Evidence for inhibition of cholinesterases in insect and mammalian nervous systems by the insect repellent deet.
Evidence for inhibition of cholinesterases in insect and mammalian nervous systems by the insect repellent deet.
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DOI：
10.1186/1741-7007-7-47
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发表时间：
2009-08-05
期刊：
影响因子：
5.4
通讯作者：
Lapied B
中科院分区：
文献类型：
--
作者：
Corbel V;Stankiewicz M;Pennetier C;Fournier D;Stojan J;Girard E;Dimitrov M;Molgó J;Hougard JM;Lapied B
N，N-二乙基-3-甲基苄胺（避蚊胺）仍然是驱蚊剂的黄金标准。每年约有2亿人使用它，在过去50年里已经使用了80多亿剂。尽管人们对在公共卫生规划中使用避蚊胺的兴趣越来越大，但在确定避蚊胺在嗅觉系统中的靶点及其对昆虫、哺乳动物和人类的毒性机制方面仍存在争议。在这里，我们研究了deet的分子靶点及其与氨基甲酸酯类杀虫剂相互作用对胆碱能系统的影响。通过使用毒理学、生物化学和电生理技术，我们发现避蚊胺不仅仅是一种行为改变化学物质，而且在昆虫和哺乳动物的神经制剂中也能抑制胆碱酯酶的活性。避蚊胺通常与杀虫剂联合使用，我们发现避蚊胺有能力增强氨基甲酸盐的毒性，氨基甲酸盐是一类已知能阻断乙酰胆碱酯酶的杀虫剂。这些发现对避蚊胺的安全性提出了质疑，特别是与其他化学品结合使用时，它们强调了采用多学科方法开发用于公共卫生的更安全驱蚊剂的重要性。
N,N-Diethyl-3-methylbenzamide (deet) remains the gold standard for insect repellents. About 200 million people use it every year and over 8 billion doses have been applied over the past 50 years. Despite the widespread and increased interest in the use of deet in public health programmes, controversies remain concerning both the identification of its target sites at the olfactory system and its mechanism of toxicity in insects, mammals and humans. Here, we investigated the molecular target site for deet and the consequences of its interactions with carbamate insecticides on the cholinergic system. By using toxicological, biochemical and electrophysiological techniques, we show that deet is not simply a behaviour-modifying chemical but that it also inhibits cholinesterase activity, in both insect and mammalian neuronal preparations. Deet is commonly used in combination with insecticides and we show that deet has the capacity to strengthen the toxicity of carbamates, a class of insecticides known to block acetylcholinesterase. These findings question the safety of deet, particularly in combination with other chemicals, and they highlight the importance of a multidisciplinary approach to the development of safer insect repellents for use in public health.
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影响因子：
7.8
作者：
Feng, G;Krejci, E;Molgo, J;Cunningham, J M;Massoulie, J;Sanes, J R
通讯作者：
Sanes, J R
影响因子：
7.3
作者：
Minic, J;Chatonnet, A;Molgó, J
通讯作者：
Molgó, J
影响因子：
5.8
作者：
ELLMAN, GL;COURTNEY, KD;FEATHERSTONE, RM
通讯作者：
FEATHERSTONE, RM
影响因子：
6.2
作者：
LIPSCOMB, JW;KRAMER, JE;LEIKIN, JB
通讯作者：
LEIKIN, JB
影响因子：
2.6
作者：
Montero-Solis, C;Gonzalez-Ceron, L;de la Cruz Hernandez-Hernandez, F
通讯作者：
de la Cruz Hernandez-Hernandez, F