Biodegradation of the Steroid Progesterone in Surface Waters
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Expression of Recombinant Human Androgen Receptor and Its Use for Screening Methods
Institut für Physiologie FML Weihenstephan Technische Universität München Expression of recombinant human androgen receptor and its use for screening methods Ellinor Rose Sigrid Bauer Vollständiger Abdruck der von der Fakultät Wissenschaftszentrum Weihenstephan für Ernährung, Landnutzung und Umwelt der Technischen Universität München zur Erlangung des akademischen Grades eines Doktors der Naturwissenschaften genehmigten Dissertation. Vorsitzender: Univ.-Prof. Dr. B. Hock Prüfer der Dissertation: Univ.-Prof. Dr. H. H. D. Meyer Univ.-Prof. Dr. H. Sauerwein (Rheinische Friedrich-Wilhelms-Universität Bonn) Die Dissertation wurde am 31.10.2002 bei der Technischen Universität München eingereicht und durch die Fakultät Wissenschaftszentrum Weihenstephan für Ernährung, Landnutzung und Umwelt am 03.12.2002 angenommen. Introduction Content 1. INTRODUCTION ..................................................................................................................................... 5 1.1. ENDOCRINE DISRUPTERS 5 1.2. ANDROGENS AND ANTIANDROGENS 7 1.2.1. DEFINITIONS 7 1.2.2. MODE OF ACTION 8 1.3. STRUCTURES OF ENDOCRINE DISRUPTERS 10 1.4. STRATEGIES FOR MONITORING ANDROGEN ACTIVE SUBSTANCES 13 1.4.1. IN VIVO METHODS 13 1.4.2. IN VITRO METHODS 15 1.5. OBJEKTIVE OF THE STUDIES 18 2. MATERIALS AND METHODS ................................................................................................................. 19 2.1. PREPARATION OF RECEPTORS 19 2.2. ASSAY SYSTEMS 19 2.2.1. IN SOLUTION AR ASSAY 19 2.2.2. IMMUNO-IMMOBILISED RECEPTOR ASSAY (IRA) 20 2.2.3. PR AND SHBG ASSAYS 21 2.2.4. DATA EVALUATION 21 2.3. ANALYTES 22 3. RESULTS AND DISCUSSION ................................................................................................................. 23 3.1. DEVELOPMENT OF NEW ASSAY SYSTEMS 23 3.1.1. BAR ASSAY 23 3.1.2. CLONING OF THE HUMAN AR AND PRODUCTION OF FUNCTIONAL PROTEIN 24 3.1.3. DEVELOPMENT OF A SCREENING ASSAY ON MICROTITRE PLATES (IRA) 25 3.2. -
(Cyp19a1b-GFP) Zebrafish Embryos
Screening Estrogenic Activities of Chemicals or Mixtures In Vivo Using Transgenic (cyp19a1b-GFP) Zebrafish Embryos Franc¸ois Brion1, Yann Le Page2, Benjamin Piccini1, Olivier Cardoso1, Sok-Keng Tong3, Bon-chu Chung3, Olivier Kah2* 1 Unite´ d’Ecotoxicologie in vitro et in vivo, Direction des Risques Chroniques, Institut National de l’Environnement Industriel et des Risques (INERIS), Verneuil-en- Halatte, France, 2 Universite´ de Rennes 1, Institut de Recherche Sante´ Environnement & Travail (IRSET), INSERM U1085, BIOSIT, Campus de Beaulieu, Rennes France, 3 Taiwan Institute of Molecular Biology, Academia Sinica, Taipei, Taiwan Abstract The tg(cyp19a1b-GFP) transgenic zebrafish expresses GFP (green fluorescent protein) under the control of the cyp19a1b gene, encoding brain aromatase. This gene has two major characteristics: (i) it is only expressed in radial glial progenitors in the brain of fish and (ii) it is exquisitely sensitive to estrogens. Based on these properties, we demonstrate that natural or synthetic hormones (alone or in binary mixture), including androgens or progestagens, and industrial chemicals induce a concentration-dependent GFP expression in radial glial progenitors. As GFP expression can be quantified by in vivo imaging, this model presents a very powerful tool to screen and characterize compounds potentially acting as estrogen mimics either directly or after metabolization by the zebrafish embryo. This study also shows that radial glial cells that act as stem cells are direct targets for a large panel of endocrine disruptors, calling for more attention regarding the impact of environmental estrogens and/or certain pharmaceuticals on brain development. Altogether these data identify this in vivo bioassay as an interesting alternative to detect estrogen mimics in hazard and risk assessment perspective. -
