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제125회 대한화학회 학술발표회 및 총회 Synthetic velutin derivatives as potent inhibitors against melanin formation

2020년 2월 6일 16시 33분 13초
MEDI.P-708 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
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Medicinal Chemistry
저자 및
Kooyeon Lee*, Jung Won Choe
Department of Bio-Health Technology, Kangwon National University, Korea
Velutin, a flavonoid compound, has potent inhibitory activity against melanin biosynthesis through inhibiting tyrosinase acitivity. However, inhibitory activity of velutin according to its chemical structure has not been well known. In this study, to reveal relationship between velutin structure and activity, we synthesized 11 derivatives by modifying four functional sites with hydrogen, hydroxyl, and methoxy functionalities. Modification of methoxy (C-4) in B ring with hydroxyl (V-8,V-10) increased cytotoxicity, while other functionality has no effect on cytotoxicity in B16F10 melanoma cells. Inhibitory effect of velutin derivatives on melanogenesis was evaluated by determination of melanin contents and tyrosinase acitivty in melanoma cells. Substitution of hydroxyl (C-5) with methoxy functionalities in A ring of the backbone increased its melanin content, while substitution of methoxy (C-3) with hydrogen functionalities in B ring(V-9) had decrease like as velutin. To confirm these results, we investigated inhibitory effect of two derivatives in vitro using purified enzyme. Based on these results, this study would be helpful for development of novel compound for inhibiting melanogenesis.