the苯并咪唑氨基甲酸酯类药物抗猪囊尾蚴的作用靶点guidedownload.pdfVIP

中国农业科学 2007,40(5):1024-1032 Scientia Agricultura Sinica 苯并咪唑氨基甲酸酯类药物抗猪囊尾蚴的作用靶点 李庆章，郝艳红，高学军，刘永杰，高文学，赵 冰 （东北农业大学生命科学学院，哈尔滨 150030 ） 摘要：【目的】研究苯并咪唑氨基甲酸酯类抗囊药物对猪带绦虫囊尾蚴的作用靶点，为药物的类型衍化和 新药开发提供理论依据。【方法】测定体外培养的和猪体内的囊尾蚴于阿苯哒唑和奥芬哒唑分别作用后能量代谢 途径物质含量及其关键酶活性变化。【结果】阿苯哒唑和奥芬哒唑对体外培养猪六钩蚴、未成熟期和成熟期猪囊 尾蚴，以及体内发育未成熟期和成熟期猪囊尾蚴的糖无氧分解途径、丙酮酸羧化支路与逆向三羧酸循环途径均 有一定程度抑制作用，代偿性促进糖异生及蛋白质、脂类和核酸分解途径，葡萄糖吸收受阻。阿苯哒唑和奥芬 哒唑体外非竞争性抑制延胡索酸还原酶复合体活性。【结论】并咪唑氨基甲酸酯类抗囊药物非竞争性抑制猪囊尾 蚴FR复合体活性，抑制葡萄糖的摄取。 关键词：阿苯哒唑；奥芬哒唑；猪囊尾蚴；作用靶点；能量代谢 The Target of Benzimidazole Ccarbamate Against Cysticerci cellulosae LI Qing-zhang ，HAO Yan-hong ，GAO Xue-jun ，LIU Yong-jie ，GAO Wen-xue ，ZHAO Bing （College of Biological Science, Northeast Agricultural University, Harbin 150030 ） Abstract: 【Objective 】The objective was to study the target of benzimidazole carbamate drugs against Cysticerci cellulosae and give theoretical basis for type evolution and new drug design. 【Method 】Changes of key enzyme activities and metabolite contents in pathway of energy metabolism in Cysticerci cellulosae in vitro and in vivo were tested with albendazole and oxfendazole respectively. 【Results 】Albendazole and oxfendazole both inhibited the pathways of anaerobic glycolysis, partial inversed tricarboxylic acid cycle of Taenia Solium oncosphere, immature and mature cysticerci in vitro and immature and mature cysticerci in vivo in certain degree. They enhanced decomposing in fat, amino acid, and xanthine metabolism. On the other hand, absorption of glucose was hindered. Albendazole and oxfendazole both inhibited the activities of fumaric reductase complex noncompetently in vito respectively. 【Conclusion 】Benzimidazole carbamate drugs can inhibit the activities of fumaric reductase complex no