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(IC_(50))。结果复方苦参注射液在0.600g/mL时对CYP2C8的抑制率为100.0%,其IC50值为0.052 8g/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。
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 concentra- tions of compound sophora injection （v/v） were co-incubated with human liver microsomes and the substrates of CYP2C8 （pa- clitaxel）. After the co-incubation, 6a-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 in- jection 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.
出处
《南京中医药大学学报》
CAS
CSCD
北大核心
2018年第1期87-90,共4页
Journal of Nanjing University of Traditional Chinese Medicine
基金
江苏省药学会医院药学基金(201409)
