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KMID : 0613820190290070755
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Journal of Life Science
2019 Volume.29 No. 7 p.755 ~ p.761
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Kojic Acid Derivatives, Have Tyrosinase Inhibitory Activity to Suppress the Production of Melanin in the Biosynthetic Pathway
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Park Jung-Youl
Lee Ha-Neul
Hu Meng-Yang
Park Jeong-Ho
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Abstract
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Kojic acid (KA) is produced by Aspergillus oryzae-sort of like mushrooms, which is commonly called as koji in Japan. KA is used as a chelation agent and a preservative preventing oxidative browning of fruits. KA also shows antibacterial and antifungal properties. Because KA stops the production of melanin by inhibiting tyrosinase in the biosynthetic pathway from tyrosine to melanin in skin, it has been applied as a skin lightening ingredient in cosmetics. Since some animal studies have shown that high amounts of KA had side effects such as in liver, kidney, reproductive, cardiovascular, gastrointestinal, respiratory, brain, and nervous system, more efficient KA derivatives are needed to be developed in order to safely apply as a skin lightening ingredient. A series of KA derivatives via conjugated with triazole by click reaction were synthesized and their in vitro tyrosinase inhibitory activities were evaluated. Most of all KA derivatives have shown in moderate tyrosinase inhibitory activities. In case of KA-hybrid compound, 1~3 have shown tyrosinase inhibitory activities about 50~10,000 times more effective tyrosinase inhibitor compared to KA itself. Specifically, the IC50 value of KA-hybrid compound, 2 was 0.0044±0.74 μM against tyrosinase. It is about 10,000 times more effective tyrosinase inhibitor compared to KA itself (IC50=45.2±4.6 μM).
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KEYWORD
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Antioxidant, Kojic acid, melanin, tyrosinase inhibitory activity, tyrosine
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