【摘要】 洛克沙胂是一种常用的饲料添加药物,细胞色素P450酶系(CYP或P450)是动物体内药物代谢的主要酶类。本文研究了洛克沙胂对猪肝微粒体P450酶系中的2种酶CYP3A4和CYP2E1的蛋白表达的影响,为揭示该药的代谢机理、残留机制以及临床安全用药提供理论依据。实验将洛克沙胂以5、25和125mmol/L 3个剂量,分别添加到猪肝微粒体体外孵育体系中,以生理盐水作对照,于37℃孵育1h,测定微粒体蛋白含量及CYP3A4及2E1的蛋白表达。结果表明中剂量和高剂量的洛克沙胂对猪肝细胞微粒体的CYP3A4及2E1的蛋白表达均呈现抑制作用,而低剂量的洛克沙胂对CYP3A4和CYP2E1的蛋白表达影响很小。更多还原

【Abstract】 Roxarsone is widely used as a feed additive in animal production.Cytochrome P450(CYP,P450)is the main enzymatic family that metabolize the drugs.The objective of this paper was to investigate the effects of roxarsone on the expression of CYP3A4 and 2E1in swine liver hepatic microsome,and thus to provide the theory basis for revealing the mechanism of metabolism,residue generation and clinical safe usage of roxarsone.Roxarsone was added into in vitro incubation system of swine liver hepatic microsome with the doses of 5,25 and 125mmol/L respectively.The control was added with physiological saline.Then the reaction systems were incubated at 37 ℃for 1hour.Western blotting was used to measure the protein expression.The results showed that all middle and high dose of roxarsone could inhibit the expression of CYP3A4 and CYP2E1in swine liver hepatic microsome,but the low dose has a little effect on them.更多还原