鉴定6,7,4'-三羟基异黄酮为一种有效的酪氨酸酶抑制剂。
Identifying 6,7,4'-trihydroxyisoflavone as a potent tyrosinase inhibitor.
作者信息
Chang Te-Sheng, Ding Hsiou-Yu, Lin Hang-Ching
机构信息
Department of Biological Science and Technology, National University of Tainan, Taiwan.
出版信息
Biosci Biotechnol Biochem. 2005 Oct;69(10):1999-2001. doi: 10.1271/bbb.69.1999.
A known biotransformed compound, 6,7,4'-trihydroxyisoflavone, was identified as a potent tyrosinase inhibitor. It inhibited mushroom tyrosinase with an IC50 value of 9.2 microM, which is six times the anti-tyrosinase activity of kojic acid (IC50 = 54.4 microM). The inhibition kinetics, analyzed by Lineweaver-Burk plots, indicated 6,7,4'-trihydroxyisoflavone to be a competitive inhibitor of tyrosinase when L-tyrosine was used as a substrate. Its biosynthesis precursors and analogs, including glycitein, daidzein, and genistein, showed little anti-tyrosinase activity. The results suggest that hydroxyl groups at the C-6 and C-7 positions of the isoflavone skeleton might play an important role in the expression of tyrosinase inhibitory activity.
一种已知的生物转化化合物6,7,4'-三羟基异黄酮被鉴定为一种有效的酪氨酸酶抑制剂。它对蘑菇酪氨酸酶的抑制中浓度（IC50）值为9.2微摩尔，是曲酸抗酪氨酸酶活性（IC50 = 54.4微摩尔）的6倍。通过Lineweaver-Burk图分析的抑制动力学表明，当以L-酪氨酸为底物时，6,7,4'-三羟基异黄酮是酪氨酸酶的竞争性抑制剂。其生物合成前体和类似物，包括大豆黄素、黄豆苷元和染料木黄酮，几乎没有抗酪氨酸酶活性。结果表明，异黄酮骨架C-6和C-7位的羟基可能在酪氨酸酶抑制活性的表达中起重要作用。
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