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Inhibition of melanogenesis by 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908).

Abstract
Tyrosinase inhibitors might have potential use in cosmetic and medicinal products for the prevention of pigmentation disorders. However, only a few inhibitors are currently used due to their cytotoxicity, and lack of selectivity and stability. In this study, we synthesized several tyrosinase inhibitors and investigated their activity. To investigate the action of 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908) specifically in the inhibition of melanogenesis, a mushroom tyrosinase activity assay was performed. We confirmed the inhibitory effect of MHY908 at various melanin concentrations using α-MSH-induced melanoma cells. Our results indicate that MHY908 potently inhibited mushroom tyrosinase activity (IC50 = 8.19 μM) in a dose-dependent manner. Through a docking simulation, we also analyzed its binding mode to inhibit tyrosinase activity. MHY908 also decreased melanin synthesis without inducing cytotoxicity. These results suggest that MHY908 is a good candidate for prevention and treatment of pigmentation disorders.
AuthorsMin Hi Park, Seong Jin Kim, Hyoung Oh Jeong, Kyoung Mi Moon, Sujin Son, Dae Hyun Kim, Hye Rim Kim, Min Jo Kim, Hwi Young Yun, Pusoon Chun, Nam Kyung Je, Takako Yokozawa, Hyung Ryong Moon, Hae Young Chung
JournalArchives of pharmacal research (Arch Pharm Res) Vol. 38 Issue 4 Pg. 505-11 (Apr 2015) ISSN: 1976-3786 [Electronic] Korea (South)
PMID25502981 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Enzyme Inhibitors
  • Melanins
  • Pyrones
  • kojic acid
  • Monophenol Monooxygenase
Topics
  • Agaricales (enzymology)
  • Animals
  • Cell Survival (drug effects)
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors (chemistry, pharmacology, therapeutic use)
  • Melanins (antagonists & inhibitors)
  • Melanoma, Experimental (drug therapy, pathology)
  • Mice
  • Molecular Docking Simulation
  • Monophenol Monooxygenase (antagonists & inhibitors, metabolism)
  • Protein Structure, Secondary
  • Pyrones (chemistry, pharmacology, therapeutic use)
  • Skin Neoplasms (drug therapy, pathology)

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