Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches
The suppression of tyrosinase (TYR), a key enzyme in melanogenesis, has been suggested as an effective strategy for preventing melanin accumulation. We previously discovered the novel chrysin derivative hydroxyethyl chrysin (HE-chrysin) through an irradiation technique, which exerted higher anti-inf...
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Elsevier
2025-01-01
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844025000982 |
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| author | Yuna Lee Ha-Yeon Song Eui-Baek Byun |
| author_facet | Yuna Lee Ha-Yeon Song Eui-Baek Byun |
| author_sort | Yuna Lee |
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| description | The suppression of tyrosinase (TYR), a key enzyme in melanogenesis, has been suggested as an effective strategy for preventing melanin accumulation. We previously discovered the novel chrysin derivative hydroxyethyl chrysin (HE-chrysin) through an irradiation technique, which exerted higher anti-inflammatory and anti-cancer activities than original chrysin. In the present study, we explored whether HE-chrysin has antioxidant and anti-melanogenic capacity using in vitro B16F10 murine melanoma cells and in silico molecular docking. HE-chrysin exhibited enhanced antioxidant capacity in DPPH, ABTS, and FRAP assays, and it decreased cellular H2O2-stimulated reactive oxygen species levels in comparison to original chrysin. At 2.5 μM, HE-chrysin reduced 3-isobutyl-1-methylxanthine-stimulated melanin production significantly by suppressing intracellular TYR activity without cytotoxicity. Furthermore, molecular docking showed that HE-chrysin inhibited TYR activity by interacting with key residues (Glu256 and Asn260) and chelating Cu+ ions at the active site, with a binding free energy of −7.00 kcal/mol compared with arbutin (−5.12 kcal/mol). Our findings show that HE-chrysin is an anti-melanogenic candidate and a potential antioxidant for use in dermatologic therapy. |
| format | Article |
| id | doaj-art-cb06310db1b7402db0cce6e029c5aaa5 |
| institution | Kabale University |
| issn | 2405-8440 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Elsevier |
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| series | Heliyon |
| spelling | doaj-art-cb06310db1b7402db0cce6e029c5aaa52025-02-02T05:28:01ZengElsevierHeliyon2405-84402025-01-01112e41718Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approachesYuna Lee0Ha-Yeon Song1Eui-Baek Byun2Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, 56212, Republic of KoreaAdvanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, 56212, Republic of KoreaCorresponding author.; Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, 56212, Republic of KoreaThe suppression of tyrosinase (TYR), a key enzyme in melanogenesis, has been suggested as an effective strategy for preventing melanin accumulation. We previously discovered the novel chrysin derivative hydroxyethyl chrysin (HE-chrysin) through an irradiation technique, which exerted higher anti-inflammatory and anti-cancer activities than original chrysin. In the present study, we explored whether HE-chrysin has antioxidant and anti-melanogenic capacity using in vitro B16F10 murine melanoma cells and in silico molecular docking. HE-chrysin exhibited enhanced antioxidant capacity in DPPH, ABTS, and FRAP assays, and it decreased cellular H2O2-stimulated reactive oxygen species levels in comparison to original chrysin. At 2.5 μM, HE-chrysin reduced 3-isobutyl-1-methylxanthine-stimulated melanin production significantly by suppressing intracellular TYR activity without cytotoxicity. Furthermore, molecular docking showed that HE-chrysin inhibited TYR activity by interacting with key residues (Glu256 and Asn260) and chelating Cu+ ions at the active site, with a binding free energy of −7.00 kcal/mol compared with arbutin (−5.12 kcal/mol). Our findings show that HE-chrysin is an anti-melanogenic candidate and a potential antioxidant for use in dermatologic therapy.http://www.sciencedirect.com/science/article/pii/S2405844025000982MelanogenesisB16F10 cellsMolecular docking |
| spellingShingle | Yuna Lee Ha-Yeon Song Eui-Baek Byun Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches Heliyon Melanogenesis B16F10 cells Molecular docking |
| title | Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches |
| title_full | Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches |
| title_fullStr | Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches |
| title_full_unstemmed | Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches |
| title_short | Anti-melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity: In vitro and in silico approaches |
| title_sort | anti melanogenic effects of hydroxyethyl chrysin through the inhibition of tyrosinase activity in vitro and in silico approaches |
| topic | Melanogenesis B16F10 cells Molecular docking |
| url | http://www.sciencedirect.com/science/article/pii/S2405844025000982 |
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