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[PMID]:27133901
[Au] Autor:Hussain Z; Dastagir N; Hussain S; Jabeen A; Zafar S; Malik R; Bano S; Wajid A; Choudhary MI
[Ad] Endereço:H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
[Ti] Título:Aspergillus niger-mediated biotransformation of methenolone enanthate, and immunomodulatory activity of its transformed products.
[So] Source:Steroids;112:68-73, 2016 Aug.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two fungal cultures Aspergillus niger and Cunninghamella blakesleeana were used for the biotransformation of methenolone enanthate (1). Biotransformation with A. niger led to the synthesis of three new (2-4), and three known (5-7) metabolites, while fermentation with C. blakesleeana yielded metabolite 6. Substrate 1 and the resulting metabolites were evaluated for their immunomodulatory activities. Substrate 1 was found to be inactive, while metabolites 2 and 3 showed a potent inhibition of ROS generation by whole blood (IC50=8.60 and 7.05µg/mL), as well as from isolated polymorphonuclear leukocytes (PMNs) (IC50=14.0 and 4.70µg/mL), respectively. Moreover, compound 3 (34.21%) moderately inhibited the production of TNF-α, whereas 2 (88.63%) showed a potent inhibition of TNF-α produced by the THP-1 cells. These activities indicated immunomodulatory potential of compounds 2 and 3. All products were found to be non-toxic to 3T3 mouse fibroblast cells.
[Mh] Termos MeSH primário: Aspergillus niger/metabolismo
Fatores Imunológicos/metabolismo
Fatores Imunológicos/farmacologia
Metenolona/análogos & derivados
[Mh] Termos MeSH secundário: Adulto
Biotransformação
Células Cultivadas
Cunninghamella/metabolismo
Fermentação/fisiologia
Seres Humanos
Fatores Imunológicos/química
Metenolona/química
Metenolona/metabolismo
Estrutura Molecular
Neutrófilos/efeitos dos fármacos
Neutrófilos/metabolismo
Espécies Reativas de Oxigênio/metabolismo
Fator de Necrose Tumoral alfa/metabolismo
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Immunologic Factors); 0 (Reactive Oxygen Species); 0 (Tumor Necrosis Factor-alpha); 0SPD480WFH (methenolone enanthate); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170705
[Lr] Data última revisão:
170705
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160503
[St] Status:MEDLINE


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[PMID]:26519767
[Au] Autor:He G; Yang S; Lu J; Xu Y
[Ad] Endereço:National Anti-doping Laboratory, China Anti-Doping Agency, 1st Anding Road, ChaoYang District, Beijing 100029, PR China; Sport Science College, Beijing Sport University, Beijing 100084, PR China.
[Ti] Título:New long term metabolite in human urine for metenolone misuse by liquid chromatography quadrupole time-of-flight mass spectrometry.
[So] Source:Steroids;105:1-11, 2016 Jan.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In this study, metenolone metabolic profiles were investigated. Metenolone was administered to one healthy male volunteer. Liquid-liquid extraction and direct-injection were applied to processing urine samples. Urinary extracts were analyzed by liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOFMS) using full scan and product ion scan with accurate mass measurement for the first time. Due to the lack of useful fragment ion for structural elucidation, GC-MS instrumentation was employed to obtain structural details of the trimethylsilylated phase I metabolite released after hydrolysis, and the EI mass spectrum was always informative in steroidal structure studies owing to more useful fragment ions than the ESI mass spectrum. 16 metabolites including 6 glucuronide and 9 unreported sulfate conjugates were characterized and tentatively identified. All the metabolites were evaluated in terms of how long they could be detected. The sulfate conjugate S6 (1-methylen-5α-androst-3,17-dione-2ξ-sulfate) was considered to be a new long term metabolite for metenolone misuse that could be detected 40 days by liquid-liquid extraction and up to 30 days by direct-injection analysis after oral administration.
