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[PMID]:28445846
[Au] Autor:Zhang Y; Li J; Meng Z; Zhu X; Gan H; Gu R; Wu Z; Zheng Y; Wei J; Dou G
[Ad] Endereço:Guangxi Medical University, 22 Shuangyong Road, Nanning 530000, China; Laboratory of Drug Metabolism and Pharmacokinetics, Beijing Institute of Transfusion Medicine, 27 Taiping Road, Beijing 100850, China. Electronic address: eve63443@163.com.
[Ti] Título:A sharp, robust, and quantitative method by liquid chromatography tandem mass spectrometry for the measurement of EAD for acute radiation syndrome and its application.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1055-1056:45-50, 2017 Jun 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:17-Ethinyl-3,17-dihydroxyandrost-5-ene (EAD) is an agent designed for the treatment of acute radiation syndrome (ARS). Given its vital role played in the prevention and mitigation of ARS, the development of a sharp, sensitive and robust liquid chromatography tandem mass spectrometry (LC-MS/MS) method to monitor the metabolism of EAD in vivo was crucial. A new method was constructed and validated for the determination of EAD with the internal standard of androst-5-ene-3ß,17ß-diol (5-AED). The blood samples were precipitated with methanol, centrifuged, from which the supernatant was separated on UPLC with C18 column and eluted in gradient with acetonitrile and Milli-Q water both containing 0.1% formic acid (FA). Quantification was performed by a triple quadrupole mass spectrometer with electro spray ionization (ESI) in multiple reactive monitoring (MRM) positive mode. A good linearity was obtained with R>0.99 for EAD within its calibration range from 5 to 1000ngmL with a lowest limit of quantification (LLOQ) of 5ngmL . Inter- and intra-day accuracy and precision of three levels of quality control (QC) samples were within the range of 15%, while the LLOQ was within 20%. Samples were stable under the circumstances of the experiments. The method was simple, accurate and robust applied to determine the concentrations of EAD in Wistar rat after a single administration of EAD orally at the dose of 100mgkg .
[Mh] Termos MeSH primário: Androstenodióis/farmacocinética
Protetores contra Radiação/farmacocinética
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Síndrome Aguda da Radiação/tratamento farmacológico
Administração Oral
Androstenodióis/administração & dosagem
Animais
Cromatografia Líquida/métodos
Feminino
Limite de Detecção
Masculino
Protetores contra Radiação/administração & dosagem
Ratos Wistar
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (17-ethinyl-3,17-dihydroxyandrost-5-ene); 0 (Androstenediols); 0 (Radiation-Protective Agents)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170619
[Lr] Data última revisão:
170619
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170427
[St] Status:MEDLINE


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[PMID]:28139245
[Au] Autor:Vehof J; Hysi PG; Hammond CJ
[Ad] Endereço:Department of Twin Research & Genetic Epidemiology, King's College London, St. Thomas' Hospital, London, United Kingdom; Department of Ophthalmology, King's College London, St. Thomas' Hospital, London, United Kingdom; Department of Ophthalmology, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands; Department of Epidemiology, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands. Electronic address: jelle.vehof@kcl.ac.uk.
[Ti] Título:A Metabolome-Wide Study of Dry Eye Disease Reveals Serum Androgens as Biomarkers.
[So] Source:Ophthalmology;124(4):505-511, 2017 Apr.
