menstrual cramps, organic farming, domestic market.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 42
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 40
DESIGN AND DEVELOPMENT OF MICROEMULSION DRUG DELIVERY SYSTEM OF FELODIPINE FOR IMPROVEMENT OF ORAL BIOAVAILABILITY
Verma Rinku, Darwhekar G.N., Gupta Ashish, Sharma Praveen
Acropolis Institute of Pharmaceutical Education and Research
ABSTRACT
Microemulsion drug delivery system is a novel and versatile approach for overcoming the formulation difficulties of drugs with poor aqueous solubility. The main purpose of this work was to develop an oral microemulsion formulation for enhancing the bioavailability of felodipine. Felodipine is an antihypertensive drug a calcium channel blocker it belongs to BCS classⅡ. It shows extensive first pass metabolism. The bioavailability of felodipine is 15% hence it was suitable candidate for design microemulsion.
The solubility of drug was determined in various oils, surfactants and cosurfactants for selection of components of formulations. Pseudo ternary phase diagram is a useful and important tool to study the phase behaviour of microemulsions Pseudo-ternary phase diagrams were constructed to obtain the appropriate components and their concentration ranges that result in large existence area of microemulsion.
Microemulsion was prepared with 6%Isopropyl Myristate (IPM), 30% Tween 80&10% PEG-400 and54% water respectively. Phase behaviour of the selected components was investigated by construction of ternary phase diagrams. Optimized formulation was evaluated for drug content, zeta potential, droplet size, pH, viscosity, in-vitro drug release profile and stability study. Globule size of optimize batch F3 was found to be 77.57nm. In vitro release study had shown 85.34% drug release from microemulsion which was more compared to pure drug suspension (55.1%).
Keywords: Microemulsion, antihypertensive, pseudo-ternary.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 43
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 41
NEW ECO-FRIENDLY APPLICATION OF MIXED HYDROTROPIC SOLUBILISATION FOR TITRIMETRIC ANALYSIS OF ACECLOFENAC TABLETS
Goyal Sunil *, Shah Mitali, Maheshwari, R.K.
Department of Pharmacy, Shri G.S. Institute of Technology and Science, Indore-452003, India
ABSTRACT
In the present study, a blend of 20% w/v sodium benzoate and 10% w/v niacinamideis prepared to carry out estimation of aceclofenac tablets. The solubility of aceclofenac in distilled water at room temperature was found to be0.11 mg/ml. The solubility of aceclofenac was significant in this mixe hydrotropic blend (108.8 mg/ml). The crushed powder of the tablets of aceclofenac were extracted using this blend. The analysis of the drug was done by titrimetric analysis in 0.1 N NaOH solution. Various organic solvents like methanol, chloroform, dimethyl formamide and ethanol have been employed for solubilisation of poorly water soluble drugs to conduct their titrimetric analysis. This proposed method for analysis is recommended because it eliminates the use of toxic solvents and it is a novel, rapid, accurate and reproducible method that is economic as well. Statistical data proved accuracy, precision and reproducibility of the proposed analytical method.
The proposed method uses the concept of mixed hydrotropy and provides an alternative method of analysis where the toxicity of solvents can be eliminated.
Keywords: Mixed hydrotropic solubilsation, titrimetry, aceclofenac, sodium benzoate, niacinamide.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 44
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 42
MEMORY ENHANCING ACTIVITY OF BUCHANANIA LANZAN BY SCOPOLAMINE INDUCED AMNESIA IN RATS
Shekar Priyanshu*, Joshi Ankur, Malviya Sapna, & Kharia Anil
Modern Institute of Pharmaceutical Sciences, Indore
ABSTRACT
The present study was undertaken to investigate the effect of Buchanania lanzan on cognitive functions, total cholesterol levels and cholinesterase (ChE) activity in scopolamine-induced amnesia in rats. The paste of Buchanania lanzan was administered orally at three doses (150, 300 and 600 mg/kg) for 7 and 14 consecutive days to the respective groups of rats. Piracetam (200 mg/kg) was used as a standard nootropic agent. Learning and memory parameters were evaluated using elevated plus maze (EPM), passive avoidance and motor activity paradigms. Brain ChE activity and serum biochemical parameters like total cholesterol, total triglycerides and glucose were evaluated. It was observed that Buchanania lanzan at the above-mentioned doses after 7 and 14 days of administration in the respective groups significantly reversed scopolamine (1 mg/kg i.p.)-induced amnesia, as evidenced by a decrease in the transfer latency in the EPM task and step-down latency in the passive avoidance task. Buchanania lanzan reduced the brain ChE activity in rats. Buchanania lanzan also exhibited a remarkable cholesterol and triglyceride lowering property and slight increase in glucose levels in the present study.