[Mh] Termos MeSH primário: Cromatografia Líquida/métodos
Espectrometria de Massas/métodos
Metaboloma
Metenolona/urina
Transtornos Relacionados ao Uso de Substâncias/urina
[Mh] Termos MeSH secundário: Doping nos Esportes/prevenção & controle
Cromatografia Gasosa-Espectrometria de Massas
Glucuronídeos/metabolismo
Seres Humanos
Masculino
Metenolona/química
Peso Molecular
Espectrometria de Massas por Ionização por Electrospray
Sulfatos/metabolismo
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Glucuronides); 0 (Sulfates); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151101
[St] Status:MEDLINE


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[PMID]:26259657
[Au] Autor:Fragkaki AG; Angelis YS; Kiousi P; Georgakopoulos CG; Lyris E
[Ad] Endereço:Doping Control Laboratory of Athens, Olympic Athletic Center of Athens 'Spyros Louis', 37 Kifisias Avenue, 15123, Marousi, Greece.
[Ti] Título:Comparison of sulfo-conjugated and gluco-conjugated urinary metabolites for detection of methenolone misuse in doping control by LC-HRMS, GC-MS and GC-HRMS.
[So] Source:J Mass Spectrom;50(5):740-8, 2015 May.
[Is] ISSN:1096-9888
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Methenolone (17ß-hydroxy-1-methyl-5α-androst-1-en-3-one) misuse in doping control is commonly detected by monitoring the parent molecule and its metabolite (1-methylene-5α-androstan-3α-ol-17-one) excreted conjugated with glucuronic acid using gas chromatography-mass spectrometry (GC-MS) and liquid chromatography mass spectrometry (LC-MS) for the parent molecule, after hydrolysis with ß-glucuronidase. The aim of the present study was the evaluation of the sulfate fraction of methenolone metabolism by LC-high resolution (HR)MS and the estimation of the long-term detectability of its sulfate metabolites analyzed by liquid chromatography tandem mass spectrometry (LC-HRMSMS) compared with the current practice for the detection of methenolone misuse used by the anti-doping laboratories. Methenolone was administered to two healthy male volunteers, and urine samples were collected up to 12 and 26 days, respectively. Ethyl acetate extraction at weak alkaline pH was performed and then the sulfate conjugates were analyzed by LC-HRMS using electrospray ionization in negative mode searching for [M-H](-) ions corresponding to potential sulfate structures (comprising structure alterations such as hydroxylations, oxidations, reductions and combinations of them). Eight sulfate metabolites were finally detected, but four of them were considered important as the most abundant and long term detectable. LC clean up followed by solvolysis and GC/MS analysis of trimethylsilylated (TMS) derivatives reveal that the sulfate analogs of methenolone as well as of 1-methylene-5α-androstan-3α-ol-17-one, 3z-hydroxy-1ß-methyl-5α-androstan-17-one and 16ß-hydroxy-1-methyl-5α-androst-1-ene-3,17-dione were the major metabolites in the sulfate fraction. The results of the present study also document for the first time the methenolone sulfate as well as the 3z-hydroxy-1ß-methyl-5α-androstan-17-one sulfate as metabolites of methenolone in human urine. The time window for the detectability of methenolone sulfate metabolites by LC-HRMS is comparable with that of their hydrolyzed glucuronide analogs analyzed by GC-MS. The results of the study demonstrate the importance of sulfation as a phase II metabolic pathway for methenolone metabolism, proposing four metabolites as significant components of the sulfate fraction.
[Mh] Termos MeSH primário: Doping nos Esportes
Cromatografia Gasosa-Espectrometria de Massas/métodos
Glucuronídeos/urina
Metenolona/urina
Sulfatos/urina
[Mh] Termos MeSH secundário: Adulto
Cromatografia Líquida/métodos
Glucuronídeos/química
Glucuronídeos/metabolismo
Seres Humanos
Masculino
Metenolona/química
Metenolona/metabolismo
Meia-Idade
Sulfatos/química
Sulfatos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Glucuronides); 0 (Sulfates); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:150811
[Lr] Data última revisão:
150811
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150812
[St] Status:MEDLINE
[do] DOI:10.1002/jms.3583


  4 / 169 MEDLINE  
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[PMID]:25319132
[Au] Autor:Edvardsson B
[Ad] Endereço:Department of Clinical Sciences, Lund University, Skane University Hospital, Lund, 221 85, Sweden, Bengt.Edvardsson@med.lu.se.