Part I Biopharmaceuticals
1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modifications 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays -
伊域化學藥業(香港)有限公司 Cyclopentyl Substituted Compounds
® 伊 域 化 學(香 藥 香 港) 業 港有 有 限 限 公 公 司 司 YICK-VIC CHEMICALS & PHARMACEUTICALS (HK) LTD Rm 1006, 10/F, Hewlett Centre, Tel: (852) 25412772 (4 lines) No. 52-54, Hoi Yuen Road, Fax: (852) 25423444 / 25420530 / 21912858 Kwun Tong, E-mail: [email protected] YICKYICK----VICVICVICVIC 伊域伊域伊域 Kowloon, Hong Kong. Site: http://www.yickvic.com Cyclopentyl Substituted Compounds Product Code CAS Product Name CC-0052BA 39746-00-4 (-)-COREY LACTONE BENZOATE CC-3702AD 1211-29-6 (-)-METHYL JASMONATE SPI-4467C 87269-86-1 (-)-OCTAHYDROCYCLOPENTA[B]PYRROLE-2-CARBOXYLIC ACID HYDROCHLORIDE SPI-4467A 93779-30-7 (+/-)-OCTAHYDROCYCLOPENTA[B]PYRROLE-2-CARBOXYLIC ACID HYDROCHLORIDE SPI-2956FG 142217-81-0 (1S,3R,4S)-2-AMINO-9-(4-BENZYLOXY)-3-(BENZYLOXYMETHYL)-2-METHYLIDENECYCLOPENTYL-3H-PURINE-9-ONE SPI-2956FJ 142217-78-5 (2R,3S,5S)-3-(BENZYLOXY)-5-[2-[[(4-METHOXYPHENYL)DIPHENYLMETHYL]AMINO]-6-(PHENYLMETHOXY)-9H-PURIN-9-Y L]-2-(BENZYLOXYMETHYL)CYCLOPENTANOL SPI-1560DH 4167-77-5 1,1-CYCLOPENTANEDICARBOXYLIC ACID DIETHYL ESTER SPI-2808C 5763-44-0 1,2-CYCLOPENTANE DICARBOXIMIDE CC-1957B 1222-05-5 1,3,4,6,7,8-HEXAHYDRO-4,6,6,7,8,8-HEXAMETHYLCYCLOPENTA[G]-2-BENZOPYRAN SPI-1246B 3859-41-4 1,3-CYCLOPENTANEDIONE SPI-1955AA 646-06-0 1,3-DIOXOLANE SPI-3082AA 54078-29-4 1,8-DIAZAFLUOREN-9-ONE UNIE-13864 564-35-2 11-KETOTESTOSTERONE SPI-0098CA 640-87-9 17-ALPHA,21-DIHYDROXYPREGN-4-ENE-3,20-DIONE 21-ACETATE UNIE-13126 302-76-1 17ALPHA-METHYL-17BETA-ESTRADIOL UNIE-14695 3563-27-7 17BETA-DIHYDROQUILIN UNIE-2836 10316-79-7 1-AMINO-1-CYCLOPENTANEMETHANOL SPI-3077CB 61379-64-4 1-AMINO-4-CYCLOPENTYLPIPERAZINE -
A New Highly Specific and Robust Yeast Androgen Bioassay for the Detection of Agonists and Antagonists
Anal Bioanal Chem (2007) 389:1549–1558 DOI 10.1007/s00216-007-1559-6 ORIGINAL PAPER A new highly specific and robust yeast androgen bioassay for the detection of agonists and antagonists Toine F. H. Bovee & Richard J. R. Helsdingen & Astrid R. M. Hamers & Majorie B. M. van Duursen & Michel W. F. Nielen & Ron L. A. P. Hoogenboom Received: 27 April 2007 /Revised: 3 July 2007 /Accepted: 15 August 2007 / Published online: 12 September 2007 # Springer-Verlag 2007 Abstract Public concern about the presence of natural and very specific and also suited to detect compounds that have anthropogenic compounds which affect human health by an antiandrogenic mode of action. modulating normal endocrine functions is continuously growing. Fast and simple high-throughput screening methods Keywords Antagonists . Brominated flame retardants . for the detection of hormone activities are thus indispens- Crosstalk . Metabolism . Receptor . Saccharomyces able. During the last two decades, a panel of different in vitro cerevisiae assays has been developed, mainly for compounds with an estrogenic mode of action. Here we describe the develop- ment of an androgen transcription activation assay that is Introduction easy to use in routine screening. Recombinant yeast cells were constructed that express the human androgen receptor There is concern that chemicals in our food, water, and and yeast enhanced green fluorescent protein (yEGFP), the environment affect human health by disrupting normal latter in response to androgens. Compared with other endocrine function, possibly leading to reproductive failure reporters, the yEGFP reporter protein is very convenient in humans and tumors in sensitive tissues [1, 2]. This because it is directly measurable in intact living cells, i.e., relates to chemicals with previously unknown hormonal cell wall disruption and the addition of a substrate are not properties, like certain pesticides and plasticizers, but also needed. -
