Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors.

Yi W; Cao R; Wen H; Yan Q; Zhou B; Wan Y; Ma L; Song H

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Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors.

机译：螺旋类似物作为蘑菇酪氨酸酶抑制剂的合成和生物学评估。

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A series of helicid analogues were synthesized and evaluated as tyrosinase inhibitors. The results demonstrated that some compounds had more potent inhibitory activities than arbutin (IC(50) 7.3 mM). In particular, compound 1c bearing 4,6-O-benzylidene substituent on the sugar moiety was found to be the most potent inhibitor with IC(50) value of 0.052 mM. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that helicid analogues were competitive inhibitors. The Circular dichroism spectra indicated that those compounds induced conformational changes of mushroom tyrosinase upon binding.

机译：合成了一系列螺旋类似物，并评价为酪氨酸酶抑制剂。结果表明，某些化合物比熊果苷具有更强的抑制活性（IC（50）7.3 mM）。特别地，发现在糖部分上带有4,6-O-亚苄基取代基的化合物1c是最有效的抑制剂，IC（50）值为0.052 mM。通过Lineweaver-Burk图分析的抑制动力学表明，螺旋类似物是竞争性抑制剂。圆二色性光谱表明，这些化合物在结合后诱导了蘑菇酪氨酸酶的构象变化。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Yi W; Cao R; Wen H; Yan Q; Zhou B; Wan Y; Ma L; Song H;
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原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
helicide; tyrosinase inhibitor; Agaricales; Synthesis; 伞菌目;

机译：杀icide剂;酪氨酸酶抑制剂;木耳;合成;伞菌目;

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1. Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors. [J] . Yi W, Cao R, Wen H, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

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Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors.

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