Selective inhibition of overactive warmth-sensitive Ca2+-permeable TRPV3 channels by antispasmodic agent flopropione for alleviation of skin inflammation

Xu, Yimei; Qu, Yaxuan; Zhang, Congxiao; Niu, Canyang; Tang, Xiaowen; Sun, Xiaoying; Wang, KeWei

doi:10.1016/j.jbc.2023.105595

Journal of Biological Chemistry

2024

DOI: 10.1016/j.jbc.2023.105595

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Selective inhibition of overactive warmth-sensitive Ca2+-permeable TRPV3 channels by antispasmodic agent flopropione for alleviation of skin inflammation

Yimei Xu,

Yaxuan Qu,

Congxiao Zhang

et al.

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Cited by 2 publications

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Effects of postbiotics produced by Lactobacillus plantarum JM015 isolated from traditional fermented dairy products on Salmonella-induced intestinal inflammation: A preventive strategy

Pang,

Huang,

et al. 2025

Food Chemistry

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Effects of postbiotics produced by Lactobacillus plantarum JM015 isolated from traditional fermented dairy products on Salmonella-induced intestinal inflammation: A preventive strategy

Pang,

Huang,

et al. 2025

Food Chemistry

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Inhibition of Cutaneous TRPV3 Channels by Natural Caffeic Acid for the Alleviation of Skin Inflammation

Zhang,

Wang,

et al. 2024

Molecules

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Natural caffeic acid (CA) and its analogues have been studied for their potential applications in the treatment of various inflammatory and infectious skin diseases. However, the molecular mechanism underlying the effects of the CA remains largely unknown. Here, we report that CA and its two analogues, caffeic acid phenethyl ester (CAPE) and caffeic acid methyl caffeate (CAMC), inhibit TRPV3 currents in their concentration- and structure-dependent manners with IC50 values ranging from 102 to 410 μM. At the single-channel level, CA reduces the channel open probability and open frequency without alteration of unitary conductance. CA selectively inhibits TRPV3 relative to other subtypes of thermo-TRPs, such as TRPA1, TRPV1, TRPV4, and TRPM8. Molecular docking combined with site-specific mutagenesis reveals that a residue T636 in the Pore-loop is critical for CA binding to TRPV3. Further in vivo evaluation shows that CA significantly reverses TRPV3-mediated skin inflammation induced by skin sensitizer carvacrol. Altogether, our findings demonstrate that CA exerts its anti-inflammatory effects by selectively inhibiting TRPV3 through binding to the pocket formed by the Pore-loop and the S6. CA may serve as a lead for further modification and identification of specific TRPV3 channel inhibitors.

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Selective inhibition of overactive warmth-sensitive Ca2+-permeable TRPV3 channels by antispasmodic agent flopropione for alleviation of skin inflammation

Cited by 2 publications

References 43 publications

Effects of postbiotics produced by Lactobacillus plantarum JM015 isolated from traditional fermented dairy products on Salmonella-induced intestinal inflammation: A preventive strategy

Effects of postbiotics produced by Lactobacillus plantarum JM015 isolated from traditional fermented dairy products on Salmonella-induced intestinal inflammation: A preventive strategy

Inhibition of Cutaneous TRPV3 Channels by Natural Caffeic Acid for the Alleviation of Skin Inflammation

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