摘要
目的:综述近年来雷公藤对药物代谢酶及转运体的调控进展。方法:查阅近年来国内外报道中雷公藤对药物代谢酶及转运体调控的文献,并进行归纳总结。结果:雷公藤可以抑制CYP3A4、CYP2C11等多种Ⅰ相代谢酶体外活性。而在体内实验中,大剂量的雷公藤可以强抑制CYP3A、并诱导CYP2C11和CYP2E1的表达。雷公藤对UGT1A6、UGT2B7以及GST也有抑制,但可以诱导Nrf2基因的表达。此外,雷公藤对P-gp和MDR1的基因表达存在抑制作用。结论:雷公藤对多种药物代谢酶和转运体具有抑制或诱导作用,因而雷公藤可能与其他药物发生相互作用。
OBJECTIVE To summarize the recent research progress in the influence of tripterygium on drug metabolizing enzymes and transporter.METHODS The literatures on the regulation of drug metabolizing enzymes and transporters by Tripterygium wilfordii in recent years were reviewed and summarized.RESULTS Tripterygium wilfordii can inhibit the activity of CYP3 A4,CYP2 C11 and other phase I metabolic enzymes in vitro.In vivo,high doses of Tripterygium wilfordii strongly inhibited CYP3 A and induced the expression of CYP2 C11 and CYP2 E1.Tripterygium wilfordii also inhibited UGT1 A6,UGT2 B7 as well as GST,but could induce the expression of Nrf2 gene.In addition,Tripterygium wilfordii has an inhibitory effect on gene expression of P-gp and MDR1.CONCLUSION Tripterygium wilfordii can inhibit or induce many drug metabolizing enzymes and transporters,so Tripterygium wilfordii may interact with other drugs.
作者
周锦屏
张蕊
师少军
刘亚妮
ZHOU Jin-ping;ZHANG Rui;SHI Shao-jun;LIU Ya-ni(Department of pharmacy,Tongji Hospital,Huazhong University of Science and Technology,430022,Wuhan Hubei,China)
出处
《中国医院药学杂志》
CAS
北大核心
2020年第14期1595-1599,共5页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金资助项目(编号:81503161,81874326)
国家重点研发计划资助项目(编号:2017YFC0909900)。
关键词
雷公藤
药物代谢酶
转运体
调控作用
Tripterygium
drug-metabolizing enzymes
transporter
modulation
