Guo Lian-qing, Yamazoe Yasushi
Department of Clinical Pharmacology, Jinling Hospital, Nanjing 210002, China.
Acta Pharmacol Sin. 2004 Feb;25(2):129-36.
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.
呋喃香豆素（补骨脂素）存在于多种植物中，其中一些被用于治疗皮肤病。这些化学物质近来引起了关注，因为它们能够通过抑制细胞色素P450引发药物相互作用。葡萄柚汁是食物与药物相互作用的一个著名例子。但体外和体内研究表明，致病成分主要是带有香叶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的竞争性和基于机制的抑制剂。虽然二聚体中的抑制作用似乎比单体中的更强，但所有这些都对葡萄柚汁与药物的相互作用有综合影响。对其他呋喃香豆素以及相关柑橘类水果或伞形科草药的进一步实验表明，除葡萄柚汁外，其他物质尤其是传统药物也可能发生药物相互作用。
