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INVESTIGATION of NATURAL PRODUCT SCAFFOLDS for the DEVELOPMENT of OPIOID RECEPTOR LIGANDS by Katherine M
INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS By Katherine M. Prevatt-Smith Submitted to the graduate degree program in Medicinal Chemistry and the Graduate Faculty of the University of Kansas in partial fulfillment of the requirements for the degree of Doctor of Philosophy. _________________________________ Chairperson: Dr. Thomas E. Prisinzano _________________________________ Dr. Brian S. J. Blagg _________________________________ Dr. Michael F. Rafferty _________________________________ Dr. Paul R. Hanson _________________________________ Dr. Susan M. Lunte Date Defended: July 18, 2012 The Dissertation Committee for Katherine M. Prevatt-Smith certifies that this is the approved version of the following dissertation: INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS _________________________________ Chairperson: Dr. Thomas E. Prisinzano Date approved: July 18, 2012 ii ABSTRACT Kappa opioid (KOP) receptors have been suggested as an alternative target to the mu opioid (MOP) receptor for the treatment of pain because KOP activation is associated with fewer negative side-effects (respiratory depression, constipation, tolerance, and dependence). The KOP receptor has also been implicated in several abuse-related effects in the central nervous system (CNS). KOP ligands have been investigated as pharmacotherapies for drug abuse; KOP agonists have been shown to modulate dopamine concentrations in the CNS as well as attenuate the self-administration of cocaine in a variety of species, and KOP antagonists have potential in the treatment of relapse. One drawback of current opioid ligand investigation is that many compounds are based on the morphine scaffold and thus have similar properties, both positive and negative, to the parent molecule. Thus there is increasing need to discover new chemical scaffolds with opioid receptor activity. -
Opportunities and Pharmacotherapeutic Perspectives
biomolecules Review Anticoronavirus and Immunomodulatory Phenolic Compounds: Opportunities and Pharmacotherapeutic Perspectives Naiara Naiana Dejani 1 , Hatem A. Elshabrawy 2 , Carlos da Silva Maia Bezerra Filho 3,4 and Damião Pergentino de Sousa 3,4,* 1 Department of Physiology and Pathology, Federal University of Paraíba, João Pessoa 58051-900, Brazil; [email protected] 2 Department of Molecular and Cellular Biology, College of Osteopathic Medicine, Sam Houston State University, Conroe, TX 77304, USA; [email protected] 3 Department of Pharmaceutical Sciences, Federal University of Paraíba, João Pessoa 58051-900, Brazil; [email protected] 4 Postgraduate Program in Bioactive Natural and Synthetic Products, Federal University of Paraíba, João Pessoa 58051-900, Brazil * Correspondence: [email protected]; Tel.: +55-83-3216-7347 Abstract: In 2019, COVID-19 emerged as a severe respiratory disease that is caused by the novel coronavirus, Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). The disease has been associated with high mortality rate, especially in patients with comorbidities such as diabetes, cardiovascular and kidney diseases. This could be attributed to dysregulated immune responses and severe systemic inflammation in COVID-19 patients. The use of effective antiviral drugs against SARS-CoV-2 and modulation of the immune responses could be a potential therapeutic strategy for Citation: Dejani, N.N.; Elshabrawy, COVID-19. Studies have shown that natural phenolic compounds have several pharmacological H.A.; Bezerra Filho, C.d.S.M.; properties, including anticoronavirus and immunomodulatory activities. Therefore, this review de Sousa, D.P. Anticoronavirus and discusses the dual action of these natural products from the perspective of applicability at COVID-19. -
A Review on Amentoflavone
