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3,4,5-Trimethoxycinnamate thymol ester inhibits melanogenesis in normal human melanocytes and 3D human epidermal equivalents via the PGC-1α-independent PPARγ partial agonism
DC Field | Value | Language |
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dc.contributor.author | Ko, Hyejin | - |
dc.contributor.author | Choi, Hyunjung | - |
dc.contributor.author | Han, Yujia | - |
dc.contributor.author | An, Seungchan | - |
dc.contributor.author | Min, Daejin | - |
dc.contributor.author | Park, Won-Seok | - |
dc.contributor.author | Jin, Sun Hee | - |
dc.contributor.author | Kim, Hyoung-June | - |
dc.contributor.author | Noh, Minsoo | - |
dc.date.accessioned | 2022-06-24T08:37:07Z | - |
dc.date.available | 2022-06-24T08:37:07Z | - |
dc.date.created | 2022-05-10 | - |
dc.date.issued | 2022-01 | - |
dc.identifier.citation | Journal of Dermatological Science | - |
dc.identifier.issn | 0923-1811 | - |
dc.identifier.uri | https://hdl.handle.net/10371/184138 | - |
dc.description.abstract | © 2022 Japanese Society for Investigative DermatologyBackground: 3,4,5-Trimethoxycinnamate thymol ester (TCTE), an anti-melanogenic cosmetic agent prescribed currently, promotes adiponectin synthesis during adipogenesis in human bone marrow mesenchymal stem cells (hBM-MSCs). Adiponectin inhibits melanin biosynthesis and its biosynthesis is directly regulated by peroxisome proliferator-activated receptor (PPAR) γ. In this regard, TCTE may potentially affect PPARγ activity. However, contradicting effects of PPARγ agonists with different chemical structures on human melanogenesis have been reported. Objective: A molecular target of TCTE was investigated to elucidate the association of both adiponectin and PPARγ with anti-melanogenic activity. Methods: The adiponectin secretion-promoting activity of TCTE was tested in an adipogenesis model of hBM-MSCs. A molecular target of TCTE for adiponectin secretion was evaluated via time-resolved fluorescence resonance energy transfer-based receptor binding and transactivation of PPARs. Results: TCTE significantly promoted adiponectin secretion (EC50, 27.9 μM) during adipogenesis in hBM-MSCs and directly bound to PPARγ (Ki, 13.2 μM). The TCTE-bound PPARγ increased the recruitment of SRC-1, SRC-3, and TRAP220/DRIP-1 coactivator peptides without affecting PGC-1α coactivation. In the docking analysis, the optimal ligand binding mode of TCTE exhibited typical ligand-receptor interactions of PPARγ partial agonists. The PPARγ partial agonism of TCTE was established experimentally and the anti-melanogenic activity of TCTE was decreased by treatment with a PPARγ antagonist in cultured normal human melanocytes and a 3D model of human epidermis. Conclusion: The anti-melanogenic activity of TCTE was associated with a PGC-1α-independent PPARγ partial agonism. | - |
dc.language | 영어 | - |
dc.publisher | Elsevier BV | - |
dc.title | 3,4,5-Trimethoxycinnamate thymol ester inhibits melanogenesis in normal human melanocytes and 3D human epidermal equivalents via the PGC-1α-independent PPARγ partial agonism | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.jdermsci.2022.02.010 | - |
dc.citation.journaltitle | Journal of Dermatological Science | - |
dc.identifier.scopusid | 2-s2.0-85125720753 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Noh, Minsoo | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
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