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<I>Efavirenz</I>, New Therapeutic Agents for AIDS
CONFERENCE REPORTS 295 CHIMIA 1999. 53. NO.6 CONFERENCE REPORTS Chimia 53 (1999) 295-304 © Neue Schweizerische Chemische Gesellschaft ISSN 0009-4293 Second Swiss/German Meeting on Medicinal Chemistry Fruhjahrsversammlung 1999 der Neuen Schweizerischen Chemischen Gesellschaft (NSCG) 22./23. Marz 1999, Basel Vier Mini-Symposia uber Virologie, Multidrug Resistance, Immunologie und Gene Therapie Organisiert von der Sektion Medizinische Ghemie der NSGG, der Fachgruppe fUr Medizinische Chemie der GDGh und der Basler Chemischen Gesellschatt mit Unterstutzung der Pharmazeutischen Industrie. Report by the Research Team of G. Folkers' 'Correspondence: Prof. Dr. G. Folkers Department of Pharmacy Winterthurerstrasse 190 CH-8057Zi.irich E-Mail: [email protected] Discovery of Indinavir and Efavirenz, New Therapeutic Agents for AIDS Terry A. Lyle, Merck Research Laboratories, West Point, PA, USA For the treatment of HIV infection, two enzymes are of major interest: The HIV-l Protease (PR) and the Reverse- Tran- scriptase (RT). The HIV -Protease, an aspartic-acid pro- tease active as a dimer, is responsible for H 0 the cleavage of polypeptides assembled at o N~' the cell membrane. The inhibition of the Y I( ; N 1\ 0 = H protease-mediated cleavage of the viral "0 o o o precursor polyproteins results in the pro- duction of noninfectious progeny viral par- ticles. The development of lndinavir start- ed with screening a collection of renin inhibitors. A seven-amino-acid analog 1 1 which contains the hydroxyethylene tran- CONFERENCE REPORTS 296 CHIMIA 1999, 53. No.6 prevents the spread of the virus. Different nucleoside inhibitors like AZT, ddI, ddC, d4T and 3TC are already known, but new QH non-nucleoside inhibitors (NNRTI) are U'O developed to decrease the cytotoxicity and N : to improve the selectivity of the viral polymerases vs. -
Psychoactive Plants Used in Designer Drugs As a Threat to Public Health
From Botanical to Medical Research Vol. 61 No. 2 2015 DOI: 10.1515/hepo-2015-0017 REVIEW PAPER Psychoactive plants used in designer drugs as a threat to public health AGNIESZKA RONDZISTy1, KAROLINA DZIEKAN2*, ALEKSANDRA KOWALSKA2 1Department of Humanities in Medicine Pomeranian Medical University Chłapowskiego 11 70-103 Szczecin, Poland 2Department of Stem Cells and Regenerative Medicine Institute of Natural Fibers and Medicinal Plants Kolejowa 2 62-064 Plewiska, Poland *corresponding author: e-mail: [email protected] Summary Based on epidemiologic surveys conducted in 2007–2013, an increase in the consumption of psychoactive substances has been observed. This growth is noticeable in Europe and in Poland. With the ‘designer drugs’ launch on the market, which ingredients were not placed on the list of controlled substances in the Misuse of Drugs Act, a rise in the number and diversity of psychoactive agents and mixtures was noticed, used to achieve a different state of mind. Thus, the threat to the health and lives of people who use them has grown. In this paper, the authors describe the phenomenon of the use of plant psychoactive sub- stances, paying attention to young people who experiment with new narcotics. This article also discusses the mode of action and side effects of plant materials proscribed under the Misuse of Drugs Act in Poland. key words: designer drugs, plant materials, drugs, adolescents INTRODUCTION Anthropological studies concerning preliterate societies have shown that psy- choactive substances have been used for ages. On the individual level, they help to Herba Pol 2015; 61(2): 73-86 A. Rondzisty, K. -
Methods of Isolation and Bioactivity of Alkaloids Obtained from Selected
