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单萜类化合物的抗胆碱酯酶和杀虱活性。

Anticholinesterase and pediculicidal activities of monoterpenoids.

作者信息

Picollo M I, Toloza A C, Mougabure Cueto G, Zygadlo J, Zerba E

机构信息

Centro de Investigaciones de Plagas e Insecticidas (CITEFA-CONICET), Juan Bautista de La Salle 4397, (B1603ALO), Villa Martelli, Provincia de Buenos Aires, Argentina.

出版信息

Fitoterapia. 2008 Jun;79(4):271-8. doi: 10.1016/j.fitote.2008.01.005. Epub 2008 Feb 9.

Abstract

The repetitive and inadequate application of pediculicidal products frequently results in the development of resistance to these compounds. Essential oils are a promising alternative to synthetic insecticides, although their mode of action remains to be explored. It has been proposed that one possible target of the essential oils is the inhibition of acetylcholinesterase (AChE). The role of monoterpenoids as possible AChE inhibitors and their relationship with the toxicity was investigated both in vitro and in vivo. Inhibition of electric eel AChE activity showed that the most effective inhibitor was 1,8-cineole with IC(50) 6 x 10(-3) M. The inhibition of AChE activity of head louse homogenate by 1,8-cineole showed IC(50) 7.7 x 10(-2) M. The intoxication symptoms of head lice exposed to vapors of 1,8-cineole was recorded before the in vivo head louse AChE inhibition assay. No correlation was found between neurotoxic symptoms and inhibition of AChE activity.

摘要

灭虱产品的反复和不当使用常常导致对这些化合物产生抗性。精油是合成杀虫剂的一种有前景的替代品,尽管其作用方式仍有待探索。有人提出精油的一个可能靶点是抑制乙酰胆碱酯酶(AChE)。在体外和体内研究了单萜类化合物作为可能的AChE抑制剂的作用及其与毒性的关系。对电鳗AChE活性的抑制表明,最有效的抑制剂是1,8 - 桉叶素,其IC(50)为6×10(-3) M。1,8 - 桉叶素对人头虱匀浆AChE活性的抑制显示IC(50)为7.7×10(-2) M。在体内人头虱AChE抑制试验之前,记录了暴露于1,8 - 桉叶素蒸汽中的人头虱的中毒症状。未发现神经毒性症状与AChE活性抑制之间存在相关性。

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