Mosquitocidal carbamates with low toxicity to agricultural pests: an advantageous property for insecticide resistance management.
Mosquitocidal carbamates with low toxicity to agricultural pests: an advantageous property for insecticide resistance management.
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DOI：
10.1002/ps.3899
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发表时间：
2015-08
影响因子：
4.1
通讯作者：
Bloomquist, Jeffrey R.
中科院分区：
文献类型：
--
作者：
Swale, Daniel R.;Carlier, Paul R.;Hartsel, Joshua A.;Ma, Ming;Bloomquist, Jeffrey R.
冈比亚按蚊对杀虫剂的抗药性是有充分证据的，当拟除虫菊酯用于媒介控制时，拟除虫菊酯在农业上的广泛使用可能会加剧耐药性的发展。我们已经开发出具有高度AN的氨基甲酸酯抗胆碱酯酶。冈比亚：人类对酶抑制的选择性。这项研究的目的是评估这些氨基甲酸酯类化合物对其他蚊子和农业害虫的活性。实验中的氨基甲酸酯是蚊子乙酰胆碱酯酶的有效抑制剂，其IC50值在纳摩尔范围内。家蝇和果蝇的酶活性也有类似的变化。2种邻位取代氨基甲酸酯对蜜蜂、亚洲柑橘木虱和鳞翅目农业害虫小菜蛾和玉米象的抑制作用较差(IC50≥10−6 M)。酶抑制结果得到了对毛虫的毒性研究的证实，其中新的氨基甲酸酯的毒性比残杀威低2-3倍，活性比苯敌畏低10倍，表明这些化合物在作物保护方面几乎没有用。实验中的氨基甲酸酯对蚊子物种有广泛的活性，但对农业害虫没有作用，这应该会通过减少这些化合物的农业使用来减少对蚊子杀虫剂抗性的选择。
Insecticide resistance in the malaria mosquito, Anopheles gambiae, is well documented and widespread agricultural use of pyrethroids may exacerbate development of resistance when pyrethroids are used in vector control. We have developed carbamate anticholinesterases that possess a high degree of An. gambiae: human selectivity for enzyme inhibition. The purpose of this study was to assess the spectrum of activity of these carbamates against other mosquitoes and agricultural pests. Experimental carbamates were potent inhibitors of mosquito acetylcholinesterases, with IC50 values in the nanomolar range. Similar potencies were observed for Musca domestica and Drosophila melanogaster enzymes. Although meta-substituted carbamates were potent inhibitors, two ortho-substituted carbamates displayed poor enzyme inhibition (IC50 ≥ 10−6 M) in honey bee (Apis mellifera), Asian citrus psyllid (Diaphorina citri), and lepidopteran agricultural pests (Plutella xylostella and Ostrinia nubilalis). Enzyme inhibition results were confirmed by toxicity studies in caterpillars, where the new carbamates were 2- to 3-fold less toxic than propoxur and up to 10-fold less active than bendiocarb, indicating little utility of these compounds for crop protection. The experimental carbamates were broadly active against mosquito species but not agricultural pests, which should mitigate selection for mosquito insecticide resistance by reducing agricultural uses of these compounds.
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影响因子：
5.8
作者：
ELLMAN, GL;COURTNEY, KD;FEATHERSTONE, RM
通讯作者：
FEATHERSTONE, RM
影响因子：
2.2
作者：
Chauzat, MP;Faucon, JP;Aubert, M
通讯作者：
Aubert, M
影响因子：
2.7
作者：
Hartsel, Joshua A.;Wong, Dawn M.;Mutunga, James M.;Ma, Ming;Anderson, Troy D.;Wysinski, Ania;Islam, Rafique;Wong, Eric A.;Paulson, Sally L.;Li, Jianyong;Lam, Polo C. H.;Totrov, Maxim M.;Bloomquist, Jeffrey R.;Carlier, Paul R.
通讯作者：
Carlier, Paul R.
影响因子：
56.9
作者：
Henry, Mickael;Beguin, Maxime;Decourtye, Axel
通讯作者：
Decourtye, Axel
影响因子：
2.2
作者：
Abbott, WS
通讯作者：
Abbott, WS