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  • Title: Inhibitory effects of 1,3-thiazine derivatives on melanogenesis.
    Author: Ha SK, Koketsu M, Lee M, Moon E, Kim SH, Yoon TJ, Kim SY.
    Journal: J Pharm Pharmacol; 2009 Dec; 61(12):1657-63. PubMed ID: 19958589.
    Abstract:
    OBJECTIVES: The aim of this study was to identify a novel skin-depigmenting agent from synthetic 1,3-thiazine derivatives. METHODS: We investigated the inhibitory effects of six kinds of 1,3-thiazine derivative on melanogenesis by examining their effects on tyrosinase activity and melanin biosynthesis in melan-a cells and the zebrafish model. KEY FINDINGS: Of the six compounds, 4-hydroxy-2,6-dimethyl-5,6-dihydro-4H-1,3-thiazine (TZ-6) had the strongest anti-melanogenic effects in cultured melan-a cells (30.4% inhibition at 100 microm). In addition, TZ-6 exhibited an inhibitory effect on mushroom and cellular tyrosinase. Based on the results of Western blotting, TZ-6 reduced the expression of tyrosinase at 100 microm. Additionally, TZ-6 reduced body pigmentation and inhibited tyrosinase activity in the zebrafish model. CONCLUSIONS: The results have provided useful information for the development of a skin whitening agent.
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