Anti-epileptic/pro-epileptic effects of sodium channel modulators from Buthus martensii Karsch.
- Author:
Qian XIAO
1
;
Zhi-Ping ZHANG
2
;
Yang-Bo HOU
1
;
Dong-Xiao QU
1
;
Le-Le TANG
1
;
Li-Ji CHEN
1
;
Guo-Yi LI
1
;
Yong-Hua JI
2
;
Jie TAO
1
;
Yu-Dan ZHU
1
Author Information
1. Department of Neurology and Central Laboratory, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200333, China.
2. School of Medicine and School of Life Sciences, Shanghai University, Shanghai 200444, China.
- Publication Type:Review
- MeSH:
Animals;
Anticonvulsants/therapeutic use*;
Neurotoxins/pharmacology*;
Scorpion Venoms/pharmacology*;
Scorpions/chemistry*;
Voltage-Gated Sodium Channels
- From:
Acta Physiologica Sinica
2022;74(4):621-632
- CountryChina
- Language:English
-
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.
