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首页> 外文期刊>The American Journal of Chinese Medicine >Herb-Drug Interaction of 50 Chinese Herbal Medicines on CYP3A4 Activity in Vitro and in Vivo
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Herb-Drug Interaction of 50 Chinese Herbal Medicines on CYP3A4 Activity in Vitro and in Vivo

机译：50种中草药对CYP3A4活性的体内外相互作用

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摘要

The purpose of this study is to evaluate the effects of Chinese herbal medicines on the enzymatic activity of CYP3A4 and the possible metabolism-based herb-drug interactions in human liver microsomes and in rats. Fifty single-herbal preparations were screened for the activity of CYP3A4 using human liver microsomes for an in vitro probe reaction study. The enzymatic activity of CYP3A4 was estimated by determing the 6β-hydroxytestosterone metabolized from testosterone performed on a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Huang Qin (Scutellaria baicalensis Geprgi), Mu Dan Pi (Paeonia suffruticosa Andr.), Ji Shiee Terng (Spatholobus suberectus Dunn.) and Huang Qi (Astragalus membranaceus [Fisch] Bge) have been demonstrated to have remarkable inhibiting effects on the metabolism of CYP3A4, whereas Xi Yi Hua (Magnolia biondii Pamp.) exhibited a moderate inhibition. These five single herbs were further investigated in an animal study using midazolam. Mu Dan Pi, Ji Shiee Terng and Huang Qi were observed to have greatly increased in the Cmax and AUC of midazolam. This study provides evidence of possible herb-drug interactions involved with certain single herbs.
机译：这项研究的目的是评估中草药对人肝微粒体和大鼠中CYP3A4酶活性的影响以及可能基于代谢的中草药之间的相互作用。使用人肝微粒体筛选了50种单草药制剂的CYP3A4活性，用于体外探针反应研究。通过确定在液相色谱-串联质谱法（LC-MS / MS）上确定的从睾丸激素代谢的6β-羟基睾丸激素来评估CYP3A4的酶活性。事实证明，黄Q（Scutellaria baicalensis Geprgi），木丹皮（Paeonia suffruticosa Andr。），吉诗登（Spatholobus suberectus Dunn。）和黄芪（Astragalus membranaceus [Fisch] Bge）具有显着的抑制代谢作用。 CYP3A4，而喜华（木兰生物）表现出中度抑制作用。在使用咪达唑仑的动物研究中进一步研究了这五种单一草药。观察到木丹皮，吉时登和黄琦在咪达唑仑的Cmax和AUC中大大增加。这项研究提供了某些单一草药可能涉及的草药-药物相互作用的证据。

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