Keywords: Alzheimer’s disease, amnesia, Buchanania lanzan, scopolamine
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 45
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 43
A REVIEW: ON GASTRORESISTENT MICROPARTICLES CONTAINING SODIUM-PANTOPRAZOLE: STABILITY STUDIES AND IN-VIVO ANTIULCER ACTIVITY
Yadav Priyanka, Darwhekar G.N.
Acropolis institute of Pharmaceutical Education And Research, Indore
ABSTRACT
The aim of the present work was to verify the in-vivo capability of pantoprazole –loaded microparticles to protect the gastric mucosa against ulcer formulation and evaluate their stability under accelerated conditins. Pentoprazole is a proton pump inhibitor used in the treatment of gastric ulcer, gastroesophageal reflux disease and Helicobactor pylori infections associated to other diseases and the pantoprazole-loaded microparticles were prepared by spray-drying in pilot scale, using Eudragit® S100 as polymer. Transparent glass vials containing drug-loaded microparticals were stored for 6 months at 40˚C and 75% RH. Photostabilty was tested under UVA light. Ulcers were induced by the oral administration of absolute ethanol to rats. Regarding the drug content during the accelerate stability study, samples showed complete encapsulation efficiency and were considered stable. The microencapsulation of pantoprazole reduced its photodegradation. The in vivo evaluation showed that the microparticles presented ulcers index lower than the solutions. Enteric microparticles had acceptable stability under accelerated conditions and were efficient in protecting the stomach against ulceration caused by ethanol.
Keywords: proton pump inhibitor, Helicobactor pylori, enteric microparticles.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 46
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 44
5 ACETIC ACID PEPTIDE HYBRID DERIVATIVES AS POTENT ANTIDIABETIC AGENTS "REVERSE PHARMACOLOGY"
Sharma R*, Zaveri M., Kawathekar N, Jain G
Department of Pharmacy, Shri G. S. Institute of Technology & Sciences,
ABSTRACT
The present investigation is concerned with the docking study of Thiazolidinedione 5acetic acid peptide hybrid derivative, with the aim of discovering novel and potent anti-diabetic agent. In this study the flexible ligand docking simulation was performed on Thiazolidinedione 5 acetic acid peptide hybrid derivative against PPAR-ϒ agonist with PDB ID – 2POB using Glide v 5.6 of Schrodinger and LLC. All the compounds show good Glide score compared to the class of thiazolidinedione (Rosiglitazone) as standard drug. The derivative of 5 acetic acid peptide hybrid shows highest GLIDE score (-10.072) compared to standard drug (-9.321). The designed compound shows Hydrogen bond interaction via Val 95 and Tyr 95 residues were found to play significant role in binding.
