Anti-melanogenic and Anti-inflammatory effect of novel synthetic compounds

Abstract

The demand for novel anti-melanogenic compounds is increasing due to the weak efficacy and unwanted side effects of present medication. To identify effective anti-melanogenic compounds for cosmetic discovery, we used zebrafish as an animal model. Synthesized compounds were evaluated for their ability to anti-melanogenic effects in the zebrafish model. We identified compounds that affected the pigmentation of developing melanophores in zebrafish. Among them, compound 3d, a novel sulfoxide isoquinoline as an anti-melanogenic agent, which strongly inhibits melanin synthesis in the developing melanophores of zebrafish. Thus, compound 3d has a potential for use in skin-whitening cosmetics. Compound 2i, a synthetic sulfide isoquinoline was first screened for its anti-melanogenic effect using zebrafish larvae. In this study, we also examined its anti-inflammatory activities in vitro using lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Among them, compound 5h and compound 5i, a synthetic 4-fluorophenyl sulfoxide purine and pyrrolo pyrimidine show enhanced the anti-inflammatory effect and Phase 1 liver microsomal stability. These results demonstrated that compound 5h and compound 5i may be effective as anti-inflammatory agents.