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A novel synthetic compound, (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-iminothiazolidin-4-one (MHY773) inhibits mushroom tyrosinase
Jung Hee Jin
Lee Min Jung
Park Yeo Jin
Noh Sang Gyun
Lee A Kyoung
Moon Kyoung Mi
Lee Eun Kyeong
Bang Eun Jin
Park Yun Jung
Kim Su Jeong
Yang Jungho
Ullah Sultan
Chun Pusoon
Jung Young Suk
Moon Hyung Ryong
Chung Hae Young
Bioscience Biotechnology and Biochemistry, 2018, 82(5): 759-767.
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 -phenyl-,-unsaturated carbonyl scaffold template. Among these compounds, (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-iminothiazolidin-4-one (1e, MHY773) exhibited the greatest tyrosinase inhibition (IC50 = 2.87 M and 8.06 M for monophenolase and diphenolase), and outperformed the positive control, kojic acid (IC50 = 15.59 and 31.61 M). The kinetic and docking studies demonstrated that MHY773 interacted with active site of tyrosinase. Moreover, a melanin quantification assay demonstrated that MHY773 attenuates -melanocyte-stimulating hormone (-MSH) and 3-isobutyl-1-methylxanthine (IBMX)-induced melanin contents in B16F10 melanoma cells. 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.
Tyrosinase; alpha-melanocyte-stimulating hormone(-MSH); 3-isobutyl-1-methylxanthine (IBMX); MHY773
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