Background/Aims: Excessive melanogenesis often causes unaesthetic hyperpigmentation. In a previous report, our group introduced a newly synthesized depigmentary agent, Melasolv™ (3,4,5-trimethoxycinnamate thymol ester). In this study, we demonstrated the significant whitening efficacy of Melasolv using various melanocytes and human skin equivalents as in vitro experimental systems. Methods: The depigmentary effect of Melasolv was tested in melan-a cells (immortalized normal murine melanocytes), α-melanocyte-stimulating hormone (α-MSH)-stimulated B16 murine melanoma cells, primary normal human melanocytes (NHMs), and human skin equivalent (MelanoDerm). The whitening efficacy of Melasolv was further demonstrated by photography, time-lapse microscopy, Fontana-Masson (F&M) staining, and 2-photon microscopy. Results: Melasolv significantly inhibited melanogenesis in the melan-a and α-MSH-stimulated B16 cells. In human systems, Melasolv also clearly showed a whitening effect in NHMs and human skin equivalent, reflecting a decrease in melanin content. F&M staining and 2-photon microscopy revealed that Melasolv suppressed melanin transfer into multiple epidermal layers from melanocytes as well as melanin synthesis in human skin equivalent. Conclusion: Our study showed that Melasolv clearly exerts a whitening effect on various melanocytes and human skin equivalent. These results suggest the possibility that Melasolv can be used as a depigmentary agent to treat pigmentary disorders as well as an active ingredient in cosmetics to increase whitening efficacy.

1.
Swalwell H, Latimer J, Haywood RM, Birch-Machin MA: Investigating the role of melanin in UVA/UVB- and hydrogen peroxide-induced cellular and mitochondrial ROS production and mitochondrial DNA damage in human melanoma cells. Free Radic Biol Med 2012;52:626-634.
2.
Briganti S, Camera E, Picardo M: Chemical and instrumental approaches to treat hyperpigmentation. Pigment Cell Res 2003;16:101-110.
3.
Ando H, Kondoh H, Ichihashi M, Hearing V: Approaches to identify inhibitors of melanin biosynthesis via the quality control of tyrosinase. J Invest Dermatol 2007;127:751-761.
4.
Solano F, Briganti S, Picardo M, Ghanem G: Hypopigmenting agents: an updated review on biological, chemical and clinical aspects. Pigment Cell Res 2006;19:550-571.
5.
Kang HH, Rho HS, Hwang JS, Oh SG: Depigmenting activity and low cytotoxicity of alkoxy benzoates or alkoxy cinnamte in cultured melanocytes. Chem Pharm Bull (Tokyo) 2003;51:1085-1088.
6.
Lee ES, Park JH, Lee SW, Hahn J, Lee H, Chae SW, Lee TG, Moon DW, Kim SH: Lipid crystals mechanically stimulate adjacent extracellular matrix in advanced atherosclerotic plaques. Atherosclerosis 2014;37:769-776.
7.
Han M, Giese G, Schmitz-Valckenberg S, Bindewald-Wittich A, Holz FG, Yu J, Bille JF, Niemz MH: Age-related structural abnormalities in the human retina-choroid complex revealed by two-photon excited autofluorescence imaging. J Biomed Opt 2007;12:024012.
8.
Siegrist W, Eberle AN: In situ melanin assay for MSH using mouse B16 melanoma cells in culture. Anal Biochem 1986;159:191-197.
9.
Santiago-Walker A, Li L, Haass NK, Herlyn M: Melanocytes: from morphology to application. Skin Pharmacol Physiol 2009;22:114-121.
10.
Lee CS, Shin YJ, Won C, Lee YS, Park CG, Ye SK, Chung MH: Simvastatin acts as an inhibitor of interferon gamma-induced cycloxygenase-2 expression in human THP-1 cells, but not in murine RAW264.7 cells. Biocell 2009;33:107-114.
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