[Ti] Título:Hypertensive encephalopathy associated with anabolic-androgenic steroids used for bodybuilding.
[So] Source:Acta Neurol Belg;115(3):457-8, 2015 Sep.
[Is] ISSN:2240-2993
[Cp] País de publicação:Italy
[La] Idioma:eng
[Mh] Termos MeSH primário: Anabolizantes/efeitos adversos
Androgênios/efeitos adversos
Encefalopatia Hipertensiva/induzido quimicamente
Metandrostenolona/efeitos adversos
Metenolona/análogos & derivados
[Mh] Termos MeSH secundário: Seres Humanos
Imagem por Ressonância Magnética
Masculino
Metenolona/efeitos adversos
Adulto Jovem
[Pt] Tipo de publicação:CASE REPORTS; LETTER
[Nm] Nome de substância:
0 (Anabolic Agents); 0 (Androgens); 0SPD480WFH (methenolone enanthate); 9062ZT8Q5C (Methenolone); COZ1R7EOCC (Methandrostenolone)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:150824
[Lr] Data última revisão:
150824
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141017
[St] Status:MEDLINE
[do] DOI:10.1007/s13760-014-0378-8


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[PMID]:24681931
[Au] Autor:Shimoda K; Takenaka K; Kitanaka A; Akashi K
[Ti] Título:[Clinical aspects of primary myelofibrosis in Japan].
[So] Source:Rinsho Ketsueki;55(3):289-94, 2014 03.
[Is] ISSN:0485-1439
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Mh] Termos MeSH primário: Mielofibrose Primária
[Mh] Termos MeSH secundário: Contagem de Células Sanguíneas
Danazol/uso terapêutico
Transplante de Células-Tronco Hematopoéticas/métodos
Seres Humanos
Hidroxiureia/uso terapêutico
Japão
Metenolona/análogos & derivados
Metenolona/uso terapêutico
Cuidados Paliativos
Prednisolona/uso terapêutico
Mielofibrose Primária/sangue
Mielofibrose Primária/mortalidade
Mielofibrose Primária/fisiopatologia
Mielofibrose Primária/terapia
Prognóstico
Radioterapia/métodos
Baço
Taxa de Sobrevida
Condicionamento Pré-Transplante
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
9062ZT8Q5C (Methenolone); 9PHQ9Y1OLM (Prednisolone); N29QWW3BUO (Danazol); W75590VPKQ (methenolone acetate); X6Q56QN5QC (Hydroxyurea)
[Em] Mês de entrada:1406
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140401
[St] Status:MEDLINE


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[PMID]:24062630
[Au] Autor:Ikeda S; Kamikawa Y; Ohwatashi A; Harada K; Yoshida A
[Ad] Endereço:Department of Rehabilitation and Physical Medicine, Graduate School of Medical and Dental Sciences, Kagoshima University, 8-35-1 Sakuragaoka, Kagoshima 890-8506, Japan.
[Ti] Título:The effect of anabolic steroid administration on passive stretching-induced expression of mechano-growth factor in skeletal muscle.
[So] Source:ScientificWorldJournal;2013:313605, 2013.