[Is] ISSN:1549-4713
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To test the association between serum metabolites and dry eye disease (DED) using a hypothesis-free metabolomics approach. DESIGN: Cross-sectional association study. PARTICIPANTS: A total of 2819 subjects from the population-representative TwinsUK cohort in the United Kingdom, with a mean age of 57 years (range, 17-82 years). METHODS: We tested associations between 222 known serum metabolites and DED. All subjects underwent nontargeted metabolomic analysis of plasma samples using gas and liquid chromatography in combination with mass spectrometry (Metabolon Inc., Durham, NC). Dry eye disease was defined from the validated Short Questionnaire for Dry Eye Syndrome (SQDES) as a previous diagnosis of DED by a clinician or "often" or "constant" symptoms of dryness and irritation. Analyses were performed with linear mixed effect models that included age, BMI, and sex as covariates, corrected for multiple testing. MAIN OUTCOME MEASURES: Primary outcome was DED as defined by the SQDES, and secondary outcomes were symptom score of DED and a clinical diagnosis of DED. RESULTS: Prevalence of DED as defined by the SQDES was 15.5% (n = 436). A strong and metabolome-wide significant association with DED was found with decreased levels of the metabolites androsterone sulfate (P = 0.00030) and epiandrosterone sulfate (P = 0.00036). Three other metabolites involved in androgen metabolism, 4-androsten-3beta,17beta-diol disulfate 1 and 2, and dehydroepiandrosterone sulfate, were the next most strongly associated of the 222 metabolites, but did not reach metabolome-wide significance. Dryness and irritation symptoms, as opposed to a clinical diagnosis, were particularly strongly associated with decreased androgen steroid metabolites, with all reaching metabolome-wide significance (androsterone sulfate, P = 0.000000029; epiandrosterone sulfate, P = 0.0000040; 4-androsten-3beta,17beta-diol disulfate 1, P = 0.000016; 4-androsten-3beta,17beta-diol disulfate 2, P = 0.000064; and dehydroepiandrosterone sulfate, P = 0.00011). Of these 5 androgens, epiandrosterone sulfate (P = 0.0076) was most associated with 2-year incidence of clinician-diagnosed DED. In addition, we found decreased glycerophosphocholines to be associated with DED, although not at metabolome-wide significance. CONCLUSIONS: This hypothesis-free metabolomic approach found decreased serum androgens to be highly associated with DED and adds important evidence to the growing body of research that links androgens to ocular surface disease and DED.
[Mh] Termos MeSH primário: Androgênios/sangue
Biomarcadores/sangue
Síndromes do Olho Seco/sangue
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Androstenodióis/sangue
Androsterona/análogos & derivados
Androsterona/sangue
Estudos de Coortes
Estudos Transversais
Sulfato de Desidroepiandrosterona/sangue
Síndromes do Olho Seco/diagnóstico
Feminino
Cromatografia Gasosa-Espectrometria de Massas
Seres Humanos
Masculino
Metaboloma
Meia-Idade
Fatores de Risco
Inquéritos e Questionários
[Pt] Tipo de publicação:JOURNAL ARTICLE; TWIN STUDY
[Nm] Nome de substância:
0 (Androgens); 0 (Androstenediols); 0 (Biomarkers); 1852-61-5 (4-androstene-3,17-diol); 57B09Q7FJR (Dehydroepiandrosterone Sulfate); C24W7J5D5R (Androsterone); UK5M12Z93J (androsterone sulfate)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170707
[Lr] Data última revisão:
170707
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170201
[St] Status:MEDLINE


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[PMID]:27813048
[Au] Autor:Casas S; Gonzalez Deniselle MC; Gargiulo-Monachelli GM; Perez AF; Tourreilles M; Mattiazzi M; Ojeda C; Lotero Polesel D; De Nicola AF
[Ad] Endereço:Service of Neurology, Cir My 'Dr. Cosme Argerirch' Central Military Hospital, Buenos Aires, Argentina.
[Ti] Título:Neuroactive Steroids in Acute Ischemic Stroke: Association with Cognitive, Functional, and Neurological Outcomes.
[So] Source:Horm Metab Res;49(1):16-22, 2017 Jan.
