Dang, T.H.; Kim, J.Y.; Kim, H.J.; Kim, B.J.; Kim, W.K.; Nam, J.H. Alpha-Mangostin: A Potent Inhibitor of TRPV3 and Pro-Inflammatory Cytokine Secretion in Keratinocytes. Int. J. Mol. Sci.2023, 24, 12930.
Dang, T.H.; Kim, J.Y.; Kim, H.J.; Kim, B.J.; Kim, W.K.; Nam, J.H. Alpha-Mangostin: A Potent Inhibitor of TRPV3 and Pro-Inflammatory Cytokine Secretion in Keratinocytes. Int. J. Mol. Sci. 2023, 24, 12930.
Dang, T.H.; Kim, J.Y.; Kim, H.J.; Kim, B.J.; Kim, W.K.; Nam, J.H. Alpha-Mangostin: A Potent Inhibitor of TRPV3 and Pro-Inflammatory Cytokine Secretion in Keratinocytes. Int. J. Mol. Sci.2023, 24, 12930.
Dang, T.H.; Kim, J.Y.; Kim, H.J.; Kim, B.J.; Kim, W.K.; Nam, J.H. Alpha-Mangostin: A Potent Inhibitor of TRPV3 and Pro-Inflammatory Cytokine Secretion in Keratinocytes. Int. J. Mol. Sci. 2023, 24, 12930.
Abstract
The TRPV3 calcium ion channel is vital for maintaining skin health and has been associated with various skin-related disorders. Since TRPV3 is involved in the development of skin inflammation, inhibiting TRPV3 could be a potential treatment strategy. Alpha-mangostin isolated from Garcinia mangostana L. extract exhibits diverse positive effects on skin health; however, the underlying mechanisms remain obscure. This study investigated the TRPV3-inhibitory properties of alpha-mangostin on TRPV3 hyperactive mutants associated with Olmsted syndrome and its impact on TRPV3-induced cytokine secretion and cell death. Our findings demonstrate that alpha-mangostin effectively inhibits TRPV3, with an IC50 of 0.077 ± 0.013 μM, showing inhibitory effects on both wild-type and mutant TRPV3. TRPV3 inhibition with alpha-mangostin decreased calcium influx and cytokine release, protecting cells from TRPV3-induced death. These results indicate that alpha-mangostin reduced inflammation in TRPV3-activated skin keratinocytes, suggesting that alpha-mangostin could be potentially used for improving inflammatory skin conditions such as dermatitis.
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