Indo American Journal of Pharmaceutical Research, 2017 ISSN NO: 2231-6876 A REVIEW ON AMENTOFLAVONE * Aroosa Siddique , Madiha Jabeen, Osman Ahmed Department of Pharmaceutical Chemistry, Deccan School of Pharmacy, Hyderabad, T.S. ARTICLE INFO ABSTRACT Article history Amentoflavone, is a bioflavonoid constituent of some of flora which includes ginkgo biloba, Received 06/02/2017 hypericum perforatum. It can have interaction with many medicinal drugs by using being a Available online potent inhibitor of CYP3A4 and CYP2C9 which are enzymes chargeable for the metabolism 28/02/2017 of some drugs in the body. Flavonoids exhibit a extensive variety of activities including antioxidant, antiviral, Antibacterial and anticancer pastime. As formerly we showed that Keywords amentoflavone is an activator of hPPARγ. Human PPARγ (hPPARγ) regulates the Amentoflavone, proliferation, apoptosis, and various human most cancers cells. Activated hPPARγ has both Flavonoid, tumor suppressor and tumor promoter. To affirm the mechanism of motion of amentoflavone Synthetic, in most cancers cells, we analyzed whether or not amentoflavone remedy affects the RSV, Hpparγ, appearance of hPPARy the use of opposite transcription polymerase chain response and CYP3A4 & CYP2C9. actual time quantitive PCR. Amentoflavone is synthesized with the aid of way of three techniques i.e natural, semi synthetic and synthetic methods. Among this synthetic method is widely used industrially. Application of the Suzuki-Miyaura response within the synthesis of flavonoids, is of vital magnificence of natural merchandise, is studied. Amentoflavone and three different flavonoids were separated from the ethanol extract of Selaginella sinensis. Amentoflavone show strong antiviral pastime in opposition to respiratory syncytial virus (RSV). The cytotoxic interest of amentoflavone is examined against 5 human most cancers cell strains (MCF-7, A549, HeLa, MDA-MB231, and PC3) treating with tetrazolium- primarily based colorimetric MTT assay. -
Medicinal Plants As Sources of Active Molecules Against COVID-19
REVIEW published: 07 August 2020 doi: 10.3389/fphar.2020.01189 Medicinal Plants as Sources of Active Molecules Against COVID-19 Bachir Benarba 1* and Atanasio Pandiella 2 1 Laboratory Research on Biological Systems and Geomatics, Faculty of Nature and Life Sciences, University of Mascara, Mascara, Algeria, 2 Instituto de Biolog´ıa Molecular y Celular del Ca´ ncer, CSIC-IBSAL-Universidad de Salamanca, Salamanca, Spain The Severe Acute Respiratory Syndrome-related Coronavirus 2 (SARS-CoV-2) or novel coronavirus (COVID-19) infection has been declared world pandemic causing a worrisome number of deaths, especially among vulnerable citizens, in 209 countries around the world. Although several therapeutic molecules are being tested, no effective vaccines or specific treatments have been developed. Since the COVID-19 outbreak, different traditional herbal medicines with promising results have been used alone or in combination with conventional drugs to treat infected patients. Here, we review the recent findings regarding the use of natural products to prevent or treat COVID-19 infection. Furthermore, the mechanisms responsible for this preventive or therapeutic effect are discussed. We conducted literature research using PubMed, Google Scholar, Scopus, and WHO website. Dissertations and theses were not considered. Only the situation Edited by: Michael Heinrich, reports edited by the WHO were included. The different herbal products (extracts) and UCL School of Pharmacy, purified molecules may exert their anti-SARS-CoV-2 actions by direct inhibition of the virus United Kingdom replication or entry. Interestingly, some products may block the ACE-2 receptor or the Reviewed by: Ulrike Grienke, serine protease TMPRRS2 required by SARS-CoV-2 to infect human cells. -
General Guidelines for Drug Development of Ayurvedic Formulations
