Oxyresveratrol as the potent inhibitor on dopa oxidase activity of mushroom tyrosinase
Oxyresveratrol as the potent inhibitor on dopa oxidase activity of mushroom tyrosinase
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DOI：
10.1006/bbrc.1998.8169
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发表时间：
1998-02-24
影响因子：
3.1
通讯作者：
Kim, Y
中科院分区：
文献类型：
--
作者：
Shin, NH;Ryu, SY;Kim, Y
氧化白藜芦醇（2，3 '，4，5'-四羟基芪），一种天然存在的化合物，特别是在桑树中发现，对酪氨酸酶的多巴氧化酶活性表现出有效的抑制作用，酪氨酸酶催化黑色素生物合成的限速步骤。0.3至5 μ M的氧化白藜芦醇对酶活性表现出强效且剂量依赖性的抑制作用（25至84%），其中在约1 μ M的浓度下显示出50%的抑制作用。当以左旋多巴为底物时，氧化白藜芦醇对酪氨酸酶的多巴氧化酶活性呈非竞争性抑制（Ki = 9.1 × 10 ~（-7）M）。氧化白藜芦醇表现出比白藜芦醇（3，4 '，5-三羟基芪）强约150倍的抑制作用。羟基芪类化合物中的羟基甲基化为甲氧基的程度越高，对酶活性的抑制作用越小。结果表明，羟基的数量和位置的氧化白藜芦醇似乎在发挥蘑菇酪氨酸酶的多巴氧化酶活性的抑制作用中起着关键作用，（C）1998学术出版社。
Oxyresveratrol (2,3',4,5'-tetrahydroxystilbene), a naturally occurring compound particularly found in Morus alba L., exhibited a potent inhibitory effect on dopa oxidase activity of tyrosinase which catalyzes rate limiting steps of melanin biosynthesis. Oxyresveratrol with 0.3 to 5 mu M exhibited potent and dose dependent inhibitions (25 to 84%) on the enzyme activity, where 50% of inhibition was shown at the concentration of about 1 mu M. Oxyresveratrol seemed to inhibit the dopa oxidase activity of tyrosinase via a noncompetitive manner (Ki = 9.1 x 10(-7) M) when L-dopa was used as a substrate. Oxyresveratrol exhibited about a 150-fold more potent inhibitory effect than resveratrol (3,4',5-trihydroxystilbene). The more hydroxy groups of the hydroxystilbenes are methylated to be methoxy groups, while the less inhibitory effects on the enzyme activity were exhibited. The results indicate that both the number and positions of hydroxy groups in oxyresveratrol seem to play a critical role in exerting the inhibitory effect on dopa oxidase activity of mushroom tyrosinase, (C) 1998 Academic Press.