三叶 五叶木通提取物药效及对药酶影响的比较研究

A Comparative Study on Pharmacodynamic Action of Akebia Trifoliata(Thunb.) Koidz and Akebia Quinata(Thunb)Decne and Effect on Drug Metabol Izing-enzymes

目的:比较三叶木通[Akebia trifolia ta(Thunb.)Koidz,简称AK]和五叶木通[Akebia quina ta(Thunb)Decne,简称AD]水提物抗炎、利尿及抗菌作用的同时,探索性观察了两种木通对细胞色素P4503A(CYP3A)活性和P-糖蛋白(P-gp)水平的影响。方法:抗炎作用采用小鼠腹腔毛细血管通透法和小鼠耳肿胀法,观察其抗炎作用;利尿作用采用大鼠代谢笼法,观察其利尿作用;采用体外抑菌实验,观察其抑菌作用。用聚乙二醇制备肝微粒体,测定肝和小肠CYP3A活性;以免疫组化法检测肝和小肠组织P-gp水平。结果:两种木通均明显抑制小鼠腹腔毛细血管炎性渗出,抑制二甲苯所致小鼠耳廓肿胀;并利尿和抑菌作用明显;三叶木通对肝脏CYP3A活性和P-gp水平有一定的抑制作用。与正常对照组相比差异显著(P<0.05);五叶木通对肝脏CYP3A活性和P-gp水平无明显作用,与正常对照组相比无统计学意义(P>0.05)。结论:两种木通抗炎、利尿及抑菌作用基本相等;三叶木通水提物可能是肝CYP3A和P-gp的抑制剂;但五叶木通对CYP3A和P-gp影响不明显。

Objective ： To compare the anti -inflammatory, diuretic and bacteriostatic action between Akebia trifoliata （Thunb.） Koidz and Akebia quinata （Thunb）Decne aqueous, extract, and to observe the influence of Akebiatrifoliata （Thunb.） Koidz and Akebia quinata （Thunb） Decne on the content of P -glycoprotein and activity of cytochrome P4503A. Methods ： the anti - inflammatory action was assessed by HAc - induced abdominal cavity capillary permeability and xylene - induced ear edema in mice. The diuretic effect was verified by metabolic cage of rats. The bacteriostatic action was monitored by bacteriostasis experiment in vitro. The liver and small intestine microsomes were prepared with polyethylene glycol and the activities of CYP450 3A in the microsomes were determined by the substrate of erythromycin and the content of P - glycoprotein in liver and small intestine tissue by SP staining methods of Immunohistochemistry. Results ： both Akebia trifoliata （Thunb.）Koidz and Akebia quinata （Thunb）Decne reduce the capillary permeability of abdominal cavity, inhibit xylene - induced ear edema in mice significantly, and show obvious diuretic, bacteriostatic action. Compared with normal control group, Akebia trifoliata （ Thunb. ） Koidz inhibit the activities of CYP450 3A and reduce the level of P-gp in liver significantly,and Akebia quinata （Thunb）Decne is not statistically significant. Conclusion ： the anti- inflammatory, diuretic and bacteriostatic action between Akebia trifoliata （Thunb.）Koidz and Akebia quinata （Thunb） Decne are equal,the aqueous extract ofAkebia trifoliata （Thunb.）Koidz might be the inhibitor of CYP450 3A and P- gp. Akebia quinata （Thunb）Decne shows no obvious influence on CYP450 3A and P- gp.