[KSCI] Korea Science Citation Index Service

http://dx.doi.org/10.5012/bkcs.2013.34.10.3017

Synthesis and Evaluation of Coumaroyl Dipeptide Amide as Potential Whitening Agents

Lee, Hye-Suk (Central Research Laboratories, Aekyung Co., Ltd.)
Shin, Kyong-Hoon (Central Research Laboratories, Aekyung Co., Ltd.)
Ryu, Geun-Seog (Central Research Laboratories, Aekyung Co., Ltd.)
Cho, In-Shik (Central Research Laboratories, Aekyung Co., Ltd.)
Kim, Jae-Il (Department of Life Science, Gwangju Institute of Science and Technology (GIST))
Lee, Jae-Ho (Department of Life Science, Gwangju Institute of Science and Technology (GIST))
Kim, Han-Young (Central Research Laboratories, Aekyung Co., Ltd.)

Publication Information

Bulletin of the Korean Chemical Society / v.34, no.10, 2013 , pp. 3017-3021 More about this Journal

Abstract

Coumaroyl dipeptide amide, Coumaric acid-LG- $NH_2$ , was prepared successfully using the solid-phase method, and its efficacy as a skin whitening agent was studied. Coumaric acid-LG- $NH_2$ 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- $NH_2$ inhibited tyrosinase activity dose-dependently and showed superior tyrosinase inhibitory activity to well-known whitening agent, arbutin. $IC_{50}$ value of Coumaric acid-LG- $NH_2$ was 182.4 ${\mu}M$ , and $IC_{50}$ value of arbutin was 384.6 ${\mu}M$ . Also, in measurement of melanin contents using B16F1 melanoma cell lines, Coumaric acid-LG- $NH_2$ reduced melanin production induced by ${\alpha}$ -MSH statistically significant, and showed superior melanin inhibitory activity to p-coumaric acid or arbutin. In addition, Coumaric acid-LG- $NH_2$ reduced MC1R mRNA expression level. Thus, we concluded that MC1R pathway is the significant pathway of Coumaric acid-LG- $NH_2$ , and Coumaric acid-LG- $NH_2$ has great potential to be used as novel whitening agents.

Keywords

Coumaroyl dipeptide amide; Tyrosinase; Melanin; Whitening agent;

Citations & Related Records

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