[Is] ISSN:1439-4286
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Despite several scientific and technological advances, there is no single neuroprotective treatment that can reverse the brain damage after acute ischemic stroke (AIS). Neuroactive steroids are cholesterol-derived hormones that have the ability to modulate the normal and pathologic nervous system employing genomic and nongenomic mechanisms. In this work, we first investigated if AIS affects the plasma concentration of 5 neuroactive steroids (cortisol, estradiol, progesterone, testosterone, and 3α-androstenediol glucuronide). Second, we studied if levels of circulating steroids associate with neurological, cognitive, and functional outcome in a cohort of 60- to 90 year-old male and female patients with AIS. For this purpose, we recruited patients who were hospitalized at the Emergency Room of the Central Military Hospital within the first 24 h after stroke onset. We designed 2 experimental groups, each one composed of 30 control subjects and 30 AIS patients, both males and females. The assessment of neurological deficit was performed with the NIHSS and the tests used for the functional and cognitive status were: (1) modified Rankin Scale; (2) Photo test, and (3) abbreviated Pfeiffer's mental status questionnaire. We observed a significant difference in plasma concentration of cortisol and estradiol between both experimental groups. In the AIS group, higher levels of these neuroactive steroids were associated with more pronounced neurological, cognitive and functional deficits in women compared to men. We propose that in elderly patients, high levels of circulating neuroactive steroids like cortisol and estradiol could potentiate AIS-mediated neuropathology in the ischemic and penumbra areas.
[Mh] Termos MeSH primário: Androstenodióis/sangue
Isquemia Encefálica/sangue
Cognição/fisiologia
Hormônios Esteroides Gonadais/sangue
Hidrocortisona/sangue
Acidente Vascular Cerebral
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Isquemia Encefálica/diagnóstico
Isquemia Encefálica/fisiopatologia
Isquemia Encefálica/psicologia
Estudos de Casos e Controles
Feminino
Seres Humanos
Masculino
Meia-Idade
Neurotransmissores/sangue
Prognóstico
Recuperação de Função Fisiológica
Acidente Vascular Cerebral/sangue
Acidente Vascular Cerebral/diagnóstico
Acidente Vascular Cerebral/fisiopatologia
Acidente Vascular Cerebral/psicologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androstenediols); 0 (Gonadal Steroid Hormones); 0 (Neurotransmitter Agents); WI4X0X7BPJ (Hydrocortisone)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170327
[Lr] Data última revisão:
170327
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE
[do] DOI:10.1055/s-0042-119201


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[PMID]:26197789
[Au] Autor:Yang S; Lu J; Xu Y; Wang X
[Ad] Endereço:National Anti-doping Laboratory, China Anti-Doping Agency, 1st Anding Road, ChaoYang District, Beijing, 100029, P. R. China.
[Ti] Título:New oxymesterone metabolites in human by gas chromatography-tandem mass spectrometry and their application for doping control.
[So] Source:Drug Test Anal;8(7):633-43, 2016 Jul.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Oxymesterone (17α-methyl-4, 17ß-dihydroxy-androst-4-ene-3-one) is one of the anabolic androgenic steroids (AAS) banned by the World Anti-Doping Agency (WADA). The biotransformation of oxymesterone is performed in vitro by human heptocytes and human urinary metabolic profiles are investigated after single dose of 20 mg to two adult males as well. Cell cultures and urine samples were hydrolyzed by ß-glucuronidase, extracted, and reacted with N-Methyl-N-trimethylsilyltrifluoroacetamide (MSTFA), ammonium iodide (NH4 I), and dithioerythritol. After derivatization, a gas chromatography triple quadruple tandem mass spectrometry (GC-MS/MS) using full scan and MS/MS modes was applied. The total ion chromatographs of the blank and the positive samples are compared, and 7 new metabolites were found. In addition to the well-known 17-epioxymesterone, oxymesterone is metabolized by 4-ene-reduction, 3-keto-reduction, 11ß-hydroxylation, and 16ξ-hydroxylation. Based on the behavior of the MS/MS results of product ion and precursor ion modes, a GC-MS/MS method has been developed monitoring these metabolites. The structures of metabolite 2 and 4 are tentatively identified as 17α-methyl-3ß, 17ß-dihydroxy-5α-androstane-4-one and 17α-methyl-3α, 4ξ, 17ß-trihydroxy-5α-androstane, respectively. Detection of oxymesterone using new metabolites M2 and M4 can extend the detection window up to 4 days since the parent steroid was not detectable. Copyright © 2015 John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Androgênios/metabolismo
