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苯并咪唑氨基甲酸盐对哺乳动物微管蛋白聚合的抑制作用与杀蠕虫卵活性的比较。

Comparison of inhibition of polymerisation of mammalian tubulin and helminth ovicidal activity by benzimidazole carbamates.

作者信息

Lacey E, Brady R L, Prichard R K, Watson T R

出版信息

Vet Parasitol. 1987 Jan;23(1-2):105-19. doi: 10.1016/0304-4017(87)90029-x.

DOI:10.1016/0304-4017(87)90029-x
PMID:3564338
Abstract

The correlation between the inhibition of hatching of Haemonchus contortus eggs and inhibition of mammalian tubulin polymerisation by benzimidazole carbamates has been investigated. The hatching process was observed to be independent of the biomass (eggs plus debris) over a 6-fold range and the early (E1-E3) stages of egg development, but was dependent on the concentration of co-solvent (DMSO) and time of incubation. Benzimidazole carbamates with strong inhibitory activity against mammalian tubulin were potent inhibitors of egg hatch, while non-inhibitors failed to prevent hatching. It is postulated that the primary mode of action of these drugs on nematode eggs is the inhibition of microtubule-dependent processes within the developing egg. The implications and limitations of this correlation are discussed.

摘要

研究了苯并咪唑氨基甲酸盐对捻转血矛线虫虫卵孵化的抑制作用与对哺乳动物微管蛋白聚合的抑制作用之间的相关性。观察到在6倍的生物量(虫卵加碎片)范围内以及虫卵发育的早期(E1 - E3)阶段,孵化过程与生物量无关,但依赖于助溶剂(二甲基亚砜)的浓度和孵育时间。对哺乳动物微管蛋白具有强抑制活性的苯并咪唑氨基甲酸盐是虫卵孵化的有效抑制剂,而非抑制剂则不能阻止孵化。据推测,这些药物对线虫虫卵的主要作用方式是抑制发育中虫卵内依赖微管的过程。讨论了这种相关性的意义和局限性。

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