DOI: 10.2478/cipms-2021-0016 Curr. Issues Pharm. Med. Sci., Vol. 34, No. 2, Pages 81-86 Current Issues in Pharmacy and Medical Sciences Formerly ANNALES UNIVERSITATIS MARIAE CURIE-SKLODOWSKA, SECTIO DDD, PHARMACIA journal homepage: http://www.curipms.umlub.pl/ Methods of isolation and bioactivity of alkaloids obtained from selected species belonging to the Amaryllidaceae and Lycopodiaceae families Aleksandra Dymek* , Tomasz Mroczek Independent Laboratory of Chemistry of Natural Products, The Chair of Pharmacognosy, Medical University of Lublin, Poland ARTICLE INFO ABSTRACT Received 17 February 2021 Alkaloids obtained from plants belonging to the Amaryllidaceae and Lycopodiaceae Accepted 20 May 2021 families are of great interest due to their numerous properties. They play a very important Keywords: role mainly due to their strong antioxidant, anxiolytic and anticholinesterase activities. Lycopodium sp., The bioactive compounds obtained from these two families, especially galanthamine Narcissus sp., and huperzine A, have found application in the treatment of the common and AChE inhibitors, TLC, incurable dementia-like Alzheimer’s disease. Thanks to this discovery, there has been SPE, a breakthrough in its treatment by significantly improving the patient’s quality of life and PLE, slowing down disease symptoms – albeit with no chance of a complete cure. Therefore, TLC-bioatography. a continuous search for new compounds with potent anti-AChE activity is needed in modern medicine. In obtaining new therapeutic bioactive phytochemicals from plant material, the isolation process and its efficiency are crucial. Many techniques are known for isolating bioactive compounds and determining their amounts in complex samples. The most commonly utilized methods are extraction using different variants of organic solvents allied with chromatographic and spectrometric techniques. -
2D6 Substrates 2D6 Inhibitors 2D6 Inducers
Physician Guidelines: Drugs Metabolized by Cytochrome P450’s 1 2D6 Substrates Acetaminophen Captopril Dextroamphetamine Fluphenazine Methoxyphenamine Paroxetine Tacrine Ajmaline Carteolol Dextromethorphan Fluvoxamine Metoclopramide Perhexiline Tamoxifen Alprenolol Carvedilol Diazinon Galantamine Metoprolol Perphenazine Tamsulosin Amiflamine Cevimeline Dihydrocodeine Guanoxan Mexiletine Phenacetin Thioridazine Amitriptyline Chloropromazine Diltiazem Haloperidol Mianserin Phenformin Timolol Amphetamine Chlorpheniramine Diprafenone Hydrocodone Minaprine Procainamide Tolterodine Amprenavir Chlorpyrifos Dolasetron Ibogaine Mirtazapine Promethazine Tradodone Aprindine Cinnarizine Donepezil Iloperidone Nefazodone Propafenone Tramadol Aripiprazole Citalopram Doxepin Imipramine Nifedipine Propranolol Trimipramine Atomoxetine Clomipramine Encainide Indoramin Nisoldipine Quanoxan Tropisetron Benztropine Clozapine Ethylmorphine Lidocaine Norcodeine Quetiapine Venlafaxine Bisoprolol Codeine Ezlopitant Loratidine Nortriptyline Ranitidine Verapamil Brofaramine Debrisoquine Flecainide Maprotline olanzapine Remoxipride Zotepine Bufuralol Delavirdine Flunarizine Mequitazine Ondansetron Risperidone Zuclopenthixol Bunitrolol Desipramine Fluoxetine Methadone Oxycodone Sertraline Butylamphetamine Dexfenfluramine Fluperlapine Methamphetamine Parathion Sparteine 2D6 Inhibitors Ajmaline Chlorpromazine Diphenhydramine Indinavir Mibefradil Pimozide Terfenadine Amiodarone Cimetidine Doxorubicin Lasoprazole Moclobemide Quinidine Thioridazine Amitriptyline Cisapride -
GABA Receptors
D Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews Review No.7 / 1-2011 GABA receptors Wolfgang Froestl , CNS & Chemistry Expert, AC Immune SA, PSE Building B - EPFL, CH-1015 Lausanne, Phone: +41 21 693 91 43, FAX: +41 21 693 91 20, E-mail: [email protected] GABA Activation of the GABA A receptor leads to an influx of chloride GABA ( -aminobutyric acid; Figure 1) is the most important and ions and to a hyperpolarization of the membrane. 16 subunits with γ most abundant inhibitory neurotransmitter in the mammalian molecular weights between 50 and 65 kD have been identified brain 1,2 , where it was first discovered in 1950 3-5 . It is a small achiral so far, 6 subunits, 3 subunits, 3 subunits, and the , , α β γ δ ε θ molecule with molecular weight of 103 g/mol and high water solu - and subunits 8,9 . π bility. At 25°C one gram of water can dissolve 1.3 grams of GABA. 2 Such a hydrophilic molecule (log P = -2.13, PSA = 63.3 Å ) cannot In the meantime all GABA A receptor binding sites have been eluci - cross the blood brain barrier. It is produced in the brain by decarb- dated in great detail. The GABA site is located at the interface oxylation of L-glutamic acid by the enzyme glutamic acid decarb- between and subunits. Benzodiazepines interact with subunit α β oxylase (GAD, EC 4.1.1.15). It is a neutral amino acid with pK = combinations ( ) ( ) , which is the most abundant combi - 1 α1 2 β2 2 γ2 4.23 and pK = 10.43. -
