Yi Wei, Cao Rihui, Wen Huan, Yan Qin, Zhou Binhua, Wan Yiqian, Ma Lin, Song Huacan
School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xin Gang West Road, Guangzhou 510275, PR China.
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6490-3. doi: 10.1016/j.bmcl.2008.10.056. Epub 2008 Oct 17.
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.
合成了一系列的螺旋藻类似物，并将其作为酪氨酸酶抑制剂进行评估。结果表明，一些化合物具有比熊果苷（IC(50) 7.3 mM）更强的抑制活性。特别是，在糖部分带有4,6-O-亚苄基取代基的化合物1c被发现是最有效的抑制剂，IC(50)值为0.052 mM。通过Lineweaver-Burk图分析的抑制动力学表明，螺旋藻类似物是竞争性抑制剂。圆二色光谱表明，这些化合物在结合时会诱导蘑菇酪氨酸酶的构象变化。
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