Androgênios/urina
Androstenodióis/metabolismo
Androstenodióis/urina
Cromatografia Gasosa-Espectrometria de Massas
Hepatócitos/metabolismo
[Mh] Termos MeSH secundário: Adulto
Androgênios/análise
Androstenodióis/análise
Linhagem Celular
Doping nos Esportes
Cromatografia Gasosa-Espectrometria de Massas/métodos
Hepatócitos/química
Hepatócitos/efeitos dos fármacos
Seres Humanos
Masculino
Meia-Idade
Detecção do Abuso de Substâncias/métodos
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androgens); 0 (Androstenediols); 0 (oxymesterone)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170315
[Lr] Data última revisão:
170315
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150723
[St] Status:MEDLINE
[do] DOI:10.1002/dta.1836


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[PMID]:26554883
[Au] Autor:Stanczyk FZ
[Ad] Endereço:Keck School of Medicine University of Southern California Los Angeles, California.
[Ti] Título:Effect of intravaginal dehydroepiandrosterone treatment on the endometrium: should androstenediol be a concern?
[So] Source:Menopause;22(12):1273-5, 2015 Dec.
[Is] ISSN:1530-0374
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Androstenodiol
Desidroepiandrosterona
[Mh] Termos MeSH secundário: Androstenodióis
Endométrio
Feminino
Seres Humanos
[Pt] Tipo de publicação:COMMENT; EDITORIAL
[Nm] Nome de substância:
0 (Androstenediols); 459AG36T1B (Dehydroepiandrosterone); 95PS51EMXY (Androstenediol)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:151201
[Lr] Data última revisão:
151201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151112
[St] Status:MEDLINE
[do] DOI:10.1097/GME.0000000000000558


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[PMID]:26203081
[Au] Autor:Prokai L; Nguyen V; Szarka S; Garg P; Sabnis G; Bimonte-Nelson HA; McLaughlin KJ; Talboom JS; Conrad CD; Shughrue PJ; Gould TD; Brodie A; Merchenthaler I; Koulen P; Prokai-Tatrai K
[Ad] Endereço:Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, Fort Worth, TX 76107, USA. AgyPharma LLC, Mansfield, TX 76063, USA. laszlo.prokai@unthsc.edu.
[Ti] Título:The prodrug DHED selectively delivers 17ß-estradiol to the brain for treating estrogen-responsive disorders.
[So] Source:Sci Transl Med;7(297):297ra113, 2015 Jul 22.
[Is] ISSN:1946-6242
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Many neurological and psychiatric maladies originate from the deprivation of the human brain from estrogens. However, current hormone therapies cannot be used safely to treat these conditions commonly associated with menopause because of detrimental side effects in the periphery. The latter also prevents the use of the hormone for neuroprotection. We show that a small-molecule bioprecursor prodrug, 10ß,17ß-dihydroxyestra-1,4-dien-3-one (DHED), converts to 17ß-estradiol in the brain after systemic administration but remains inert in the rest of the body. The localized and rapid formation of estrogen from the prodrug was revealed by a series of in vivo bioanalytical assays and through in vivo imaging in rodents. DHED treatment efficiently alleviated symptoms that originated from brain estrogen deficiency in animal models of surgical menopause and provided neuroprotection in a rat stroke model. Concomitantly, we determined that 17ß-estradiol formed in the brain from DHED elicited changes in gene expression and neuronal morphology identical to those obtained after direct 17ß-estradiol treatment. Together, complementary functional and mechanistic data show that our approach is highly relevant therapeutically, because administration of the prodrug selectively produces estrogen in the brain independently from the route of administration and treatment regimen. Therefore, peripheral responses associated with the use of systemic estrogens, such as stimulation of the uterus and estrogen-responsive tumor growth, were absent. Collectively, our brain-selective prodrug approach may safely provide estrogen neuroprotection and medicate neurological and psychiatric symptoms developing from estrogen deficiency, particularly those encountered after surgical menopause, without the adverse side effects of current hormone therapies.