GUIDELINES SERIES-I GENERAL GUIDELINES FOR DRUG DEVELOPMENT OF AYURVEDIC FORMULATIONS CENTRAL COUNCIL FOR RESEARCH IN AYURVEDIC SCIENCES Ministry of AYUSH, Government of India New Delhi Illllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllll GENERAL GUIDELINES FOR DRUG DEVELOPMENT OF AYURVEDIC FORMULATIONS Volume - 1 CENTRAL COUNCIL FOR RESEARCH IN AYURVEDIC SCIENCES Ministry of AYUSH, Govt, of India New Delhi Miiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiiii Illllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllllll © Central Council for Research in Ayurvedic Sciences Ministry of AYUSH, Government of India, New Delhi - 110058 First Edition - 2018 Publisher: Central Council for Research in Ayurvedic Sciences, Ministry of AYUSH, Government of India, New Delhi, J. L. N. B. C. A. H. Anusandhan Bhavan, 61-65, Institutional Area, Opp. D-Block, Janakpuri, New Delhi - 110 058, E-mail: [email protected], Website : www.ccras.nic.in Disclaimer: All possible efforts have been made to ensure the correctness of the contents. However Central Council for Research in Ayurvedic Sciences, Ministry of AYUSH, shall not be accountable for any inadvertent error in the content. Corrective measures shall be taken up once such errors are brought to notice. ISBN : 978-93-83864-23-2 Other Related -
Effect of Byrsonima Crassa and Phenolic Constituents on Helicobacter Pylori-Induced Neutrophils Oxidative Burst
Int. J. Mol. Sci. 2012, 13, 133-141; doi:10.3390/ijms13010133 OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 www.mdpi.com/journal/ijms Article Effect of Byrsonima crassa and Phenolic Constituents on Helicobacter pylori-Induced Neutrophils Oxidative Burst Cibele Bonacorsi 1, Maria Stella G. Raddi 1,*, Luiz Marcos da Fonseca 1,*, Miriam Sannomiya 2 and Wagner Vilegas 3 1 School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, 14801-902, Brazil; E-Mail: [email protected] 2 School of Arts, Sciences and Humanities, University of São Paulo (USP), São Paulo, SP, 03828-000, Brazil; E-Mail: [email protected] 3 Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14800-900, Brazil; E-Mail: [email protected] * Authors to whom correspondence should be addressed; E-Mails: [email protected] (M.S.G.R.); [email protected] (L.M.F); Tel.:+55-16-3301-5720; Fax: +55-16-3322-0073. Received: 29 August 2011; in revised form: 28 November 2011 / Accepted: 13 December 2011 / Published: 23 December 2011 Abstract: Byrsonima crassa Niedenzu (Malpighiaceae) is used in Brazilian folk medicine for the treatment of diseases related mainly to gastric ulcers. In a previous study, our group described the gastric protective effect of the methanolic extract from the leaves of B. crassa. The present study was carried out to investigate the effects of methanolic extract and its phenolic compounds on the respiratory burst of neutrophils stimulated by H. pylori using a luminol-based chemiluminescence assay as well as their anti-H. pylori activity. -
Assessment of Anti-Inflammatory Effects of Japanese Kampo Medicine and Functional Foods
Functional Foods in Health and Disease 2019; 9(2): 79-91 Page 79 of 91 Review Article Open Access Assessment of anti-inflammatory effects of Japanese Kampo medicine and functional foods Mikio Nishizawa1, Tadayoshi Okumura2,3, and Yukinobu Ikeya4 1Department of Biomedical Sciences, College of Life Sciences, Ritsumeikan University, Kusatsu, Shiga, 525-8577, Japan; 2Research Organization of Science and Technology, Ritsumeikan University, Kusatsu, Shiga, 525-8577, Japan; 3Department of Surgery, Kansai Medical University, Hirakata, Osaka, 573-1010, Japan; 4Department of Pharmacy Educational Assist Center, Daiich University of Pharmacy, Minami-ku, Fukuoka, 815-8511, Japan Corresponding author: Mikio Nishizawa, M.D., Ph.D., Department of Biomedical Sciences, College of Life Sciences, Ritsumeikan University, 1-1-1 Nojihigashi, Kusatsu, Shiga, 525- 8577, Japan. Submission Date: October 3rd, 2018, Acceptance Date: February 25th, 2019, Publication Date: February 28th, 2019 Citation: Nishizawa M., Okumura T., Ikeya Y. Comparison of anti-inflammatory effects of Japanese Kampo medicine and functional foods. Functional Foods in Health and Disease 2019; 9(2): 79-91. DOI: https://doi.org/10.31989/ffhd.v9i2.566 ABSTRACT Traditional Japanese drugs called Kampo medicine are widely used in Japan. Each Kampo medicine consists of several crude drugs, most of which are derived from medicinal plants. Clinical administration has empirically evaluated the effects of Kampo medicine. In contrast, functional foods are prepared from foods and edible plants (e.g., herbs, vegetables, and fruits). Due to the relatively low content of pharmacologically active constituents in functional foods, their effectiveness has not been well evaluated and thus should be better investigated. Kampo medicine and functional foods have beneficial effects for humans, and many of them exhibit anti-inflammatory effects. -
