Effects of BmKNJX11, a bioactive polypeptide purified from Buthus martensi Karsch, on TTX-R sodium channels in rat dorsal root ganglion neurons

Xijie Wang; Peng Xu; Shanshan An; Qin Sun; Jie Cheng; Rong Gao; Hang Xiao

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Effects of BmKNJX11, a bioactive polypeptide purified from Buthus martensi Karsch, on TTX-R sodium channels in rat dorsal root ganglion neurons

Xijie Wang 1 #,Peng Xu 2,Shanshan An 2,Qin Sun 2,Jie Cheng 2,Rong Gao 2,Hang Xiao 2 *

1.1.Laboratory of neurotoxicology, School of Public Health , Nanjing Medical University 2.National Shanghai Center for New Drug Safety Evaluation and Research

2.Laboratory of neurotoxicology, School of Public Health , Nanjing Medical University

*Correspondence author

#Submitted by

Subject:

Funding: 教育部博士点基金（No.20060312001）

Opened online:28 July 2009

Accepted by: none

Citation: Xijie Wang,Peng Xu,Shanshan An.Effects of BmKNJX11, a bioactive polypeptide purified from Buthus martensi Karsch, on TTX-R sodium channels in rat dorsal root ganglion neurons[OL]. [28 July 2009] http://en.paper.edu.cn/en_releasepaper/content/34118

BmKNJX11is a 7036.85 Da polypeptide purified from the venom of Asian scorpion Buthus martensi Karsch (BmK). With whole cell recording, BmKNJX11 inhibited tetrodotoxin- resistant voltage-gated sodium channels (TTX-R VGSC) in freshly isolated rat dorsal root ganglion (DRG) neurons in a concentration- and voltage-dependent manner. At a concentration of 40 μg/ml BmKNJX11 increased the activation threshold and produced positive shifting of TTX-R sodium current (INa) activation curve. In addition, BmKNJX11 induced shifting of the steady-state inactivation curve to left, delayed the recovery of TTX-R INa from inactivation, and also reduced the fraction of available sodium channels. These results suggested that BmKNJX11 might exert effects on VGSC by binding to a specific site. Considering that TTX-R VGSC expressed in DRG neurons play a critical role in nociceptive transmission, the interaction of BmKNJX11 with TTX-R VGSC might lead to a change in excitability of nociceptive afferent fibers which may be involved in the observed peripheral pain expression.

Keywords:Buthus martensi Karsch;Patch Clamp;Sodium Channel

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