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目的 初步了解阿苯哒唑 (albendazole,ABZ)及其主要代谢物亚砜 (albendazole- sulfoxide,ABZSX)和砜(albendazole- sulfone,ABZSN)对猪蛔虫的作用机制。方法 应用紫外分光光度计扫描系统对猪蛔虫肌肉线粒体中四种酶复合体 (com plex - NADH细胞色素 C脱氢酶 ;complex —琥珀酸 Co Q脱氢酶 ;complex — Co Q细胞色素还原酶 ;complexIV—细胞色素 C氧化酶 )活性进行测定 ,以鼠肝线粒体作对照 ,再经 ABZ及其代谢物 ABZSX,ABZSN作用后观察其活性改变。结果 ABZ及其代谢物 ABZSX对猪蛔虫肌肉线粒体中琥珀酸脱氢酶 (complex )的活性有明显的抑制作用 ,而对鼠肝线粒体中四种酶复合体均无明显抑制作用。结论 ABZ及其代谢物主要抑制了蛔虫肌肉线粒体中琥珀酸脱氢酶的活性 ,使其不能完成呼吸链的氧化磷酸化过程 ,从而达到杀虫效果。
Objective To study the mechanism of albendazole (ABZ) and its major metabolites albendazole-sulfoxide (ABZSX) and albendazole-sulfone (ABZSN) on Ascaris suum. Methods The UV - Vis spectrophotometer system was used to detect the activity of four complex enzymes (com plex - NADH cytochrome C dehydrogenase, complex - Co Q dehydrogenase and complex - Co Q cytochrome reductase) complexIV-cytochrome C oxidase) activity was measured to mitochondrial rat liver as a control, and then by the ABZ and its metabolites ABZSX, ABZSN role after the change was observed. Results ABZ and its metabolite ABZSX significantly inhibited the activity of succinate dehydrogenase in the muscle mitochondria of Ascaris suum but had no obvious inhibitory effect on the four enzyme complexes in rat liver mitochondria. Conclusion ABZ and its metabolites mainly inhibit the activity of succinate dehydrogenase in roundworm muscle mitochondria, which can not complete the process of oxidative phosphorylation of respiratory chain, so as to achieve the insecticidal effect.