Keywords: reverse pharmacology, anti-diabetic agent, Thiazolidinedione, PPAR-ϒ.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 47
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 45
NOVEL CARBAZOLE TETHERED PYRROLE DERIVATIVES AS POTENT INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS "REVERSE PHARMACOLOGY"
Adhav Rohit, Zaveri M, Jain G, Kawathekar N
Department of Pharmacy, Shri G.S. Institute of Technology and Science,
ABSTRACT
Tuberculosis (TB) is a highly dangerous infectious disease caused by the bacterial pathogen Mycobacterium tuberculosis (Mtb). Amongst the worldwide health threats, TB continued to remain as second leading cause of mortality from a single infectious disease. In 2012 alone, nearly 1.3 million fatalities are due to TB and over 95% of them are occurred in low- and middle income countries. Further TB threat has acquired a new dimension with the emergence of both multidrug- resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB).Recent focus in the tubercular drug research is on the development of agents inhibiting the enzyme targets involved in potential role in the life cycle of the pathogen. Inh A, the enoyl acyl carrier protein reductase from Mycobacterium tuberculosis is one of the key enzymes involved in the mycobacterial fatty acid elongation cycle and has been considered as a promising target in antitubercular screening. Inhibition of Inh A disrupts the biosynthesis of the mycolic acids that are central constituents of the mycobacterial cell wall. Docking was performed against enoyl acyl carrier protein reductase protein (PDB ID: 4TZK) and enoyl acyl carrier protein reductase transpeptidase (PDB ID: 2H7M) using the GLIDE molecular docking tool implemented in the Schrodinger software.
Keywords: Tuberculosis, multidrug- resistant TB, Inh A, Docking, pyrrole
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 48
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 46
ANTI-DIABETIC EFFECT OF MAHANIMBINE FROM MURRAYA KOENIGII: REVERSE PHARMACOLOGY
Shidhaye Supriya*, Mishra Kamlendra, Mahajan S. C.
Mahakal Institute of Pharmaceutical Studies, Ujjain
ABSTRACT
Reverse pharmacology is defined as the modern technique of drug discovery, which integrates documented clinical/experimental data into leads by transdisciplinary exploratory studies and further develops it into promising drug candidate and then in form of formulation by experimental and clinical research. RP is comparatively safer and better way of drug discovery because it is based on the knowledge of traditional, folk and ayurvedic use of medicinal plants. Traditional knowledge can help to eliminate three main hurdles in drug development these are time, money and safety/toxicity. In general, path of drug discovery starts with research in laboratory and ends with the effect in human volunteer but in reverse pharmacology westarts from patient and then go to the laboratory for finding the pharmacologically active molecule. There is need to understand and execute the basic principles of ayurveda in a scientific manner that is RP, in order to integrate safe, effective and promising use of medicinal plants. Here we discus reverse pharmacological approach for treatment of diabetes with special reference to antidiabetic molecule mahanimbine from medicinal plant Murraya koenigii.
Keywords: Reverse pharmacology, ayurveda, antidiabetic, Murraya koenigii.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 49
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 47
NATURAL GUMS AS SUPERDISINTEGRANTS IN FORMULATION OF MOUTH DISSOLVING TABLETS- A REVIEW
Thakur Sovran S *, Niranjan Swatantra, Verma Kaushilya, Chatterjee D. P.
Mittal Institute of Technology, Bhopal
ABSTRACT
The aim is to study the use of natural gums as natural superdisintegrants in formulation of mouth dissolving tablets. Fast disintegrating tablet have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical area. Particularly the fast dissolving drug delivery systems formulated with natural polymers have more demand because natural materials like gums and mucilage have been extensively used in the field of drug delivery for their easy availability, ease of administration, non-toxicity, non-irritant nature, biodegradability etc. Mouth dissolving tablets with natural gums and mucilage generally show better disintegrating property as well as release profile. Tablets which needs rapid disintegration, the inclusion of the right disintegrant is a prerequisite for optimal bioavailability. So superdisintegrants are used to improve the efficacy of such solid dosage forms. Use of natural gums as such disintegrants is rapidly increasing nowadays. Hence it can be concluded that natural gums can be efficiently used as natural superdisintegrants with many advantages over synthetic superdisintegrants in formulation of mouth dissolving tablets.
