Inhibition of cytochrome P450 by furanocoumarins in grapefruit juice and herbal medicines  

作　　者：Lian-qingGUO YasushiYAMAZOE 

机构地区：[1]DepartmentofClinicalPharmacology,JinlingHospital,Nanjing210002 [2]DivisionofDrugMetabolismandMolecularToxicology,GraduateSchoolofPharmaceuticalSciences,TohokuUniversity,Sendai980-8578,Japan

出　　处：《Acta Pharmacologica Sinica》2004年第2期129-136,共8页中国药理学报（英文版）

摘　　要：Furanocoumarins (psoralens) exist in various plants and some of them are used to cure skin diseases. Thesechemicals draw attentions recently because of their abilities to arouse drug interaction through inhibition of cyto-chrome P450. Grapefruit juice is a well-known example for food-drug interaction. But in vitro and in vivo studieshave shown that the causative components are mainly furanocoumarin derivatives with geranyloxy side chains. Invitro 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 furanocoumarinsand related citrus fruits or umbelliferous herbal medicines indicate that drug interaction might also occur with stuffsother than grapefruit juice, especially with traditional medicine.Furanocoumarins (psoralens) exist in various plants and some of them are used to cure skin diseases. Thesechemicals draw attentions recently because of their abilities to arouse drug interaction through inhibition of cyto-chrome P450. Grapefruit juice is a well-known example for food-drug interaction. But in vitro and in vivo studieshave shown that the causative components are mainly furanocoumarin derivatives with geranyloxy side chains. Invitro 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 furanocoumarinsand related citrus fruits or umbelliferous herbal medicines indicate that drug interaction might also occur with stuffsother than grapefruit juice, especially with traditional medicine.

关 键 词：PSORALENS grapefruit juice herbal medicine enzyme inhibitors cytochrome P-450 enzyme system drug interaction 

分 类 号：R282.71[医药卫生—中药学]