[Mh] Termos MeSH primário: Androstenodióis/farmacologia
Encéfalo/metabolismo
Estradiol/metabolismo
Estrogênios/metabolismo
Pró-Fármacos/farmacologia
[Mh] Termos MeSH secundário: Androstenodióis/uso terapêutico
Animais
Antidepressivos/farmacologia
Antidepressivos/uso terapêutico
Biomarcadores/metabolismo
Encéfalo/efeitos dos fármacos
Isquemia Encefálica/complicações
Isquemia Encefálica/tratamento farmacológico
Neoplasias da Mama/tratamento farmacológico
Neoplasias da Mama/patologia
Proliferação Celular/efeitos dos fármacos
Modelos Animais de Doenças
Estradiol/química
Estrogênios/química
Feminino
Seres Humanos
Células MCF-7
Neuroproteção/efeitos dos fármacos
Pró-Fármacos/metabolismo
Acidente Vascular Cerebral/complicações
Acidente Vascular Cerebral/tratamento farmacológico
Útero/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androstenediols); 0 (Antidepressive Agents); 0 (Biomarkers); 0 (Estrogens); 0 (Prodrugs); 131061-48-8 (3,16-dihydroxyandrost-5-ene-17,19-dione); 4TI98Z838E (Estradiol)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150724
[St] Status:MEDLINE
[do] DOI:10.1126/scitranslmed.aab1290


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[PMID]:25814068
[Au] Autor:Cui J; Lin Q; Gan C; Zhan J; Su W; Zhao D; Qi B; Huang Y
[Ad] Endereço:College of Chemistry and Materials Science, Guangxi Teachers Education University, Nanning 530001, China.
[Ti] Título:Synthesis and antiproliferative evaluation of some novel B-nor-D-homosteroids.
[So] Source:Steroids;98:138-42, 2015 Jun.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Using 3ß-hydroxy-5-androsten-17-one as a starting material, a series of novel nitrogen-containing B-nor-D-homosteroids were designed and synthesized by the oximation, Beckman rearrangement, ozonation, cyclization and condensation reaction. The structures of all new compounds were determined by analysis of their NMR, MS and IR spectra. The antiproliferative activity of compounds was evaluated against HT-29 (colonic carcinoma), HeLa (human cervical carcinoma) and Bel 7404 (human liver carcinoma) cells.
[Mh] Termos MeSH primário: Androstenodióis/química
Antineoplásicos
Proliferação Celular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Antineoplásicos/farmacologia
Ensaios de Seleção de Medicamentos Antitumorais
Células HeLa
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3,15-dihydroxy-5-androst-en-17-one); 0 (Androstenediols); 0 (Antineoplastic Agents)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150429
[Lr] Data última revisão:
150429
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150328
[St] Status:MEDLINE


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[PMID]:24709032
[Au] Autor:Cleary MR; Andersson PF; Broberg A; Elfstrand M; Daniel G; Stenlid J
[Ad] Endereço:Department of Forest Mycology and Plant Pathology, Uppsala BioCenter, Swedish University of Agricultural Sciences, Almas allé 5, PO Box 7026, SE-750 07 Uppsala, Sweden. Electronic address: Michelle.Cleary@slu.se.
[Ti] Título:Genotypes of Fraxinus excelsior with different susceptibility to the ash dieback pathogen Hymenoscyphus pseudoalbidus and their response to the phytotoxin viridiol - a metabolomic and microscopic study.
