Han-Young Kim

Synthesis and Evaluation of Coumaroyl Dipeptide Amide as Potential Whitening Agents

Coumaroyl dipeptide amide, Coumaric acid-LG-, was prepared successfully using the solid-phase method, and its efficacy as a skin whitening agent was studied. Coumaric acid-LG- was prepared with Rink-amide resin, and 96.354% of purity was obtained. Using MTT assay and LDH release assay, we found that it exhibited very low cytotoxicity. And, we found that Coumaric acid-LG- inhibited tyrosinase activity dose-dependently and showed superior tyrosinase inhibitory activity to well-known whitening agent, arbutin. value of Coumaric acid-LG- was 182.4 , and value of arbutin was 384.6 . Also, in measurement of melanin contents using B16F1 melanoma cell lines, Coumaric acid-LG- reduced melanin production induced by -MSH statistically significant, and showed superior melanin inhibitory activity to p-coumaric acid or arbutin. In addition, Coumaric acid-LG- reduced MC1R mRNA expression level. Thus, we concluded that MC1R pathway is the significant pathway of Coumaric acid-LG-, and Coumaric acid-LG- has great potential to be used as novel whitening agents.