Qian Xiao, Zhi-Ping Zhang, Yang-Bo Hou, Dong-Xiao Qu, Le-Le Tang, Li-Ji Chen, Guo-Yi Li, Yong-Hua Ji, Jie Tao, Yu-Dan Zhu
Sheng li xue bao : [Acta physiologica Sinica] 2022 Aug 25The East Asian scorpion Buthus martensii Karsch (BmK) is one of the classical traditional Chinese medicines for treating epilepsy for over a thousand years. Neurotoxins purified from BmK venom are considered as the main active ingredients, acting on membrane ion channels. Voltage-gated sodium channels (VGSCs) play a crucial role in the occurrence of epilepsy, which make them become important drug targets for epilepsy. Long chain toxins of BmK, composed of 60-70 amino acid residues, could specifically recognize VGSCs. Among them, α-like neurotoxins, binding to the receptor site-3 of VGSC, induce epilepsy in rodents and can be used to establish seizure models. The β or β-like neurotoxins, binding to the receptor site-4 of VGSC, have significant anticonvulsant effects in epileptic models. This review aims to illuminate the anticonvulsant/convulsant effects of BmK polypeptides by acting on VGSCs, and provide potential frameworks for the anti-epileptic drug-design.
Qian Xiao, Zhi-Ping Zhang, Yang-Bo Hou, Dong-Xiao Qu, Le-Le Tang, Li-Ji Chen, Guo-Yi Li, Yong-Hua Ji, Jie Tao, Yu-Dan Zhu. Anti-epileptic/pro-epileptic effects of sodium channel modulators from Buthus martensii Karsch. Sheng li xue bao : [Acta physiologica Sinica]. 2022 Aug 25;74(4):621-632
PMID: 35993213
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