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
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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。Abstract: 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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Keywords:
- paclitaxel /
- compound sophora injection /
- CYP450 enzyme /
- drug interaction /
- liver microsomes
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期刊类型引用(5)
1. 秦佳琪，张帆，吕东霞，贺震，魏玉辉. PXR/CAR-代谢酶/转运体解毒系统的功能及研究进展. 中国药物警戒. 2024(06): 709-715 . 
百度学术
2. 施嫣嫣，杭永付，黄玉宇. 注射用紫杉醇(白蛋白结合型)临床应用合理性分析. 中国医院用药评价与分析. 2024(08): 999-1002 . 百度学术
3. 戚姝娅，张玉君，张铭予. 肺癌治疗相关中成药药学服务专家共识(2024). 中国医院用药评价与分析. 2024(10): 1153-1166 . 百度学术
4. 陈伟，王燕婷，王宇，范琳琳，周海燕，杨珺，张建颖. 紫杉类抗肿瘤药物药学服务中国专家共识. 中国医院用药评价与分析. 2022(12): 1409-1427 . 百度学术
5. 张绮悦，杨长青. 食物、中药及其有效成分单体对CYP2C8的抑制作用研究进展. 中国当代医药. 2020(24): 33-36 . 百度学术
其他类型引用(2)
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