[So] Source:Phytochemistry;102:115-25, 2014 Jun.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Eight European ash (Fraxinus excelsior) genotypes with different known susceptibility to Hymenoscyphus pseudoalbidus were tested against the phytotoxin viridiol and their response described at the microscopic and metabolomic level. All ash genotypes were sensitive to the toxin and necrosis was detectable after 24h. Among the three viridiol concentrations used in the experiment, the lowest concentration (14.7µM) yielded markedly lower mean damage scores compared to those resulting from seedlings tested at higher dosages. The highest damage scores were associated with the susceptible ash clones S-101, S-106 and S-125, but also with resistant clone R-104. Three resistant clones (R-131, R-121, and R-118) had lower mean damage scores compared to susceptible clones. Wilting of leaves was more common 48h after treatment and more pronounced on seedlings with high damage scores. The resulting lesions generally lacked browning of tissue and displayed only surface disruption of cells in direct contact with the toxin. A delay in symptom development was evident on all five resistant clones tested with the two higher concentrations of viridiol. LC-HRMS and MS/MS analyses of ash seedling extracts suggest several secoiridoid compounds as well as compounds related to abscisic acid (ABA) to be produced in response to viridiol. ABA-cysteine and xanthoxin were found at significantly higher concentrations in susceptible clones compared to resistant clones after treatment with viridiol, suggesting a primary role of ABA in response to stress. The results observed in this study suggest that genetic resistance to H. pseudoalbidus among ash genotypes may be explained, in part, by the varied response to phytotoxins produced by the fungus.
[Mh] Termos MeSH primário: Androstenodióis/farmacologia
Ascomicetos/fisiologia
Fraxinus
Genótipo
Metabolômica
Doenças das Plantas/microbiologia
[Mh] Termos MeSH secundário: Ascomicetos/patogenicidade
Fraxinus/efeitos dos fármacos
Fraxinus/genética
Fraxinus/metabolismo
Fraxinus/microbiologia
Variação Genética/efeitos dos fármacos
Doenças das Plantas/genética
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Androstenediols); 23820-80-6 (viridiol)
[Em] Mês de entrada:1412
[Cu] Atualização por classe:140423
[Lr] Data última revisão:
140423
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140409
[St] Status:MEDLINE


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[PMID]:24239478
[Au] Autor:Dobricic V; Markovic B; Nikolic K; Savic V; Vladimirov S; Cudina O
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11000 Belgrade, Serbia. Electronic address: vladimir@pharmacy.bg.ac.rs.
[Ti] Título:17ß-carboxamide steroids--in vitro prediction of human skin permeability and retention using PAMPA technique.
[So] Source:Eur J Pharm Sci;52:95-108, 2014 Feb 14.
[Is] ISSN:1879-0720
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this paper, twenty-two 17ß-carboxamide steroids were synthesized from five corticosteroids (hydrocortisone, prednisolone, methylprednisolone, dexamethasone and betamethasone) in two steps. The first step was periodic acid oxydation of these corticosteroids to corresponding cortienic acids and the second step was amidation of thus obtained cortienic acids with esterified l-amino acids. These compounds are potential soft corticosteroids with local anti-inflammatory activity in the skin. Parallel artificial membrane permeability assay (PAMPA) was applied in order to predict permeability and retention of these compounds in human skin. Comparison of permeability and retention parameters between 17ß-carboxamide steroids and corresponding corticosteroids was performed. Compounds with significantly higher retention were identified and the derivative that does not have significantly higher permeability was underlined. Molecular structures of all compounds were optimized by use of Gaussian semiempirical/PM3 method. Geometrical, thermodynamic, physicochemical and electronical molecular parameters of the optimized structures were calculated and quantitative structure-property relationship (QSPR) analysis was performed in order to explain permeability and retention of these compounds. ANN-, PLS- and MLR-QSPR models were created. Quality of these models was evaluated by commonly used statistical parameters and the most reliable models were selected. Analyzing descriptors in the selected models, main molecular properties that influence permeability and retention in the PAMPA artificial membrane were identified. Based on these data, further structural modifications could be applied in order to increase retention without significant increase of permeability, which can positively affect potential local anti-inflammatory activity of these compounds. Selected QSPR models could be used as in silico tool for predicting human skin permeability and retention of novel 17ß-carboxamide steroids without performing PAMPA experiments.