[Is] ISSN:1537-744X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Stretching of skeletal muscle induces expression of the genes which encode myogenic transcription factors or muscle contractile proteins and results in muscle growth. Anabolic steroids are reported to strengthen muscles. We have previously studied the effects of muscle stretching on gene expression. Here, we studied the effect of a combination of passive stretching and the administration of an anabolic steroid on mRNA expression of a muscle growth factor, insulin-like growth factor-I autocrine variant, or mechano-growth factor (MGF). METHODS: Twelve 8-week-old male Wistar rats were used. Metenolone was administered and passive repetitive dorsiflexion and plantar flexion of the ankle joint performed under deep anesthesia. After 24 h, the gastrocnemius muscles were removed and the mRNA expression of insulin-like growth factor-I autocrine variant was measured using quantitative real-time polymerase chain reaction. RESULTS: Repetitive stretching in combination with metenolone, but not stretching alone, significantly increased MGF mRNA expression. CONCLUSION: Anabolic steroids enhance the effect of passive stretching on MGF expression in skeletal muscle.
[Mh] Termos MeSH primário: Anabolizantes/farmacologia
Fator de Crescimento Insulin-Like I/metabolismo
Mecanotransdução Celular/efeitos dos fármacos
Metenolona/farmacologia
Exercícios de Alongamento Muscular
Músculo Esquelético/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Fator de Crescimento Insulin-Like I/genética
Masculino
Músculo Esquelético/metabolismo
Músculo Esquelético/fisiologia
RNA Mensageiro/metabolismo
Ratos
Ratos Wistar
Reação em Cadeia da Polimerase em Tempo Real
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anabolic Agents); 0 (RNA, Messenger); 0 (mechano-growth factor, rat); 67763-96-6 (Insulin-Like Growth Factor I); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130925
[St] Status:MEDLINE
[do] DOI:10.1155/2013/313605


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[PMID]:23280519
[Au] Autor:Ozdemir O; Bozkurt I; Ozdemir M; Yavuz O
[Ad] Endereço:Selcuk University Faculty of Veterinary Medicine, Department of Pathology, 42079, Campus, Konya, Turkey. oozdemir@selcuk.edu.tr
[Ti] Título:Side effect of metenolone enanthate on rats heart in puberty: morphometrical study.
[So] Source:Exp Toxicol Pathol;65(6):745-50, 2013 Sep.
[Is] ISSN:1618-1433
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The aim of this study was the investigation of effects of the metenolone enanthate (ME) that is used among athletes as doping and muscle amplifier, on hearts of male and female rats that are in puberty using morphometrical methods. A total of 36 rats which were divided into three separate groups (Experiment, ME; vehicle, PO; control, C) each consisting of 6 male and 6 female rats were used. 0.5 mg/kg metenolone enanthate was applied intraperitoneally into experiment subjects 5 times a week over a period of 4 weeks. At the end of experiment, rats were euthanized and their hearts were cut at the level of musculus papillaris after the fixation in formalin. Hearts were taken out and embedded in paraffin wax. Photos were taken at cut surfaces, and thickness, diameters and surface area levels were measured. Left ventriculus mass (LVM) and left ventriculus mass index (LVMI) were calculated. In the study LVM (p<0.005) and LVMI (p<0.05) were found to be significantly higher in the ME group in females whereas left ventricular lumen diameter (LVLD) were found to be significantly lower (p<0.05). Thus left ventricular hypertrophy development was observed. LVM and LVMI were found to be similar in ME and C groups among male rats and the highest level of these data were found in the group. LVM and LVMI were higher among females (p<0.006). In conclusion, it has been shown that the adverse effects of ME on heart were developing starting from puberty and resulting with the enlargement of the heart and left ventricular hypertrophy and especially among females this condition was more evident. It has also been discussed that the continuous use of drugs may further enhance this condition.
