Sanguinarine is an agonist of TRPA1 channel.

Hao Chi, Xian Zhang, Xueqin Chen, Sui Fang, Qiang Ding, Zhaobing Gao

Biochemical and biophysical research communications 2021 Jan 01

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Sanguinarine, a benzyl isoquinoline alkaloid extracted from the root of Papaveraceae plants, shows extensive pharmacological activities including anti-microbial, anti-trypanosoma, anti-tumor, anti-platelet, anti-hypertensive effects, as well as inhibition of osteoclast formation. Here we demonstrate that TRPA1 channel (Transient receptor potential cation channel, member A1) is a potential target for sanguinarine. Electrophysiological recordings show that sanguinarine activates TRPA1 channel potently with an EC50 0.09 (0.04-0.13) μM, 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. Copyright © 2020. Published by Elsevier Inc.

Citation

Hao Chi, Xian Zhang, Xueqin Chen, Sui Fang, Qiang Ding, Zhaobing Gao. Sanguinarine is an agonist of TRPA1 channel. Biochemical and biophysical research communications. 2021 Jan 01;534:226-232