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杀虫植物苦皮藤Celastrus angulatus的主要活性成分苦皮藤素Ⅳ和Ⅴ处理后昆虫的中毒症状分别表现为麻醉和兴奋,但苦皮藤素Ⅳ对苦皮藤素Ⅴ的毒杀效果具有增效作用,苦皮藤素Ⅴ对苦皮藤素Ⅳ的麻醉作用基本没有影响。应用全细胞膜片钳技术,就苦皮藤素Ⅳ和Ⅴ不同比例(3∶1,1∶1,1∶3)混合物对棉铃虫Helicoverpa armigera幼虫离体培养神经细胞钠离子通道的影响进行了比较。结果表明:苦皮藤素Ⅳ和苦皮藤素Ⅴ的不同比例混合物对钠通道(TTX-S)电流作用与二者所占比例有关,苦皮藤素Ⅳ比例大,表现出苦皮藤素Ⅳ对通道的阻滞效应,钠电流被抑制;苦皮藤素Ⅴ比例大,则表现出对通道的激活,钠电流增大。另外,两者不同比例混合物对钠通道(TTX-S)电流的激活电压无明显影响,但对峰值电压影响显著,可使其向正电位方向移动10~20mV。这些结果说明苦皮藤素Ⅳ和Ⅴ可能作用于一个相同的钠通道结合位点或别构偶联位点,二者对钠通道的作用是一种拮抗作用。
The insecticidal plants celastrus angulatus Celastrus angulatus main active ingredient celangulin Ⅳ and Ⅴ treatment of insects poisoning symptoms were shown as anesthesia and excitement, but celangulin Ⅳ on celangulin prime V poisoning effect with increased Effect, celangulin Ⅴ cephalosporins Ⅳ anesthesia basically no effect. The effects of mixture of celangulin Ⅳ and Ⅴ at different ratios (3:1,1:1,1:1:3) on the sodium channels in cultured neurons of Helicoverpa armigera larvae were compared using whole-cell patch clamp technique . The results showed that the effects of different ratios of celangulin Ⅳ and celangulin Ⅴ on sodium channel (TTX-S) currents were related to the proportion of both, and the content of celangulin Ⅳ was large, indicating that celangulin Ⅳ blocking effect on the channel, sodium current is inhibited; celangulin Ⅴ ratio, then showed the activation of the channel, sodium current increases. In addition, the mixtures with different proportions had no significant effect on the activation voltage of sodium channel (TTX-S) current, but had a significant effect on the peak voltage, which allowed them to move 10 to 20 mV toward the positive potential. These results indicate that celangulin Ⅳ and Ⅴ may act on the same sodium channel binding sites or allosteric coupling sites, both of which are antagonistic to sodium channels.