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472514568

至尊木虫 (职业作家)

小木虫议政大臣兼协办大学士

应助: 0 (幼儿园)
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金币: 15726.8
散金: 25
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帖子: 3248
在线: 224.2小时
虫号: 713538
注册: 2009-03-03
性别: GG
专业: 临床药理

[交流] 求文献一篇有链接

【作者(必填)】 Deng Y, Bi HC, Zhao LZ, Wang XD, Chen J, Ou ZM, Ding L, Xu LJ, Guan S, Chen X, Zhou SF, Huang M.
【文题(必填)】 Induction of cytochrome P450 3A by the Ginkgo biloba extract and bilobalides in human and rat primary hepatocytes.
【期刊名,年份,卷(期),起止页码(必填)】 Drug Metab Lett. 2008 Jan;2(1):60-6.
【全文链接或数据库名称(选填)】 http://www.ncbi.nlm.nih.gov/pubmed/19356072

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1楼2010-04-11 15:25:10

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luoxianyang

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专业: 药物代谢与药物动力学

472514568(金币+1, 博学EPI+1):虽然没有找到全文但还是很感谢你 2010-04-12 16:30

仅找到摘要，不好意思。
Abstract:

Ginkgo biloba is one of the most popular herbal medicines in the world, due to its purported pharmacological effects, including memory-enhancing, cognition-improving, and antiplatelet effects. The study aimed to investigate the activity and expression of cytochrome P450 (CYP) 3A in human and rat primary hepatocytes treated with standardized G. biloba extract (100, 500, and 2500 ng/ml) for 72 hr, and to measure the protein expression of CYP3A in human and rat primary hepatocytes treated with bilobalide (2, 10, and 50 ng/ml) and ginkgolides B (2, 10, and 50 ng/ml). The activity of CYP3A was measured by the quantification of dehydronifedipine formation using a validated tandem liquid chromatography mass spectrometry (LC/MS/MS) method. The levels of mRNA and protein of CYP3A were determined by reverse transcription-polymerase chain reaction (RT-PCR) and Western-blotting analysis, respectively. The G. biloba extract at 100-2,500 ng/ml significantly induced the activity, protein and mRNA expression of CYP3A in a dose-dependent manner in human and rat primary hepatocytes. Bilobalide at 2-50 ng/ml significantly increased CYP3A protein expression in a dose-dependent manner in human and rat primary hepatocytes. However, ginkgolide B did not affect CYP3A protein expression in vitro. The results indicate that G. biloba extract pretreatment significantly induced the expression of CYP3A protein and mRNA and increased CYP3A activity, and there was no significant species difference between human and rat. G. biloba may cause potential interactions with substrate drugs of CYP3A. Bilobalide might play a key role in the enzyme- inducing effects of G. biloba extract. Further study is needed to identify the substances in GBE that induce CYPs in vivo, and elucidate the molecular mechanism of CYP3A induction by GBE and bilobalides.

Keywords: Ginkgo biloba extract; bilobalide; ginkgolide B; cytochrome P450; CYP3A; induction; human and rat primary hepatocytes

Document Type: Research article

DOI: 10.2174/187231208783478489

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