title: 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.
authors.affiliation: Molecular Inflammation Research Center for Aging Intervention (MRCA), College of Pharmacy, Pusan National University, Busan, 609-735, Republic of Korea.
authors.forename: Min Hi
authors.initials: MH
authors.lastname: Park
authors.forename: Seong Jin
authors.initials: SJ
authors.lastname: Kim
authors.forename: Hyoung Oh
authors.initials: HO
authors.lastname: Jeong
authors.forename: Kyoung Mi
authors.initials: KM
authors.lastname: Moon
authors.forename: Sujin
authors.initials: S
authors.lastname: Son
authors.forename: Dae Hyun
authors.initials: DH
authors.lastname: Kim
authors.forename: Hye Rim
authors.initials: HR
authors.lastname: Kim
authors.forename: Min Jo
authors.initials: MJ
authors.lastname: Kim
authors.forename: Hwi Young
authors.initials: HY
authors.lastname: Yun
authors.forename: Pusoon
authors.initials: P
authors.lastname: Chun
authors.forename: Nam Kyung
authors.initials: NK
authors.lastname: Je
authors.forename: Takako
authors.initials: T
authors.lastname: Yokozawa
authors.forename: Hyung Ryong
authors.initials: HR
authors.lastname: Moon
authors.forename: Hae Young
authors.initials: HY
authors.lastname: Chung
mesh_terms: D000363:Agaricales / Q000201:enzymology; D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D008543:Melanins / Q000037:antagonists & inhibitors*; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D062105:Molecular Docking Simulation; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D017433:Protein Structure, Secondary; D011753:Pyrones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D012878:Skin Neoplasms / Q000188:drug therapy* / Q000473:pathology
chemical_list: D004791:Enzyme Inhibitors; D008543:Melanins; D011753:Pyrones; C011890:kojic acid; D014442:Monophenol Monooxygenase