摘要
目的:研究三七总皂苷(total saponins of the root and rhizome of Panax notoginseng,PNS)对大鼠肝组织内药物代谢酶CYP3A的抑制作用及其动力学分析。方法:采用差速离心法制备大鼠微粒体酶,用半数效量概率单位法及Lineweaver-Burk双倒数作图法求得大鼠肝脏CYP3A的米氏常数(Km)、最大反应速度(Vmax)和三七总皂苷对大鼠肝脏CYP3A的半数抑制浓度(IC50)以及判断三七总皂苷对CYP3A的抑制类型和抑制常数(Ki,Kis)。结果:三七总皂苷对大鼠肝组织CYP3A有抑制作用,其IC50689.54 mg·L-1;对底物氨基比林,CYP3A的Km0.036 mmol·L-1,Vmax是21.01μmol·min-1·g-1;三七总皂苷对大鼠肝组织CYP3A属于混合性抑制,其抑制常数Ki247.79 mg·L-1,Kis321.79 mg·L-1。结论:三七总皂苷对大鼠肝脏CYP3A的活性有明显抑制作用。
Objective： To study the inhibitory effect of total saponins of the root and rhizome of Panax notoginseng （PNS） on drug metabolism enzyme CYP3A in rat livers and its kinetic analysis. Method： Microsome enzyme was prepared by differential velocity centrifugation. Michaelis constant （ Km ） and maximum velocity （ Vmax ） of CYP3A, 50% inhibitory cnncentratinn of PNS on CYP3A, and the inhibitinn type and the inhibition constant of CYP3A （Ki, Kin ） of PNS on CYP3A were calculated by Lineweaver-Burk and the low of semi-effect-probit. Result： Total saponins of the root and rhizome of panax notoginseng inhibited CYP3A activity, with IC50 of 689. 54 mg· L^-1. Compared with the substrate aminopyrine, CYP3A showed Km of 0. 036 mmol· L^-1 and Vmax of 21. 01 μmol · min^-1 · g^-1 Total saponins of the root and rhizome of panax notoginseng showed a mixed inhibition on CYP3A, with the inhibition constants of 247. 79 mg · L^-1 （ Km ） and 321.79 mg· L^-1 （ Km ）. Conclusion ： Total saponins of the root and rhizome of panax notoginseng have a significant effect on CYP3A activity in rat livers.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2012年第22期3486-3489,共4页
China Journal of Chinese Materia Medica
基金
教育部新世纪优秀人才支持计划项目(教技函2010-14号NCET-10-0093)
广西自然科学基金项目(桂科基0731058
2011GXNSFF018006)