Steroids and Other Appearance and Performance Enhancing Drugs (Apeds) Research Report
Research Report Revised Febrero 2018 Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Table of Contents Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Introduction What are the different types of APEDs? What is the history of anabolic steroid use? Who uses anabolic steroids? Why are anabolic steroids misused? How are anabolic steroids used? What are the side effects of anabolic steroid misuse? How does anabolic steroid misuse affect behavior? What are the risks of anabolic steroid use in teens? How do anabolic steroids work in the brain? Are anabolic steroids addictive? How are anabolic steroids tested in athletes? What can be done to prevent steroid misuse? What treatments are effective for anabolic steroid misuse? Where can I get further information about steroids? References Page 1 Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Esta publicación está disponible para su uso y puede ser reproducida, en su totalidad, sin pedir autorización al NIDA. Se agradece la citación de la fuente, de la siguiente manera: Fuente: Instituto Nacional sobre el Abuso de Drogas; Institutos Nacionales de la Salud; Departamento de Salud y Servicios Humanos de los Estados Unidos. Introduction Appearance and performance enhancing drugs (APEDs) are most often used by males to improve appearance by building muscle mass or to enhance athletic performance. Although they may directly and indirectly have effects on a user’s mood, they do not produce a euphoric high, which makes APEDs distinct from other drugs such as cocaine, heroin, and marijuana. However, users may develop a substance use disorder, defined as continued use despite adverse consequences. -
TGA Review of Hgps
A REVIEW TO UPDATE AUSTRALIA’S POSITION ON THE HUMAN SAFETY OF RESIDUES OF HORMONE GROWTH PROMOTANTS (HGPs) USED IN CATTLE Prepared by Chemical Review and International Harmonisation Section Office of Chemical Safety Therapeutic Goods Administration of the Department of Health and Ageing Canberra July 2003 A draft of this report was tabled at the 25th Meeting of the Advisory Committee on Pesticides and Health (ACPH), held in Canberra on the 1st May 2003. The report was subsequently endorsed out-of-session by the ACPH. Hormone Growth Promotants TABLE OF CONTENTS ABBREVIATIONS ................................................................................................................................................................4 EXECUTIVE SUMMARY ..................................................................................................................................................7 INTRODUCTION..................................................................................................................................................................9 HEALTH CONCERNS ASSOCIATED WITH HGP S................................................................................................................9 DIFFICULTIES ASSOCIAT ED WITH ASSESSING THE SAFETY OF HGPS.........................................................................10 RISK ASSESSMENTS OF HGP S .........................................................................................................................................10 PURPOSE OF THE CURRENT -
Analytical Reference Standards
