穿破石对人肝微粒体CYP450酶的抑制活性研究  

Research on inhibitory activity of radix cudramiae on humanliver microsome CYP450 enzyme

作　　者：陈诗卉 梁现蕊[1] CHEN Shihui;LIANG Xianrui(College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《发酵科技通讯》2020年第3期135-141,共7页Bulletin of Fermentation Science and Technology

摘　　要：研究穿破石对人肝微粒体CYP450酶的抑制活性。将穿破石提取液与混合探针药物共同孵育,各探针药物的峰面积由超高效液相色谱进行测定,并与阳性抑制剂进行对照。穿破石提取液对CYP1A2,CYP3A4,CYP2C9和CYP2E1的IC 50值分别为0.3561,0.3324,0.4049,0.8615 mg/mL。对人肝微粒体CYP450酶的4种亚型酶来说,穿破石提取液对CYP3A4亚型酶的抑制程度最大,对CYP2E1的抑制程度最小,与阳性抑制剂对比,穿破石提取液总体抑制活性较弱。The inhibitory activities of Radix Cudramiae on human liver microsome CYP450 enzyme were investigated.The Radix Cudramiae extraction was incubated with the mixed probe drugs.The peak areas of each probe substrate drug were detected by UPLC and compared with the positive inhibitors.The IC 50 values of Radix Cudramiae extraction for CYP1A2,CYP3A4,CYP2C9 and CYP2E1 were 0.3561,0.3324,0.4049,0.8615 mg/mL,respectively.The Radix Cudramiae extraction has the largest inhibition effects on CYP3A4 subtype enzymes and the smallest inhibition effects on CYP2E1.Compared with the positive inhibitors,the Radix Cudramiae extraction exhibited weak inhibitory activity on these four subtype enzymes.

关 键 词：穿破石 人肝微粒体 CYP450酶 抑制 UPLC 

分 类 号：R285.5[医药卫生—中药学]