Keywords: natural gums, superdisintegrants, mouth dissolving tablets, drug delivery.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 50
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 48
ADR IN HERBAL MEDICATION WITH MAINSTREAM MEDICAL THERAPIES
Sharma Garima *, Chhajed Mahavir, Prachand Sumeet, Jain Sanjay
Indore Institute of Pharmacy, Indore
ABSTRACT
Natural health products (NHPs) are sold over-the-counter and are often perceived to be safe, despite potential risks. In India and China and some other countries, the use of herbal medication is to large extent because of their easy availability, no expert consultation needed, and considered safe to use and also because primary health care services fall short to the peoples need. Proper reporting of suspected ADR of herbal medicines is of great significance. The marketed Ayurvedic and other CAM medicines should be FDA approved and need to increase public awareness about pros and cons of their uses. We need to focus on the common belief that anything natural is safe is a fallacious statement. The manufacturers of herbal medicines are not required to submit the proof of safety and efficacy with rigorous analysis to the FDA before marketing. For this reason, the adverse effects and drug interactions associated with herbal remedies are largely unknown. Thus, some of the adverse effects and drug interactions reported for herbal products could be caused by impurities (e.g., allergens, pollen and spores). Ginkgo biloba extract, has been reported to cause spontaneous bleeding, and it may interact with anticoagulants and antiplatelet agents, and as a matter of fact Green Tea also have Stimulant drugs speed up the nervous system. Caffeine (contained in green tea) and ephedrine are both stimulant drugs. Taking green tea along with ephedrine might cause too much stimulation and sometimes serious side effects and heart problems. So Perception that natural safe should be seen in a new light Interest and information on alternative therapies is also need to be explore more due to lack of regulation &Information on use of these therapies must be specifically elicited from patients
Keywords: Natural health products, Ayurvedic & CAM medicines, drug interactions.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 51
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 49
ISOLATION OF AMYLASE PRODUCING BACTERIA FROM SOIL AND ITS OPTIMIZATION OF
PRODUCTION PARAMETERS BY SHAKE FLASK CULTURE METHOD
Nair Nidhi *, Chhajed Mahavir, Khambete Hemant, Jain Sanjay
Indore Institute of Pharmacy Indore
ABSTRACT
The effects of various production parameters such as pH, temperature, incubation time and sources of carbon were tested in submerged fermentation process by shake flask culture method in production of amylase by bacteria isolated from groundnut field soil. The production medium with provision of glucose as carbon source, incubated for 48 h, maintained with pH of 6.5 at 39oC, was found optimal for production of amylase.
Keywords: amylase, shake flask culture, starch agar plate, fermentation.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 52
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 50
CUTTING EDGE IN DRUG DISCOVERY AND DEVELOPMENT – REVERSE PHARMACOLOGY
Kachchawala Mehazabeen*, Chhajed Mahavir, Dumbwani Jacky, Jain Sanjay
Indore Institute of Pharmacy, Indore
ABSTRACT
A synthetic discovery is always a first recognition of an event, a phenomenon, process, or a state of affairs not previously recognized or known. Most of the stirring and deeply influential discoveries of science come under this heading. Reverse pharmacology is the science of integrating documented clinical/experimental hits, into leads by trans-disciplinary exploratory studies and further developing these into drug candidates by experimental and clinical research. To discover and develop numerous novel therapeutic agents for the treatment of a wide spectrum of diseases, scientists launched a significant and noticeable effort aimed at improving the integration of discovery technologies, chemical sourcing for route selection/delivery of active pharmaceutical ingredients. However, recent trends indicate that this model may no longer ensure high growth rates. R&D expenses have risen enormously in last decade but surprisingly it has not led to a corresponding increase in the number and efficacy of new drugs. And so numbers of approved new chemical/molecular entities are declining. The extremely time consuming, complex and capital- intensive process makes companies ‘target rich’ but ‘lead poor’. Alternatively, Reverse Pharmacology also known as Target base Drug Discovery (TDD) is now becoming a popular option in the field of drug discovery where a hypothesis is first made that modulation of the activity of a specific protein target will have beneficial therapeutic effects. Screening of chemical libraries of small molecules is then used to identify compounds that bind with high affinity to the target. The hits from these screens are then used as starting points for drug discovery. This method became popular after the sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins.
