摘要
目的研究半枝莲水相和乙醇相提取物对人细胞色素P450主要酶活性的影响,为半枝莲的开发和合理地临床应用提供参考。方法以咪哒唑仑、甲苯磺丁脲、咖啡因、氯唑沙完、异喹呱和试卤灵为探针药,用高效液相色谱法分别测定不同提取溶质的半枝莲粗提物对人细胞色素P450主要酶活性的影响。结果①半枝莲粗提物对CYP3A4、CYP2C9、CYP1A2、CYP1A1酶的活性呈现出剂量依赖性抑制作用。②半枝莲水相粗提物比乙醇相粗提物对CYP1A1和CYP1A2酶的体外抑制作用强。结论半枝莲水相提取物和乙醇相提取物是CYP3A4、CYP2C9、CYP1A2、CYP1A1体外抑制剂。
Objective To investigate the effect of water and ethanol extracts of Scutellarla barbata D. Don on the activities of cytochrome P450 in human Liver microsomes. Methods Midazolam, EOR, caffeine, tolbutamide, chlorzoxazone, and debrisoquine were incubated as probes with or without Scutellariae barbatae respectively to determine the effect of water extract and ethanol extract of Scutellaria barbara on cytochrome P450 activities including CYP3A4, CYP1A1, CYP1A2, CYP2C9, CYP2E1, and CYP2D6 in human liver microsomes. Results ① Both water and etha nol extracts of Scutellarla barbata D. Don inhibited the activities of CYPs （CYP3A4, CYP2C9, CYP1A2, and CYP1A1） in a concentration-dependent manner. ② Significant differences between the water and ethanol extracts of Scutellarla barbara D. Don were observed in CYP1A2 and CYP1A2. The water extract had stronger potential ability to inhibit the activities of the two enzymes than the enthanol extract in human liver microsomes in vitro. Conclusion Wa ter extract and ethanol extracts of Scutellarla barbata D. Don have the potential ability to inhibit the activities of drug metabolism enzymes in human liver microsomes in vitro, including CYP1A1, CYP1A2, CYP2C9, and CYP3A4.
出处
《中南药学》
CAS
2008年第1期53-55,共3页
Central South Pharmacy