The Practice and Regulatory Requirements Of
School of Public Health The Practice and Regulatory Requirements of Naturopathy and Western Herbal Medicine Vivian Lin Alan Bensoussan Stephen P. Myers Pauline McCabe Marc Cohen Sophie Hill Genevieve Howse November, 2005 Funded by the Department of Human Services, Victoria Copyright State of Victoria, Department of Human Services, 2006 This publication is copyright. No part may be reproduced by any process except in accordance with the provisions of the Copyright Act 1968 (Cth). Authorised by the State Government of Victoria, 50 Lonsdale Street Melbourne. This document may be downloaded from the following website: www.health.vic.gov.au/pracreg/naturopathy.htm ISBN-13: 978-0-9775864-0-0 ISBN-10: 0-9775864-0-5 Published by School of Public Health, La Trobe University Bundoora Victoria, 3086 Australia THE PRACTICE AND REGULATORY REQUIREMENTS OF NATUROPATHY AND WESTERN HERBAL MEDICINE CONTENTS VOLUME ONE Summary Report..........................................................................................................1 1. Introduction.......................................................................................................1 2. Methodology.....................................................................................................1 3. Key findings and recommendations..................................................................2 3.1 Definition of practice and scope of study ........................................................2 3.2 Growing use of naturopathy and WHM...........................................................3 -
Complementary and Alternative Medicine Table of Contents Related Coverage Resources
Medical Coverage Policy Effective Date ............................................. 2/15/2021 Next Review Date ....................................... 2/15/2022 Coverage Policy Number .................................. 0086 Complementary and Alternative Medicine Table of Contents Related Coverage Resources Overview.............................................................. 1 Acupuncture Coverage Policy .................................................. 1 Atherosclerotic Cardiovascular Disease Risk General Background ........................................... 3 Assessment: Emerging Laboratory Evaluations Medicare Coverage Determinations .................. 36 Attention-Deficit/Hyperactivity Disorder (ADHD): Coding/Billing Information ................................. 37 Assessment and Treatment References ........................................................ 39 Autism Spectrum Disorders/Pervasive Developmental Disorders: Assessment and Treatment Biofeedback Chiropractic Care Drug Testing Hyperbaric and Topical Oxygen Therapies Physical Therapy INSTRUCTIONS FOR USE The following Coverage Policy applies to health benefit plans administered by Cigna Companies. Certain Cigna Companies and/or lines of business only provide utilization review services to clients and do not make coverage determinations. References to standard benefit plan language and coverage determinations do not apply to those clients. Coverage Policies are intended to provide guidance in interpreting certain standard benefit plans administered by Cigna Companies. Please -
Roth 04 Pharmther Plant Derived Psychoactive Compounds.Pdf
Pharmacology & Therapeutics 102 (2004) 99–110 www.elsevier.com/locate/pharmthera Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery Bryan L. Rotha,b,c,d,*, Estela Lopezd, Scott Beischeld, Richard B. Westkaempere, Jon M. Evansd aDepartment of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH, USA bDepartment of Neurosciences, Case Western Reserve University Medical School, Cleveland, OH, USA cDepartment of Psychiatry, Case Western Reserve University Medical School, Cleveland, OH, USA dNational Institute of Mental Health Psychoactive Drug Screening Program, Case Western Reserve University Medical School, Cleveland, OH, USA eDepartment of Medicinal Chemistry, Medical College of Virginia, Virginia Commonwealth University, Richmond, VA, USA Abstract Because psychoactive plants exert