Keywords: drug discovery, reverse pharmacology, Target base Drug Discovery, chemical libraries
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 53
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 51
INHIBITION OF MATRIX METALLOPROTEINASE – 2 (MMP) IN DMH INDUCED COLON CANCER IN SD RATS IN THE PRESENCE OF DIETARY SUPPLEMENTS AND CHEMOTHERAPY: A MECHANISM AND PROBLEMS BASED APPROACH
Hakimi Taha *, Gupta Saurabh, Chhajed Mahavir, Patidar Shivangi
Indore institute of Pharmacy, Indore
ABSTRACT
Naringenin (NRG), chemically flavonoid is potentially antioxidant and chemoprotective agent. In abundance, this molecule found in citrus fruits like Citrus paradise and Citrus Sinensis. NRG evaluated against paclitaxel (PCT) and cisplatin (CPT) in inhibiting Matrix Metalloproteinase-2 (MMP-2) and angiogenesis along with oxidative stress, nephrotoxicity and bone marrow toxicity in colon cancer induced SD rats. The tested drugs ({PCT (6mg/kg) CPT (4mg/kg)} PCT.CPT, {PCT (6mg/kg) CPT (4mg/kg) NRG (40mg/kg)} PCT.CPT.NRG and NRG (40mg/kg)) were administered p.o. at 50th day after the challenge of 40mg/kg p. o. Di –Methyl Hydrazine (DMH) schedule. Different haematological parameters like Hemoglobin, total and differential leucocytes count, blood urea nitrogen were estimated in Blood. The other parameters, lipid Peroxidation (LPO), Malonaldehyde (MDA), Superoxide Dismutase (SOD) and Clastogenic activity by Micronuclei assay are estimated in kidney. Further, MMP-2 estimation was done in colon tissue preparation. The results reveal a significant increase in hemoglobin, total and differential leucocytes count, blood urea nitrogen in PCT.CPT.NRG treated group. The present investigations suggest that naringenin showed to have protected against the toxic effects of paclitaxel and cisplatin at tested doses. The chemoprotective effect of these compounds could be due to antioxidant mechanism. Further, research in MMP-2 expression with probable scope to quantify the extent of expression of the gene and to identify the relationship with angiogenesis in the tumor.
Keywords: Naringenin, Paclitaxel, Cisplatin and Matrix Metalloproteinase-2.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 54
Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges & Opportunities
PP - 52
IN VITRO ANTI OXIDANT ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF CAESALPINIA BONDUC
Koka Sweta S *, Bankar Amit
LNCP, Indore
ABSTRACT
Present study deals with the In vitro Anti oxidant activity of hydro alcoholic extract of Caesalpinia bonduc commonly known as sagargota belongs to the family. Hydro alcoholic extract of Caesalpinia bondu c was subjected to In vitro antioxidant activity screening models such as DPPH, ABTS radical scavenging activity, inhibition of Lipid peroxidation where Gallic acid, Butylated Hydroxy Toulene (BHT) and Ascorbic acid were used as the standards. In all the models studied, hydro alcoholic extract of Caesalpinia bonduc showed nearly equal activities to standards used. In conclusion, the present study approved that the Caesalpinia bonduc extract have promising In- vitro antioxidant activity.
Keywords: Caesalpinia bonduc, DPPH, ABTS, Lipid peroxidation.
Acropolis Institute of Pharmaceutical Education & Research, Indore Page 55
www.aiper.ac.in
ACROPOLIS INSTITUTE OF PHARMACEUTICAL EDUCATION & RESEARCH
Acropolis Institute of Pharmaceutical Education & Research (AIPER) is nurtured by Teach For India Education & Research Society having objective of creating state of art, world class, high quality technical education facilities at Indore. Towards fulfilment of its objective society established AIPER in the year 2008.AIPER is a philanthropic organization sprawled in an area of around 2 acres and is committed to the service of humanity through technological advancement. The institute offers Masters degree in Pharmaceutics and Bachelor’s degree in Pharmacy. The institute is approved by AICTE, New Delhi , PCI, CPCSEA and is affiliated to Rajiv Gandhi Technical University (RGPV), Bhopal.
Acropolis Institute of Pharmaceutical Education and Research Indore Dewas Bypass Road, Manglia Square, Indore, M.P. 453771 Email Id: [email protected] Contact Details: 0731-4730091, 9630080804