Herbal Medicines in Pregnancy and Lactation : an Evidence-Based
00 Prelims 1410 10/25/05 2:13 PM Page i Herbal Medicines in Pregnancy and Lactation An Evidence-Based Approach Edward Mills DPh MSc (Oxon) Director, Division of Clinical Epidemiology Canadian College of Naturopathic Medicine North York, Ontario, Canada Jean-Jacques Duguoa MSc (cand.) ND Naturopathic Doctor Toronto Western Hospital Assistant Professor Division of Clinical Epidemiology Canadian College of Naturopathic Medicine North York, Ontario, Canada Dan Perri BScPharm MD MSc Clinical Pharmacology Fellow University of Toronto Toronto, Ontario, Canada Gideon Koren MD FACMT FRCP Director of Motherisk Professor of Medicine, Pediatrics and Pharmacology University of Toronto Toronto, Ontario, Canada With a contribution from Paul Richard Saunders PhD ND DHANP 00 Prelims 1410 10/25/05 2:13 PM Page ii © 2006 Taylor & Francis Medical, an imprint of the Taylor & Francis Group First published in the United Kingdom in 2006 by Taylor & Francis Medical, an imprint of the Taylor & Francis Group, 2 Park Square, Milton Park, Abingdon, Oxon OX14 4RN Tel.: ϩ44 (0)20 7017 6000 Fax.: ϩ44 (0)20 7017 6699 E-mail: [email protected] Website: www.tandf.co.uk/medicine All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or trans- mitted, in any form or by any means, electronic, mechanical, photocopying, recording, or otherwise, without the prior permission of the publisher or in accordance with the provisions of the Copyright, Designs and Patents Act 1988 or under the terms of any licence permitting limited copying issued by the Copyright Licensing Agency, 90 Tottenham Court Road, London W1P 0LP. -
Effect of Wine and Vinegar Processing of Rhizoma Corydalis on the Tissue Distribution of Tetrahydropalmatine, Protopine and Dehydrocorydaline in Rats
Michigan Technological University Digital Commons @ Michigan Tech Michigan Tech Publications 1-18-2012 Effect of wine and vinegar processing of Rhizoma Corydalis on the tissue distribution of tetrahydropalmatine, protopine and dehydrocorydaline in rats Zhiying Dou Tianjin University of Traditional Chinese Medicine Kefeng Li Michigan Technological University Ping Wang Tianjin University of Traditional Chinese Medicine Liu Cao Tianjin University of Traditional Chinese Medicine Follow this and additional works at: https://digitalcommons.mtu.edu/michigantech-p Part of the Biology Commons Recommended Citation Dou, Z., Li, K., Wang, P., & Cao, L. (2012). Effect of wine and vinegar processing of Rhizoma Corydalis on the tissue distribution of tetrahydropalmatine, protopine and dehydrocorydaline in rats. Molecules, 17(1), 951-970. http://doi.org/10.3390/molecules17010951 Retrieved from: https://digitalcommons.mtu.edu/michigantech-p/1969 Follow this and additional works at: https://digitalcommons.mtu.edu/michigantech-p Part of the Biology Commons Molecules 2012, 17, 951-970; doi:10.3390/molecules17010951 OPEN ACCESS molecules ISSN 1420-3049 www.mdpi.com/journal/molecules Article Effect of Wine and Vinegar Processing of Rhizoma Corydalis on the Tissue Distribution of Tetrahydropalmatine, Protopine and Dehydrocorydaline in Rats Zhiying Dou 1,*, Kefeng Li 2, Ping Wang 1 and Liu Cao 1 1 College of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 2 Department of Biological Sciences, Michigan Technological University, Houghton, MI 49931, USA; E-Mail: [email protected] * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel./Fax: +86-22-5959-6235. Received: 29 November 2011; in revised form: 5 January 2012 / Accepted: 9 January 2012 / Published: 18 January 2012 Abstract: Vinegar and wine processing of medicinal plants are two traditional pharmaceutical techniques which have been used for thousands of years in China. -
