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Inhibition of cytochrome P450 by furanocoumarins in grapefruit juice and herbal medicines.
Acta Pharmacologica Sinica ( IF 8.2 ) Pub Date : 2004-02-11
Lian-qing Guo 1 , Yasushi Yamazoe
Affiliation  

Furanocoumarins (psoralens) exist in various plants and some of them are used to cure skin diseases. These chemicals draw attentions recently because of their abilities to arouse drug interaction through inhibition of cytochrome P450. Grapefruit juice is a well-known example for food-drug interaction. But in vitro and in vivo studies have shown that the causative components are mainly furanocoumarin derivatives with geranyloxy side chains. In vitro experiments confirmed that furanocoumarins from grapefruit juice are both competitive and mechanism-based inhibitors of CYP3A4. Although the inhibition appeared to be stronger in the dimers than that in the monomers, all contribute comprehensively to the grapefruit juice-drug interaction. Further experiments with other furanocoumarins and related citrus fruits or umbelliferous herbal medicines indicate that drug interaction might also occur with stuffs other than grapefruit juice, especially with traditional medicine.

中文翻译:

呋喃香豆素对葡萄柚汁和草药中细胞色素P450的抑制作用。

呋喃香豆素(补骨脂素)存在于多种植物中,其中一些可用于治疗皮肤疾病。这些化学物质由于能够通过抑制细胞色素P450引起药物相互作用而受到关注。葡萄柚汁是食品与药物相互作用的一个著名例子。但是体外和体内研究表明,致病成分主要是带有香叶酰氧基侧链的呋喃香豆素衍生物。体外实验证实葡萄柚汁中的呋喃香豆素是CYP3A4的竞争性抑制剂和基于机理的抑制剂。尽管二聚体中的抑制作用似乎比单体中的抑制作用更强,但所有这些作用都对葡萄柚汁与药物的相互作用做出了全面的贡献。
更新日期:2019-11-01
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