[Mh] Termos MeSH primário: Envelhecimento/efeitos dos fármacos
Anabolizantes/toxicidade
Coração/efeitos dos fármacos
Hipertrofia Ventricular Esquerda/induzido quimicamente
Metenolona/análogos & derivados
Caracteres Sexuais
[Mh] Termos MeSH secundário: Envelhecimento/patologia
Animais
Peso Corporal/efeitos dos fármacos
Feminino
Coração/crescimento & desenvolvimento
Hipertrofia Ventricular Esquerda/patologia
Masculino
Metenolona/toxicidade
Tamanho do Órgão/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anabolic Agents); 0SPD480WFH (methenolone enanthate); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1402
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130103
[St] Status:MEDLINE


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[PMID]:21449972
[Au] Autor:Iijima M; Shigehara K; Sugimoto K; Kouji I; Fukushima M; Maeda Y; Konaka H; Mizokami A; Koh E; Namiki M
[Ad] Endereço:Department of Integrative Cancer Therapy and Urology, Kanazawa University Graduate School of Medical Science, Kanazawa, Ishikawa, Japan. mercy1980@yahoo.co.jp
[Ti] Título:Myelodysplastic syndrome treated effectively with testosterone enanthate.
[So] Source:Int J Urol;18(6):469-71, 2011 Jun.
[Is] ISSN:1442-2042
[Cp] País de publicação:Australia
[La] Idioma:eng
[Ab] Resumo:We report a case of myelodysplastic syndrome (MDS) treated effectively with testosterone enanthate. A 70-year-old man was diagnosed with low-risk MDS in 1998, and he was first given methenolone acetate orally because of gradual progression of anemia and thrombocytopenia. However, this treatment was not effective, so we changed the treatment to testosterone enanthate because of his symptoms with late-onset hypogonadism. Three months after testosterone replacement therapy (TRT), anemia and thrombocytopenia had improved, and mean platelet count and hemoglobin had significant increases from 2.36 ± 0.45 × 10(4) to 3.83 ± 0.78 × 10(4) /µL, and from 11.7 ± 0.81 to 15.2 ± 1.00 g/dL, respectively, which contributed to a decrease in platelet transfusion requirement. Since then, the patient has been on a good clinical course. The present case suggests that testosterone enanthate administration could be an alternative treatment for men with MDS, even in the case where treatment with anabolic-androgenic steroids is not successful, and suggests another interesting effect of TRT on platelets.
[Mh] Termos MeSH primário: Androgênios/uso terapêutico
Síndromes Mielodisplásicas/tratamento farmacológico
Testosterona/análogos & derivados
[Mh] Termos MeSH secundário: Idoso
Seres Humanos
Masculino
Metenolona/análogos & derivados
Metenolona/uso terapêutico
Testosterona/uso terapêutico
Falha de Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androgens); 3XMK78S47O (Testosterone); 7Z6522T8N9 (testosterone enanthate); 9062ZT8Q5C (Methenolone); W75590VPKQ (methenolone acetate)
[Em] Mês de entrada:1109
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110401
[St] Status:MEDLINE
[do] DOI:10.1111/j.1442-2042.2011.02757.x


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[PMID]:21439121
[Au] Autor:Sequeiros RC; Neng NR; Portugal FC; Pinto ML; Pires J; Nogueira JM
[Ad] Endereço:University of Lisbon, Faculty of Sciences, Chemistry and Biochemistry Department and Center of Chemistry and Biochemistry, Campo Grande Ed. C8, 1749-016 Lisbon, Portugal.
[Ti] Título:Development and application of stir bar sorptive extraction with polyurethane foams for the determination of testosterone and methenolone in urine matrices.
[So] Source:J Chromatogr Sci;49(4):297-302, 2011 Apr.
[Is] ISSN:1945-239X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This work describes the development, validation, and application of a novel methodology for the determination of testosterone and methenolone in urine matrices by stir bar sorptive extraction using polyurethane foams [SBSE(PU)] followed by liquid desorption and high-performance liquid chromatography with diode array detection. The methodology was optimized in terms of extraction time, agitation speed, pH, ionic strength and organic modifier, as well as back-extraction solvent and desorption time. Under optimized experimental conditions, convenient accuracy were achieved with average recoveries of 49.7 8.6% for testosterone and 54.2 ± 4.7% for methenolone. Additionally, the methodology showed good precision (<9%), excellent linear dynamic ranges (>0.9963) and convenient detection limits (0.2-0.3 µg/L). When comparing the efficiency obtained by SBSE(PU) and with the conventional polydimethylsiloxane phase [SBSE(PDMS)], yields up to four-fold higher are attained for the former, under the same experimental conditions. The application of the proposed methodology for the analysis of testosterone and methenolone in urine matrices showed negligible matrix effects and good analytical performance.