Soma and Haoma: Ayahuasca Analogues from the Late Bronze Age
ORIGINAL ARTICLE Journal of Psychedelic Studies 3(2), pp. 104–116 (2019) DOI: 10.1556/2054.2019.013 First published online July 25, 2019 Soma and Haoma: Ayahuasca analogues from the Late Bronze Age MATTHEW CLARK* School of Oriental and African Studies (SOAS), Department of Languages, Cultures and Linguistics, University of London, London, UK (Received: October 19, 2018; accepted: March 14, 2019) In this article, the origins of the cult of the ritual drink known as soma/haoma are explored. Various shortcomings of the main botanical candidates that have so far been proposed for this so-called “nectar of immortality” are assessed. Attention is brought to a variety of plants identified as soma/haoma in ancient Asian literature. Some of these plants are included in complex formulas and are sources of dimethyl tryptamine, monoamine oxidase inhibitors, and other psychedelic substances. It is suggested that through trial and error the same kinds of formulas that are used to make ayahuasca in South America were developed in antiquity in Central Asia and that the knowledge of the psychoactive properties of certain plants spreads through migrants from Central Asia to Persia and India. This article summarizes the main arguments for the botanical identity of soma/haoma, which is presented in my book, The Tawny One: Soma, Haoma and Ayahuasca (Muswell Hill Press, London/New York). However, in this article, all the topics dealt with in that publication, such as the possible ingredients of the potion used in Greek mystery rites, an extensive discussion of cannabis, or criteria that we might use to demarcate non-ordinary states of consciousness, have not been elaborated. -
Effects of Enzymatic and Thermal Processing on Flavones, the Effects of Flavones on Inflammatory Mediators in Vitro, and the Absorption of Flavones in Vivo
Effects of enzymatic and thermal processing on flavones, the effects of flavones on inflammatory mediators in vitro, and the absorption of flavones in vivo DISSERTATION Presented in Partial Fulfillment of the Requirements for the Degree Doctor of Philosophy in the Graduate School of The Ohio State University By Gregory Louis Hostetler Graduate Program in Food Science and Technology The Ohio State University 2011 Dissertation Committee: Steven Schwartz, Advisor Andrea Doseff Erich Grotewold Sheryl Barringer Copyrighted by Gregory Louis Hostetler 2011 Abstract Flavones are abundant in parsley and celery and possess unique anti-inflammatory properties in vitro and in animal models. However, their bioavailability and bioactivity depend in part on the conjugation of sugars and other functional groups to the flavone core. Two studies were conducted to determine the effects of processing on stability and profiles of flavones in celery and parsley, and a third explored the effects of deglycosylation on the anti-inflammatory activity of flavones in vitro and their absorption in vivo. In the first processing study, celery leaves were combined with β-glucosidase-rich food ingredients (almond, flax seed, or chickpea flour) to determine test for enzymatic hydrolysis of flavone apiosylglucosides. Although all of the enzyme-rich ingredients could convert apigenin glucoside to aglycone, none had an effect on apigenin apiosylglucoside. Thermal stability of flavones from celery was also tested by isolating them and heating at 100 °C for up to 5 hours in pH 3, 5, or 7 buffer. Apigenin glucoside was most stable of the flavones tested, with minimal degradation regardless of pH or heating time. -
WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 36/84 (2006.01) A61K 31/5513 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/045 (2006.01) A61P 31/22 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 31/522 (2006.01) A61K 45/06 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, PCT/NL20 14/050780 KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (22) International Filing Date: MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, 13 November 2014 (13.1 1.2014) PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (25) Filing Language: English TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of regional protection available): ARIPO (BW, GH, 61/903,430 13 November 2013 (13. 11.2013) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (71) Applicant: RJG DEVELOPMENTS B.V. -
