MMS 1001 inhibits melanin synthesis via ERK activation.

Abstract	Melanin plays major a role in pigmentation of hair, eyes, and skin in mammals. In this study, the inhibitory effects of MMS 1001 on alpha-MSH-stimulated melanogenesis were investigated in B16F10 melanoma cells. MMS 1001 did not show cytotoxic effects up to 10 microM. Melanin content and intracellular tyrosinase activity were inhibited by MMS 1001 treatment in a dose-dependent manner. In Western blot analysis, MITF expression was decreased by MMS 1001. In addition, tyrosinase expressions were also reduced after MMS 1001 treatment. Further results showed that the phosphorylation of ERK was induced by MMS 1001. Moreover, a specific MEK inhibitor, PD98059, abrogated the inhibitory effects of MMS 1001 on melanin production and tyrosinase expression. These results indicate that the hypopigmentary effects of MMS 1001 resulted from the inhibition of MITF and tyrosinase expression via phosphorylation of ERK. Thus, MMS 1001 could be developed as a new effective skin-whitening agent.
Authors	Hyun-E Lee, Jiho Song, Su Yeon Kim, Kyoung-Chan Park, Kyung Hoon Min, Dong-Seok Kim
Journal	Die Pharmazie (Pharmazie) Vol. 68 Issue 3 Pg. 212-6 (Mar 2013) ISSN: 0031-7144 [Print] Germany
PMID	23556341 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Enzyme Inhibitors Flavonoids Isoxazoles MMS 1001 Melanins Microphthalmia-Associated Transcription Factor Mitf protein, mouse Piperazines Monophenol Monooxygenase Extracellular Signal-Regulated MAP Kinases 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
Topics	Animals Blotting, Western Cell Line Cell Line, Tumor Cell Survival (drug effects) Enzyme Activation (drug effects) Enzyme Inhibitors (pharmacology) Extracellular Signal-Regulated MAP Kinases (antagonists & inhibitors, metabolism) Flavonoids (pharmacology) Isoxazoles (pharmacology) MAP Kinase Signaling System (drug effects) Melanins (antagonists & inhibitors, biosynthesis) Mice Microphthalmia-Associated Transcription Factor (genetics) Monophenol Monooxygenase (biosynthesis) Phosphorylation Piperazines (pharmacology) Signal Transduction (drug effects)

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