Cerilliant Quality ISO GUIDE 34 ISO/IEC 17025 ISO 90 01:2 00 8 GM P/ GL P Analytical Reference Standards 2 011 Analytical Reference Standards 20 811 PALOMA DRIVE, SUITE A, ROUND ROCK, TEXAS 78665, USA 11 PHONE 800/848-7837 | 512/238-9974 | FAX 800/654-1458 | 512/238-9129 | www.cerilliant.com company overview about cerilliant Cerilliant is an ISO Guide 34 and ISO 17025 accredited company dedicated to producing and providing high quality Certified Reference Standards and Certified Spiking SolutionsTM. We serve a diverse group of customers including private and public laboratories, research institutes, instrument manufacturers and pharmaceutical concerns – organizations that require materials of the highest quality, whether they’re conducing clinical or forensic testing, environmental analysis, pharmaceutical research, or developing new testing equipment. But we do more than just conduct science on their behalf. We make science smarter. Our team of experts includes numerous PhDs and advance-degreed specialists in science, manufacturing, and quality control, all of whom have a passion for the work they do, thrive in our collaborative atmosphere which values innovative thinking, and approach each day committed to delivering products and service second to none. At Cerilliant, we believe good chemistry is more than just a process in the lab. It’s also about creating partnerships that anticipate the needs of our clients and provide the catalyst for their success. to place an order or for customer service WEBSITE: www.cerilliant.com E-MAIL: [email protected] PHONE (8 A.M.–5 P.M. CT): 800/848-7837 | 512/238-9974 FAX: 800/654-1458 | 512/238-9129 ADDRESS: 811 PALOMA DRIVE, SUITE A ROUND ROCK, TEXAS 78665, USA © 2010 Cerilliant Corporation. -
WO 2012/148570 Al 1 November 2012 (01.11.2012) 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 2012/148570 Al 1 November 2012 (01.11.2012) P O P C T (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, A61L 27/14 (2006.01) A61P 17/02 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, C08L 101/16 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, (21) International Application Number: KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, PCT/US20 12/027464 MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (22) International Filing Date: OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, 2 March 2012 (02.03.2012) SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, 13/093,479 25 April 201 1 (25.04.201 1) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (71) Applicant (for all designated States except US): DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, WARSAW ORTHOPEDIC, INC. -
Avaliação Do Teste De Micronúcleo Em Linfócitos Para Uso Como Biomarcador De Risco De Câncer Em Usuários De Esteroides Anabolizantes Androgênicos
UNIVERSIDADE ESTADUAL DE FEIRA DE SANTANA PROGRAMA DE PÓS-GRADUAÇÃO EM BIOTECNOLOGIA LEONARDO DA CUNHA MENEZES SOUZA AVALIAÇÃO DO TESTE DE MICRONÚCLEO EM LINFÓCITOS PARA USO COMO BIOMARCADOR DE RISCO DE CÂNCER EM USUÁRIOS DE ESTEROIDES ANABOLIZANTES ANDROGÊNICOS Feira de Santana, BA 2013 LEONARDO DA CUNHA MENEZES SOUZA AVALIAÇÃO DO TESTE DE MICRONÚCLEO EM LINFÓCITOS PARA USO COMO BIOMARCADOR DO RISCO DE CÂNCER EM USUÁRIOS DE ESTEROIDES ANABOLIZANTES ANDROGÊNICOS Dissertação apresentada ao Programa de Pós-graduação em Biotecnologia, da Universidade Estadual de Feira de Santana como requisito parcial para obtenção do título de Mestre em Biotecnologia. Orientadora: Profa. Dr. Eneida de Moraes Marcílio Cerqueira Feira de Santana, BA 2013 Aos meus pais com carinho AGRADECIMENTOS A Deus pela serenidade e coragem em momentos adversos; Ao meu pai e à minha mãe, por proporcionarem sempre um ambiente fértil ao aprendizado e à gentileza; À profa Eneida de Moraes Marcílio Cerqueira pela orientação segura, disponibilidade incondicional, e pelo carinho durante todos estes anos; À Maíza Alves Lopes pela grande ajuda e agradável companhia durante o desenvolvimento do trabalho, tornando menos árdua à empreitada; Ao professor José Roberto Cardoso Meireles pelos ensinamentos preciosos e grande ajuda ao longo de toda minha formação; À Luciara Alves da Cruz, pela disponibilidade para com as coletas, sem a qual este trabalho não seria possível; À Daisy Maria Favero Salvadori, à Luciana Maria Feliciano e à equipe da UNESP de Botucatu por terem me recebido tão -
