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苯并咪唑类药物对秀丽隐杆线虫苯并咪唑抗性和敏感品系微管蛋白的影响。

Effect of benzimidazole drugs on tubulin in benzimidazole resistant and susceptible strains of Caenorhabditis elegans.

作者信息

Enos A, Coles G C

机构信息

Department of Zoology, University of Massachusetts, Amherst 01003.

出版信息

Int J Parasitol. 1990 Apr;20(2):161-7. doi: 10.1016/0020-7519(90)90096-6.

DOI:10.1016/0020-7519(90)90096-6
PMID:2332276
Abstract

An in vitro assay was used to determine efficacy and if side resistance was present to benzimidazole anthelmintics tested against Caenorhabditis elegans after selection with albendazole. Side resistance was present to all the benzimidazoles tested, except for oxibendazole and parbendazole. At a concentration of 1 mM, all of the drugs, except thiabendazole, were effective in killing 100% of the albendazole susceptible worms. Tubulin from albendazole resistant and susceptible C. elegans was isolated and run on polyacrylamide gels. Western blots with anti-tubulin antibody showed that the albendazole resistant strain had an altered tubulin. Electron microscopy of albendazole-treated drug resistant worms showed microtubules throughout the intestinal cells. Microtubules were not observed in albendazole-treated drug susceptible worms.

摘要

采用体外试验来确定对经阿苯达唑筛选后的秀丽隐杆线虫进行测试的苯并咪唑驱虫药的疗效以及是否存在抗药性。除奥芬达唑和巴苯达唑外,对所有测试的苯并咪唑均存在抗药性。在浓度为1 mM时,除噻苯达唑外,所有药物均能有效杀死100%对阿苯达唑敏感的线虫。从对阿苯达唑耐药和敏感的秀丽隐杆线虫中分离出微管蛋白,并在聚丙烯酰胺凝胶上进行电泳。用抗微管蛋白抗体进行的蛋白质免疫印迹显示,对阿苯达唑耐药的品系微管蛋白发生了改变。对经阿苯达唑处理的耐药线虫进行电子显微镜观察,发现整个肠道细胞中都有微管。在经阿苯达唑处理的敏感线虫中未观察到微管。

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Effect of benzimidazole drugs on tubulin in benzimidazole resistant and susceptible strains of Caenorhabditis elegans.苯并咪唑类药物对秀丽隐杆线虫苯并咪唑抗性和敏感品系微管蛋白的影响。
Int J Parasitol. 1990 Apr;20(2):161-7. doi: 10.1016/0020-7519(90)90096-6.
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Interaction of benzimidazole anthelmintics with Haemonchus contortus tubulin: binding affinity and anthelmintic efficacy.苯并咪唑驱虫药与捻转血矛线虫微管蛋白的相互作用:结合亲和力与驱虫效果
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Eur J Biochem. 1987 Mar 16;163(3):449-55. doi: 10.1111/j.1432-1033.1987.tb10890.x.

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