Rinkevich Frank D, Du Yuzhe, Tolinski Josh, Ueda Atsushi, Wu Chun-Fang, Zhorov Boris S, Dong Ke
Department of Entomology, Michigan State University, East Lansing, MI 48824, United States.
Department of Biology, University of Iowa, Iowa City, IA 52242, United States.
Neurotoxicology. 2015 Mar;47:99-106. doi: 10.1016/j.neuro.2015.02.001. Epub 2015 Feb 14.
Voltage-gated sodium channels (Nav channels) are critical for electrical signaling in the nervous system and are the primary targets of the insecticides DDT and pyrethroids. In Drosophila melanogaster, besides the canonical Nav channel, Para (also called DmNav), there is a sodium channel-like cation channel called DSC1 (Drosophila sodium channel 1). Temperature-sensitive paralytic mutations in DmNav (para(ts)) confer resistance to DDT and pyrethroids, whereas DSC1 knockout flies exhibit enhanced sensitivity to pyrethroids. To further define the roles and interaction of DmNav and DSC1 channels in DDT and pyrethroid neurotoxicology, we generated a DmNav/DSC1 double mutant line by introducing a para(ts1) allele (carrying the I265N mutation) into a DSC1 knockout line. We confirmed that the I265N mutation reduced the sensitivity to two pyrethroids, permethrin and deltamethrin of a DmNav variant expressed in Xenopus oocytes. Computer modeling predicts that the I265N mutation confers pyrethroid resistance by allosterically altering the second pyrethroid receptor site on the DmNav channel. Furthermore, we found that I265N-mediated pyrethroid resistance in para(ts1) mutant flies was almost completely abolished in para(ts1);DSC1(-/-) double mutant flies. Unexpectedly, however, the DSC1 knockout flies were less sensitive to DDT, compared to the control flies (w(1118A)), and the para(ts1);DSC1(-/-) double mutant flies were even more resistant to DDT compared to the DSC1 knockout or para(ts1) mutant. Our findings revealed distinct roles of the DmNav and DSC1 channels in the neurotoxicology of DDT vs. pyrethroids and implicate the exciting possibility of using DSC1 channel blockers or modifiers in the management of pyrethroid resistance.
电压门控钠通道(Nav通道)对神经系统的电信号传导至关重要,并且是杀虫剂滴滴涕(DDT)和拟除虫菊酯的主要作用靶点。在黑腹果蝇中,除了典型的Nav通道Para(也称为DmNav)外,还有一种名为DSC1(果蝇钠通道1)的钠通道样阳离子通道。DmNav(para(ts))中的温度敏感麻痹突变赋予对DDT和拟除虫菊酯的抗性,而DSC1基因敲除果蝇对拟除虫菊酯表现出增强的敏感性。为了进一步确定DmNav和DSC1通道在DDT和拟除虫菊酯神经毒理学中的作用及相互作用,我们通过将一个para(ts1)等位基因(携带I265N突变)引入DSC1基因敲除品系中,构建了一个DmNav/DSC1双突变品系。我们证实I265N突变降低了非洲爪蟾卵母细胞中表达的DmNav变体对两种拟除虫菊酯氯菊酯和溴氰菊酯的敏感性。计算机建模预测I265N突变通过变构改变DmNav通道上的第二个拟除虫菊酯受体位点赋予拟除虫菊酯抗性。此外,我们发现para(ts1)突变果蝇中由I265N介导的拟除虫菊酯抗性在para(ts1);DSC1(-/-)双突变果蝇中几乎完全消除。然而,出乎意料的是,与对照果蝇(w(1118A))相比,DSC1基因敲除果蝇对DDT的敏感性较低,并且与DSC1基因敲除或para(ts1)突变体相比,para(ts1);DSC1(-/-)双突变果蝇对DDT的抗性更强。我们的研究结果揭示了DmNav和DSC1通道在DDT与拟除虫菊酯神经毒理学中的不同作用,并暗示了使用DSC1通道阻滞剂或调节剂来管理拟除虫菊酯抗性的令人兴奋的可能性。