Characterisation of Chemical and Pharmacological Properties of New Steroids Related to Doping of Athletes
In: W Schänzer, H Geyer, A Gotzmann, U Mareck (eds.) Recent Advances In Doping Analysis (14). Sport und Buch Strauß - Köln 2006 C. Ayotte, D. Goudreault, D. Cyr and J. Gauthier1, P. Ayotte and C. Larochelle2, and D. Poirier3 Characterisation of chemical and pharmacological properties of new steroids related to doping of athletes 1INRS-Institut Armand-Frappier, Pointe Claire, Canada 2Institut de Santé publique de Québec, U. Laval, Québec, Canada 3Centre de recherche en chimie médicinale, U. Laval, Québec, Canada In the USA, a female cyclist, T. Thomas, was banned for the use of norbolethone, a steroid which has been studied by the pharmaceutical industry in the 60s but not commercialised1. Later in 2004, following the characterisation of THG2 from a oily residue given to the American testing authorities, and in collaboration with the international athletic federation, several elite athletes’ samples were tested and found to contain that “designer” steroid. The properties of tetrahydrogestrinone were subsequently studied; it appears that THG is a potent androgen and progestin3. Public comments made by individuals involved in the “Balco” scandal were adding to the information coming from other sources, mainly informants, to the effect that other “designer”, potent and undetecTable steroids have been prepared and would be available to certain athletes. This has become a certainty in December 2003, following a seizure at the Canadian border of hGH, and two steroid-products one of which found to be THG. The identification of the second one, DMT (17α-methyl-5α-androst-2-en-17β-ol major isomer along with the 3-en isomer), is the subject of the first part of this work; picture of the bottle seized is shown at Figure 1. -
Neural Control of Human Movement
97818_ch19.qxd 8/4/09 4:16 PM Page 376 CHAPTER 19 Neural Control of Human Movement CHAPTER OBJECTIVES ➤ Draw the major structural components of the ➤ Outline motor unit facilitation and inhibition and brain, including the four lobes of the cerebral the contribution of each to exercise performance cortex and responsiveness to resistance training ➤ Discuss specific pyramidal and extrapyramidal ➤ Discuss variations in twitch characteristics, resist- tract functions ance to fatigue, and tension development in the different motor unit categories ➤ Diagram the anterior motor neuron and discuss its role in human movement ➤ Describe mechanisms that adjust force of muscle action along the continuum from slight to ➤ Draw and label the basic components of a maximum reflex arc ➤ Define fatigue and discuss factors that act and ➤ Define the terms (1) motor unit, (2) neuromuscular interact to induce neuromuscular fatigue junction, and (3) autonomic nervous system ➤ List and describe functions of the proprioceptors ➤ Summarize the events in motor unit excitation within joints, muscles, and tendons prior to muscle action 376 97818_ch19.qxd 8/4/09 4:16 PM Page 377 CHAPTER 19 Neural Control of Human Movement 377 The effective application of force during complex learned Brainstem movements (e.g., tennis serve, shot put, golf swing) depends on a series of coordinated neuromuscular patterns, not just on The medulla, pons, and midbrain compose the brain- muscle strength. The neural circuitry in the brain, spinal cord, stem. The medulla, located immediately above the spinal and periphery functions somewhat similar to a sophisticated cord, extends into the pons and serves as a bridge between computer network.