Antimelanogenic Efficacy of Melasolv (3,4,5-Trimethoxycinnamate Thymol Ester) in Melanocytes and Three-Dimensional Human Skin Equivalent

Skin Pharmacol Physiol. 2017;30(4):190-196. doi: 10.1159/000477356. Epub 2017 Jun 30.

Abstract

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.

Keywords: Depigmentary agent; Melanogenesis; Melasolv; Three-dimensional human skin equivalent.

MeSH terms

  • Animals
  • Cell Line
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cinnamates / pharmacology*
  • Esters / pharmacology*
  • Humans
  • Hyperpigmentation / drug therapy
  • Melanins / metabolism
  • Melanocytes / drug effects*
  • Melanocytes / metabolism
  • Melanoma, Experimental
  • Mice
  • Skin / drug effects
  • Skin / metabolism
  • Skin Lightening Preparations / pharmacology*

Substances

  • Cinnamates
  • Esters
  • Melanins
  • Skin Lightening Preparations