Plant-Based Medicines for Anxiety Disorders, Part 2: a Review of Clinical Studies with Supporting Preclinical Evidence
CNS Drugs 2013; 24 (5) Review Article Running Header: Plant-Based Anxiolytic Psychopharmacology Plant-Based Medicines for Anxiety Disorders, Part 2: A Review of Clinical Studies with Supporting Preclinical Evidence Jerome Sarris,1,2 Erica McIntyre3 and David A. Camfield2 1 Department of Psychiatry, Faculty of Medicine, University of Melbourne, Richmond, VIC, Australia 2 The Centre for Human Psychopharmacology, Swinburne University of Technology, Melbourne, VIC, Australia 3 School of Psychology, Charles Sturt University, Wagga Wagga, NSW, Australia Correspondence: Jerome Sarris, Department of Psychiatry and The Melbourne Clinic, University of Melbourne, 2 Salisbury Street, Richmond, VIC 3121, Australia. Email: [email protected], Acknowledgements Dr Jerome Sarris is funded by an Australian National Health & Medical Research Council fellowship (NHMRC funding ID 628875), in a strategic partnership with The University of Melbourne, The Centre for Human Psychopharmacology at the Swinburne University of Technology. Jerome Sarris, Erica McIntyre and David A. Camfield have no conflicts of interest that are directly relevant to the content of this article. 1 Abstract Research in the area of herbal psychopharmacology has revealed a variety of promising medicines that may provide benefit in the treatment of general anxiety and specific anxiety disorders. However, a comprehensive review of plant-based anxiolytics has been absent to date. Thus, our aim was to provide a comprehensive narrative review of plant-based medicines that have clinical and/or preclinical evidence of anxiolytic activity. We present the article in two parts. In part one, we reviewed herbal medicines for which only preclinical investigations for anxiolytic activity have been performed. In this current article (part two), we review herbal medicines for which there have been both preclinical and clinical investigations for anxiolytic activity. -
A Screening Tool for Acetylcholinesterase Inhibitors
RESEARCH ARTICLE Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors 1 1 2 1 Devashree N. Patil , Sushama A. Patil , Srinivas SistlaID , Jyoti P. JadhavID * 1 Department of Biotechnology, Shivaji University, Kolhapur, MS, India, 2 Institute for Structural Biology, Drug Discovery and Development, Virginia Commonwealth University, Richmond, Virginia, United States * [email protected] a1111111111 a1111111111 a1111111111 a1111111111 Abstract a1111111111 Among neurodegenerative diseases, Alzheimer's disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treat- OPEN ACCESS ment of AD. The study aims to evaluate the interactions between natural molecules and Citation: Patil DN, Patil SA, Sistla S, Jadhav JP AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols (2019) Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. and substrates of AChE have been considered for the study with a major emphasis on affin- PLoS ONE 14(5): e0215291. https://doi.org/ ity and kinetics. To better understand the activity of small molecules, the investigation is sup- 10.1371/journal.pone.0215291 ported by both experimental and theoretical approach such as fluorescence, Circular Editor: David A. Lightfoot, College of Agricultural Dichroism (CD) and molecular docking studies. Amongst the screened ones tannic acid Sciences, UNITED STATES showed promising results compared with others. The methodology followed here have Received: September 26, 2018 highlighted many molecules with a higher affinity towards AChE and these findings may Accepted: March 30, 2019 take lead molecules generated in preclinical studies to treat neurodegenerative diseases.