基于CYP450酶的复方苦参注射液代谢及其与紫杉醇相互作用的研究

蔡小军1; 陈艳2; 贺晴1; 陆一1; 张秀红1; 黄凯1; 温浩1*

文章摘要

蔡小军1，陈艳2，贺晴1，陆一1，张秀红1，黄凯1，温浩1*.基于CYP450酶的复方苦参注射液代谢及其与紫杉醇相互作用的研究[J].南京中医药大学学报(社会科学版),2018,34(1):87-90.

基于CYP450酶的复方苦参注射液代谢及其与紫杉醇相互作用的研究

Research on Metabolism of Compound Sophora and Its Interaction with Paclitaxel Based on Cytochrome P450s

DOI：

中文关键词: 紫杉醇复方苦参注射液 CYP450酶药物相互作用肝微粒体

英文关键词: paclitaxel compound sophora injection CYP450 enzyme drug interaction liver microsomes

基金项目:

作者	单位
蔡小军1，陈艳2，贺晴1，陆一1，张秀红1，黄凯1，温浩1*	1.南京医科大学附属无锡市人民医院，江苏无锡 214023；2.无锡卫生高等职业技术学校药学系，江苏无锡 214028

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中文摘要:

目的基于细胞色素P450酶（CYP450s）的代谢，考察复方苦参注射液体外与紫杉醇的相互作用，为临床应用提供参考。方法将不同体积百分比浓度的复方苦参注射液与CYP2C8同工酶的探针底物紫杉醇及人肝微粒体共同孵育，采用LC-MS/MS检测特异性探针底物代谢物6α-羟基紫杉醇的生成量，计算半数抑制浓度（IC₅₀)。结果复方苦参注射液在0.600 g/mL时对CYP2C8的抑制率为100.0%，其IC₅₀值为0.052 8 g/mL。结论复方苦参注射液在体外与紫杉醇注射液之间存在基于CYP2C8的代谢性相互作用，为临床应用两药抗肿瘤提供了参考。

英文摘要:

OBJECTIVE To evaluate the metabolism of compound sophora injection based on cytochrome P450s enzyme and its interaction with paclitaxel in vitro in order to provide references for clinical application. METHODS Different concentrations of compound sophora injection (v/v) were co-incubated with human liver microsomes and the substrates of CYP2C8 （paclitaxel）. After the co-incubation， 6α-OH-paclitaxel as the specific substrate metabolite was analyzed by LC-MS/MS assay and then the half maximal inhibitory concentration (IC₅₀) was calculated. RESULTS The inhibition rate of compound sophora injection on CYP2C8 was 100.0% at 0.600 g/mL and its IC₅₀ value was 0.052 8 g/mL. CONCLUSION Drug-drug interaction induced by the inhibition of CYP450 enzymes exists between compound sophora injection and paclitaxel in vitro， which can provide reference for the clinical application of these two drugs in cancer therapy.

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