[Mh] Termos MeSH primário: Fracionamento Químico/métodos
Metenolona/urina
Poliuretanos/química
Testosterona/urina
[Mh] Termos MeSH secundário: Adulto
Cromatografia Líquida de Alta Pressão
Seres Humanos
Concentração de Íons de Hidrogênio
Masculino
Concentração Osmolar
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Polyurethanes); 3XMK78S47O (Testosterone); 9009-54-5 (polyurethane foam); 9062ZT8Q5C (Methenolone)
[Em] Mês de entrada:1107
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110329
[St] Status:MEDLINE


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[PMID]:21381223
[Au] Autor:Wong JK; Tang FP; Wan TS
[Ad] Endereço:Racing Laboratory, The Hong Kong Jockey Club, Sha Tin Racecourse, Sha Tin, N.T., Hong Kong, China. jenny.ky.wong@hkjc.org.hk
[Ti] Título:In vitro metabolic studies using homogenized horse liver in place of horse liver microsomes.
[So] Source:Drug Test Anal;3(6):393-9, 2011 Jun.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The study of the metabolism of drugs, in particular steroids, by both in vitro and in vivo methods has been carried out in the authors' laboratory for many years. For in vitro metabolic studies, the microsomal fraction isolated from horse liver is often used. However, the process of isolating liver microsomes is cumbersome and tedious. In addition, centrifugation at high speeds (over 100 000 g) may lead to loss of enzymes involved in phase I metabolism, which may account for the difference often observed between in vivo and in vitro results. We have therefore investigated the feasibility of using homogenized horse liver instead of liver microsomes with the aim of saving preparation time and improving the correlation between in vitro and in vivo results. Indeed, the preparation of the homogenized horse liver was very simple, needing only to homogenize the required amount of liver. Even though no further purification steps were performed before the homogenized liver was used, the cleanliness of the extracts obtained, based on gas chromatography-mass spectrometry (GC-MS) analysis, was similar to that for liver microsomes. Herein, the results of the in vitro experiments carried out using homogenized horse liver for five anabolic steroids-turinabol, methenolone acetate, androst-4-ene-3,6,17-trione, testosterone, and epitestosterone-are discussed. In addition to the previously reported in vitro metabolites, some additional known in vivo metabolites in the equine could also be detected. As far as we know, this is the first report of the successful use of homogenized liver in the horse for carrying out in vitro metabolism experiments. Copyright © 2011 John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Extratos Hepáticos/metabolismo
Microssomos Hepáticos/metabolismo
Preparações Farmacêuticas/metabolismo
[Mh] Termos MeSH secundário: Androgênios/análise
Androgênios/metabolismo
Androstenos/análise
Androstenos/metabolismo
Animais
Biotransformação
Epitestosterona/análise
Epitestosterona/metabolismo
Cromatografia Gasosa-Espectrometria de Massas
Cavalos
Técnicas In Vitro
Fígado/metabolismo
Metenolona/análogos & derivados
Metenolona/análise
Metenolona/metabolismo
Estrutura Molecular
Preparações Farmacêuticas/análise
Testosterona/análogos & derivados
Testosterona/análise
Testosterona/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androgens); 0 (Androstenes); 0 (Liver Extracts); 0 (Pharmaceutical Preparations); 3XMK78S47O (Testosterone); 481-30-1 (Epitestosterone); 855-19-6 (turinabol); 9062ZT8Q5C (Methenolone); L8L0381OBP (androst-4-ene-3,6,17-trione); W75590VPKQ (methenolone acetate)
[Em] Mês de entrada:1204
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110308
[St] Status:MEDLINE
[do] DOI:10.1002/dta.273



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