[Mh] Termos MeSH primário: Corticosteroides/metabolismo
Amidas/metabolismo
Membranas Artificiais
Absorção Cutânea
[Mh] Termos MeSH secundário: Corticosteroides/química
Amidas/química
Androstenodióis/química
Seres Humanos
Permeabilidade
Relação Quantitativa Estrutura-Atividade
Pele/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenal Cortex Hormones); 0 (Amides); 0 (Androstenediols); 0 (Membranes, Artificial); 81738132XU (cortienic acid)
[Em] Mês de entrada:1409
[Cu] Atualização por classe:140113
[Lr] Data última revisão:
140113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131119
[St] Status:MEDLINE


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[PMID]:25436712
[Au] Autor:Enríquez J; Larrea F; Santillán R; Hernández Á; Herrero B; Pérez-Palacios G; Lemus AE
[Ad] Endereço:Department of Reproductive Biology, Dr. Carlos Gual Castro, National Institute of Medical Sciences and Nutrition Salvador Zubirán, Mexico. juanaenriquez@yahoo.com.mx
[Ti] Título:Neonatal rat osteoblasts bioconvert testosterone to non-phenolic metabolites with estrogen-like effects on bone cell proliferation and differentiation.
[So] Source:Horm Mol Biol Clin Investig;13(3):41-9, 2013 Jun.
[Is] ISSN:1868-1891
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Testosterone (T) restores bone mass loss in postmenopausal women and osteoporotic men mainly through its bioconversion to estradiol (E2). In target tissues, T is also biotransformed to the A-ring-reduced metabolites 3α,5α-androstanediol (3α,5α-diol) and 3ß,5α-androstanediol (3ß,5α-diol), which are potent estrogen receptor (ER) agonists; however, their biological role in bone has not been completely elucidated. To assess if osteoblasts bioconvert T to 3α,5α-diol and to 3ß,5α-diol, we studied in cultured neonatal rat osteoblasts the metabolism of [14C]-labeled T. In addition, the intrinsic estrogenic potency of diols on cell proliferation and differentiation in neonatal calvarial rat osteoblasts was also investigated. Osteoblast function was assessed by determining cell DNA, cell-associated osteocalcin, and calcium content, as well as alkaline phosphatase activity and Alp1 gene expression. The results demonstrated that diols were the major bioconversion products of T, with dihydrotestosterone being an obligatory intermediary, thus demonstrating in the rat osteoblasts the activities of 5α-steroid reductase and 3α- and 3ß-hydroxysteroid dehydrogenases. The most important finding was that 3ß,5α- and 3α,5α-diols induced osteoblast proliferation and differentiation, mimicking the effect of E2. The observation that osteoblast differentiation induced by diols was abolished by the presence of the antiestrogen ICI 182,780, but not by the antiandrogen 2-hydroxyflutamide, suggests that diols effects are mediated through an ER mechanism. The osteoblast capability to bioconvert T into diols with intrinsic estrogen-like potency offers new insights to understand the mechanism of action of T on bone cells and provides new avenues for hormone replacement therapy to maintain bone mass density.
[Mh] Termos MeSH primário: Estrogênios/metabolismo
Osteoblastos/citologia
Osteoblastos/metabolismo
Testosterona/metabolismo
[Mh] Termos MeSH secundário: Androstenodióis/metabolismo
Animais
Diferenciação Celular
Proliferação Celular
Células Cultivadas
Feminino
Masculino
Osteogênese
Ratos
Ratos Wistar
Receptores Estrogênicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Androstenediols); 0 (Estrogens); 0 (Receptors, Estrogen); 3XMK78S47O (Testosterone)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:141202
[Lr] Data última revisão:
141202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141202
[St] Status:MEDLINE



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