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Sanguinarine is an agonist of TRPA1 channel

文献类型：期刊论文

作者Chi, Hao1,3; Zhang, Xian1,3; Chen, Xueqin1; Fang, Sui1; Ding, Qiang1,2; Gao, Zhaobing1,3
刊名BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
出版日期2021
卷号534页码:226-232
ISSN号0006-291X
关键词Sanguinarine Alkaloid TRPA1 Agonist Pain
DOI10.1016/j.bbrc.2020.11.107
通讯作者Ding, Qiang() ; Gao, Zhaobing(zbgao@simm.ac.cn)
英文摘要Sanguinarine, a benzyl isoquinoline alkaloid extracted from the root of Papaveraceae plants, shows extensive pharmacological activities including anti-microbial, anti-trypanosoma, anti-tumor, antiplatelet, anti-hypertensive effects, as well as inhibition of osteoclast formation. Here we demonstrate that TRPA1 channel (Transient receptor potential cation channel, member Al) is a potential target for sanguinarine. Electrophysiological recordings show that sanguinarine activates TRPA1 channel potently with an EC50 0.09 (0.04-0.13) mu M, but has no effects on other examined TRP channels. Sanguinarine increases the intracellular calcium levels and upregulates the excitability of mouse dorsal root ganglion (DRG) neurons in vitro significantly. Plantar injection of sanguinarine evokes nociceptive behaviors similar to that elicited by allyl isothiocyanate (AITC), a classic agonist of TRPA1. Both the enhancement of excitability of DRG neurons and the nociceptive behaviors can be attenuated by treatment of TRPA1 channel antagonist HC030031 or knockout of trpa1 gene. Taken together, our data demonstrate that sanguinarine is a potent and relatively selective agonist of TRPA1 channel. (C) 2020 Published by Elsevier Inc.
WOS关键词ANKYRIN 1 TRPA1 ; NF-KAPPA-B ; EXPRESSION ; RECEPTOR ; CHELERYTHRINE ; TRPV1
资助项目National Science Fund of Distinguished Young Scholars[81825021] ; National Natural Science Foundation of China[81773707] ; Strategic Leading Science and Technology Projects of Chinese Academy of Sciences[XDA12050308] ; Fund of National Science and Technology Major Project[2018ZX09711002-002-006]
WOS研究方向Biochemistry & Molecular Biology ; Biophysics
语种英语
出版者ACADEMIC PRESS INC ELSEVIER SCIENCE
WOS记录号WOS:000607302500009
源URL[http://119.78.100.183/handle/2S10ELR8/296123]  
专题新药研究国家重点实验室
通讯作者Ding, Qiang; Gao, Zhaobing
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, CAS Key Lab Receptor Res, Shanghai, Peoples R China
2.Shanghai Leado Pharmatech Co Ltd, Shanghai, Peoples R China
3.Univ Chinese Acad Sci, Beijing, Peoples R China
推荐引用方式
GB/T 7714		 Chi, Hao,Zhang, Xian,Chen, Xueqin,et al. Sanguinarine is an agonist of TRPA1 channel[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2021,534:226-232.
APA Chi, Hao,Zhang, Xian,Chen, Xueqin,Fang, Sui,Ding, Qiang,&Gao, Zhaobing.(2021).Sanguinarine is an agonist of TRPA1 channel.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,534,226-232.
MLA Chi, Hao,et al."Sanguinarine is an agonist of TRPA1 channel".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 534(2021):226-232.

入库方式： OAI收割

来源：上海药物研究所

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