profound effects on human perception, emotion, and cognition, discovering the molecular mechanisms responsible for psychoactive plant actions will likely yield insights into the molecular underpinnings of human consciousness. Additionally, it is likely that elucidation of the molecular targets responsible for psychoactive drug actions will yield validated targets for CNS drug discovery. This review article focuses on an unbiased, discovery-based approach aimed at uncovering the molecular targets responsible for psychoactive drug actions wherein the main active ingredients of psychoactive plants are screened at the ‘‘receptorome’’ (that portion of the proteome encoding receptors). An overview of the receptorome is given and various in silico, public-domain resources are described. Newly developed tools for the in silico mining of data derived from the National Institute of Mental Health Psychoactive Drug Screening Program’s (NIMH-PDSP) Ki Database (Ki DB) are described in detail. -
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI Chemical Activity Count (+)-AROMOLINE 1 (+)-CATECHIN 5 (+)-GALLOCATECHIN 1 (+)-HERNANDEZINE 1 (+)-PRAERUPTORUM-A 1 (+)-SYRINGARESINOL 1 (+)-SYRINGARESINOL-DI-O-BETA-D-GLUCOSIDE 1 (-)-ACETOXYCOLLININ 1 (-)-APOGLAZIOVINE 1 (-)-BISPARTHENOLIDINE 1 (-)-BORNYL-CAFFEATE 1 (-)-BORNYL-FERULATE 1 (-)-BORNYL-P-COUMARATE 1 (-)-CANADINE 1 (-)-EPICATECHIN 4 (-)-EPICATECHIN-3-O-GALLATE 1 (-)-EPIGALLOCATECHIN 1 (-)-EPIGALLOCATECHIN-3-O-GALLATE 2 (-)-EPIGALLOCATECHIN-GALLATE 3 (-)-HYDROXYJASMONIC-ACID 1 (-)-N-(1'-DEOXY-1'-D-FRUCTOPYRANOSYL)-S-ALLYL-L-CYSTEINE-SULFOXIDE 1 (1'S)-1'-ACETOXYCHAVICOL-ACETATE 1 (2R)-(12Z,15Z)-2-HYDROXY-4-OXOHENEICOSA-12,15-DIEN-1-YL-ACETATE 1 (7R,10R)-CAROTA-1,4-DIENALDEHYDE 1 (E)-4-(3',4'-DIMETHOXYPHENYL)-BUT-3-EN-OL 1 1,2,6-TRI-O-GALLOYL-BETA-D-GLUCOSE 1 1,7-BIS(3,4-DIHYDROXYPHENYL)HEPTA-4E,6E-DIEN-3-ONE 1 Chemical Activity Count 1,7-BIS(4-HYDROXY-3-METHOXYPHENYL)-1,6-HEPTADIEN-3,5-DIONE 1 1,8-CINEOLE 1 1-(METHYLSULFINYL)-PROPYL-METHYL-DISULFIDE 1 1-ETHYL-BETA-CARBOLINE 1 1-O-(2,3,4-TRIHYDROXY-3-METHYL)-BUTYL-6-O-FERULOYL-BETA-D-GLUCOPYRANOSIDE 1 10-ACETOXY-8-HYDROXY-9-ISOBUTYLOXY-6-METHOXYTHYMOL 1 10-GINGEROL 1 12-(4'-METHOXYPHENYL)-DAURICINE 1 12-METHOXYDIHYDROCOSTULONIDE 1 13',II8-BIAPIGENIN 1 13-HYDROXYLUPANINE 1 14-ACETOXYCEDROL 1 14-O-ACETYL-ACOVENIDOSE-C 1 16-HYDROXY-4,4,10,13-TETRAMETHYL-17-(4-METHYL-PENTYL)-HEXADECAHYDRO- 1 CYCLOPENTA[A]PHENANTHREN-3-ONE 2,3,7-TRIHYDROXY-5-(3,4-DIHYDROXY-E-STYRYL)-6,7,8,9-TETRAHYDRO-5H- -
Herbal and Homeopathy Remedies
HERBAL AND HOMEOPATHY REMEDIES Homeopathy is based on the principle ‘like cures like’. It involves treating the individual with highly diluted substances. Recommendations These recommendations are in line with NHS ENGLAND’s guidance on items that should not routinely be prescribed in primary care Herbal and Homeopathy products should not be prescribed to patients If previously prescribed, they should be stopped and patients advised to buy over the counter in pharmacies or in health shops. Rationale In 2010 House of Commons Science and Technology Committee found that the use of homeopathy was not evidence-based, and any benefits to patients were due to placebo effect. They recommended that homeopathy should not be funded on the NHS and the Medicines and Healthcare products Regulatory Agency (MHRA) should stop licensing homeopathic products. The National Institute for Health and Care Excellence (NICE) does not recommend homeopathy for the treatment of any health condition. NHS England have categorised Homeopathy as products of low clinical effectiveness, where there is a lack of robust evidence of clinical effectiveness or there are significant safety concerns. The Specialist Pharmacy Service (SPS) review in October 2017 found that there was no clear or robust evidence base to support the use of homeopathy in the NHS. June 2018 Most homeopathic remedies will still be available to patients as they can be bought over- the-counter from a chemist or health food shop. NHS England have categorised Herbal treatments as products of low clinical effectiveness, where there is a lack of robust evidence of clinical effectiveness or there are significant safety concerns.