The Target of Benzimidazole Carbamate Against Cysticerci cellulosae

To study the target of benzimidazole carbamate drugs against Cysticerci cellulosae and give a theoretical basis for type evolution and new drug design, the changes of key enzyme activities and metabolite contents in the pathway of energy metabolism in C. cellulosae in vitro and in vivo were tested with albendazole and oxfendazole, respectively. Both albendazole and oxfendazole 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 to a certain degree, and enhanced fat decomposing, amino acid decomposing, xanthine decomposing metabolism, and on the other hand, the absorption of glucose was hindered; furthermore, both albendazole and oxfendazole inhibited the activities of the fumaric reductase （FR） complex noncompetently in vitro. Benzimidazole carbamate drugs could inhibit the activities of FR complex noncompetently and hinder the absorption of glucose.

苯并咪唑氨基甲酸酯类药物抗猪囊尾蚴的作用靶点

【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。

阿苯达唑和奥芬达唑对体外培养猪囊尾蚴能量代谢变化的影响

测定了在阿苯达唑和奥芬达唑作用下体外培养猪囊尾蚴磷酸烯醇式丙酮酸羧激酶(PEPCK)、丙酮酸激酶(PK)、延胡索酸还原酶(FR)、苹果酸酶(ME)活性的变化及葡萄糖(GLC)、乳酸(LAC)含量的变化。结果表明,2种药物作用均可在体外作用条件下显著改变未成熟期及成熟期猪囊尾蚴的能量代谢。提示,苯并咪唑氨基甲酸酯类药物的作用机理可能是通过干扰虫体能量代谢,阻断能量的产生,导致虫体死亡。