Abstract
Excessive pigmentation and reduced elasticity are the major skin problems that dermatologists and cosmetologists address. Compounds that inhibit melanin production might contribute to improving skin problems. In this study, we investigated whether coumaric acid- and caffeic acid-conjugated peptides might affect alpha-melanocyte stimulating hormone-induced melanin production, tyrosinase activity, and melanin synthesis-related gene expression in SK-MEL-2 human melanoma cells. Coumaric acid and caffeic acid showed no significant cytotoxicity, and they inhibited melanin production. In addition, coumaric acid- and caffeic acid-conjugated peptides suppressed tyrosinase activity more than arbutin, a known tyrosinase inhibitor. Quantitative real-time PCR (qRT-PCR) results also showed that both peptides inhibited the expression of melanin synthesis-related genes, TYR, TYRP1, TYRP2, and MITF. In particular, among the nine conjugated peptides tested, caffeic acid linked to a Gly-Gly-Gly linker and conjugated to the tripeptide, ARP, showed the greatest inhibition of gene expression in the qRT-PCR analysis. These results suggested that the inhibition of melanin exerted by coumaric acid- and caffeic acid-conjugated peptides might provide important information for the development of pigmentation-related skin diseases and cosmetic products.
Highlights
Melanin is a dark-colored pigment synthesized in melanocytes and transported in vesicles called melanosomes
Released alphamelanocyte stimulating hormone (a-MSH) binds to the MC1R to activate cyclic AMP (cAMP) production, which in turn promotes downstream signaling (Boo, 2019)
microphthalmia-associated transcription factor (MITF) is a key transcription factor that regulates the transcription of melanogenesis-inducing enzymes, such as TYR, tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2) (Yasumoto et al, 1997; Bertolotto et al, 1998)
Summary
Melanin is a dark-colored pigment synthesized in melanocytes and transported in vesicles called melanosomes. Melanin is a very important regulator of biological functions; it controls the color of skin, eyes, hair, and other tissues; it controls skin homeostasis (Slominski et al, 2012). Melanin is carried in melanosomes, which migrate from melanocytes to adjacent keratinocytes. This allows melanin to spread throughout the epidermis, where it protects the skin from environmental exposure, such as harmful ultraviolet (UV) radiation (Epstein, 1983; Menon and Kligman, 2009)
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