We investigated the inhibitory effects of a novel amphiphilic ascorbic derivative,
disodium isostearyl 2-O-L-ascorbyl phosphate (VCP-IS-2Na), synthesized from a hydrophilic ascorbic derivative, sodium-2-O-L-ascorbyl
phosphate (VCP-Na), on melanogenesis in cultured human
melanoma cells, normal human melanocytes, and three-dimensional cultured human skin models.
Melanin synthesis in
melanoma cells treated with
VCP-IS-2Na at 300 muM and melanocytes treated with
VCP-IS-2Na at 100 muM decreased to 23% and 52% of that in non-treated cells, respectively, and the cell viability was not affected.
VCP-IS-2Na also significantly suppressed the cellular
tyrosinase activity of
melanoma cells and melanocytes.
Melanin synthesis in human skin models was evaluated by macro- and microscopic observations of its pigmentation and quantitative measurements of
melanin. Treatment of the human skin models with 1.0%
VCP-IS-2Na did not inhibit cell viability, while
melanin synthesis was decreased to 21% of that in the control. In contrast,
L-ascorbic acid (VC) and VCP-Na did not seem to inhibit
melanin synthesis and cellular
tyrosinase activity. These results indicate that
VCP-IS-2Na may be an effective
whitening agent for the skin, and we expect the application of
VCP-IS-2Na in the cosmetic industry.