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Anti-epileptic/pro-epileptic effects of sodium channel modulators from Buthus martensii Karsch

XIAO Qian¹, ZHANG Zhi-Ping², HOU Yang-Bo¹, QU Dong-Xiao¹, TANG Le-Le^1,3, CHEN Li-Ji¹, LI Guo-Yi^1,3, JI Yong-Hua², TAO Jie^1,3, ZHU Yu-Dan^1,3,*

¹Department of Neurology and Central Laboratory, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200333, China；²School of Medicine and School of Life Sciences, Shanghai University, Shanghai 200444, China；³Putuo Clinical Medical School, Anhui Medical University, Shanghai 200333, China

Abstract

The 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.

Key words: Buthus martensii Karsch; toxin; epilepsy; voltage-gated sodium channels; receptor site

Received: 　　Accepted:

Corresponding author: 朱宇丹　　E-mail: yudanzhu_putuo@foxmail.com

DOI: 10.13294/j.aps.2022.0064

Citing This Article：

XIAO Qian, ZHANG Zhi-Ping, HOU Yang-Bo, QU Dong-Xiao, TANG Le-Le, CHEN Li-Ji, LI Guo-Yi, JI Yong-Hua, TAO Jie, ZHU Yu-Dan. Anti-epileptic/pro-epileptic effects of sodium channel modulators from Buthus martensii Karsch. Acta Physiol Sin 2022; 74 (4): 621-632