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辣椒素对德国小蠊（）突变的电压门控钠通道的影响。

Effect of capsaicin on voltage-gated sodium channels with mutation from German cockroaches ().

作者信息

Kamezaki Masashi, Nishiwaki Hisashi

机构信息

The United Graduate School of Agriculture, Ehime University.

Agro & Life Solutions Research Laboratory, Sumitomo Chemical Co. Ltd.

出版信息

J Pestic Sci. 2025 Aug 20;50(3):74-80. doi: 10.1584/jpestics.D25-023.

DOI:10.1584/jpestics.D25-023
PMID:40910013
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12405009/
Abstract

Capsaicin inhibits the current flow in the voltage-gated sodium channels (VGSCs) of mammals and insects. The aim of the present study was to elucidate capsaicin toxicity in pyrethroid-susceptible and knockdown resistant (; with reduced pyrethroid sensitivity) strains of the German cockroach () and its effects on VGSCs carrying the mutation. Injection tests revealed that adult cockroaches from susceptible and strains exhibited sluggish movement and paralysis upon abdominal capsaicin administration, consistent with its inhibitory effect on VGSC currents. The LD values of capsaicin were 16 and 36 µg per insect for the susceptible and strains, respectively, yielding a resistance ratio of 2.3. Two-electrode voltage clamp assays showed that the EC values for the capsaicin-mediated inhibition of VGSC currents were 4.27 and 9.19 µM for susceptible and mutant channels, respectively, yielding a resistance ratio of 2.2. The findings indicate that capsaicin retains inhibitory activity against insect VGSCs even in the presence of mutations.

摘要

辣椒素可抑制哺乳动物和昆虫电压门控钠通道（VGSCs）中的电流。本研究旨在阐明辣椒素对拟除虫菊酯敏感型和击倒抗性（拟除虫菊酯敏感性降低）品系德国小蠊（Blattella germanica）的毒性及其对携带L925I突变的VGSCs的影响。注射试验表明，给敏感品系和击倒抗性品系的成年蟑螂腹部注射辣椒素后，它们会出现行动迟缓及麻痹现象，这与其对VGSC电流的抑制作用一致。辣椒素对敏感品系和击倒抗性品系的半数致死剂量（LD）分别为每只昆虫16和36μg，抗性比为2.3。双电极电压钳试验表明，辣椒素介导的对VGSC电流抑制作用的半数有效浓度（EC），敏感通道和L925I突变通道分别为4.27和9.19μM，抗性比为2.2。研究结果表明，即使存在L925I突变，辣椒素对昆虫VGSCs仍具有抑制活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/9f474c67e802/jps-50-3-D25-023-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/3b8baf569e51/jps-50-3-D25-023-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/5d9577c59031/jps-50-3-D25-023-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/b290290a3f51/jps-50-3-D25-023-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/9f474c67e802/jps-50-3-D25-023-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/3b8baf569e51/jps-50-3-D25-023-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/5d9577c59031/jps-50-3-D25-023-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/b290290a3f51/jps-50-3-D25-023-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0537/12405009/9f474c67e802/jps-50-3-D25-023-figure04.jpg

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本文引用的文献

1
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Toxicon. 2025 Mar;256:108264. doi: 10.1016/j.toxicon.2025.108264. Epub 2025 Jan 29.
2
Cross resistance to brevetoxin-3 by kdr and super-kdr mutations in house flies.家蝇中 kdr 和超级 kdr 突变对布雷菲德菌素-3 的交叉抗性。
Pestic Biochem Physiol. 2024 May;201:105898. doi: 10.1016/j.pestbp.2024.105898. Epub 2024 Apr 8.
3
Leucine to tryptophane substitution in the pore helix IIP1 confer sodium channel resistance to pyrethroids and DDT.
在孔螺旋 IIp1 中的亮氨酸到色氨酸取代赋予钠离子通道对拟除虫菊酯和滴滴涕的抗性。
Pestic Biochem Physiol. 2023 Aug;194:105490. doi: 10.1016/j.pestbp.2023.105490. Epub 2023 Jun 9.
4
Transient receptor potential vanilloid 1 (TRPV1)-independent actions of capsaicin on cellular excitability and ion transport.辣椒素对细胞兴奋性和离子转运的瞬时受体电位香草素 1（TRPV1）非依赖性作用。
Med Res Rev. 2023 Jul;43(4):1038-1067. doi: 10.1002/med.21945. Epub 2023 Mar 14.
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Capsaicin Inhibits Multiple Voltage-Gated Ion Channels in Rabbit Ventricular Cardiomyocytes in TRPV1-Independent Manner.辣椒素以不依赖瞬时受体电位香草酸亚型1（TRPV1）的方式抑制兔心室肌细胞中的多种电压门控离子通道。
Pharmaceuticals (Basel). 2022 Sep 26;15(10):1187. doi: 10.3390/ph15101187.
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Pyrethroids in an AlphaFold2 Model of the Insect Sodium Channel.昆虫钠通道的AlphaFold2模型中的拟除虫菊酯
Insects. 2022 Aug 18;13(8):745. doi: 10.3390/insects13080745.
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