A novel synthetic compound, (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-iminothiazolidin-4-one (MHY773) inhibit mushroom tyrosinase

• 발행기관: 한국노년학회
• 저자명: Hee Jin Jung Min Jung Lee YeoJinPark Sang Gyn Noh A Kyoung Lee Kyoung Mi Moon Eun Kyeong Lee Eun Jin Bang Hyung Ryong Moon Hae Young Chung
• 간행물 정보: 『한국노년학회 학술대회 논문집』2017년 한국노인과학학술대회, 259~259쪽, 전체 1쪽
• 주제분류: 사회과학 > 사회복지학
• 파일형태: PDF
• 발행일자: 2017.11.03

영문 초록

As part of continued efforts for the development of new tyrosinase inhibitors, (Z)-5-(substituted benzylidene)-2-iminothiazolidin-4-one derivatives (1a–1l) were rationally synthesized and evaluated for their inhibitory potential in vitro. These compounds were designed and synthesized based on the structural attributes of a β-phenyl-α,β-unsaturated carbonyl scaffold template. Among these compounds, (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-iminothiazolidin-4-one (1e, MHY773) exhibited the greatest tyrosinase inhibition (IC 50 =2.87mM), and outperformed the positive control, kojic acid (IC 50 =15.59mM). The kinetic and docking studies demonstrated that MHY773 interacted with active site of tyrosinase. Moreover, a melanin quantification assay demonstrated that MHY773 attenuates α-melanocyte-stimulating hormone (α-MSH) and 3-isobutyl-1-methylxanthine (IBMX)-induced melanin contents in B16F10 melanoma cells, without significant cytotoxicity. Taken together, these data suggest that MHY773 suppressed the melanin production via the inhibition of tyrosinase activity. MHY773 is a promising for the development of effective pharmacological and cosmetic agents for skin-whitening.

키워드

Tyrosinase inhibitor α-MSH IBMX MHY773