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投稿时间：2018-03-13
投稿时间：2018-03-13
中文摘要: 利用紫外、荧光光谱法和圆二色谱法结合分子对接技术探讨芹菜素对黄嘌呤氧化酶（xanthine oxidase，XO）催化活性（底物黄嘌呤）抑制作用机理。结果表明：芹菜素具有明显可逆的混合竞争型抑制XO作用，其半数抑制浓度（IC50）和抑制常数（Ki）分别为8.63、2.35 μmol/L；芹菜素主要通过疏水作用力与XO形成基态复合物，并引起XO二级结构（α-螺旋含量增加）发生改变；分子对接结果显示芹菜素通过结合到XO的活性空腔，并与周围氨基酸相互作用，占据疏水通道，从而抑制XO活性。
Abstract:The inhibition mechanism of apigenin on xanthine oxidase （XO）was researched by using the methods of ultraviolet spectrum，fluorescence spectroscopy and circular dichroism，combining with molecular simulation technology.The results showed that apigenin was a good reversible XO inhibitor in a competetive way with the half inhibition concentration（IC50）and an inhibition constant（Ki）of 8.63 μmol/L and 2.35 μmol/L，respectively.Apigenin formed ground state complex with XO through hydrophobic force which induced some comformational changes of XO （the content of α-helix increased）.The result of molecular docking confirmed that apigenin bound to the active cavity of XO，interacting with some amino acid residues，plugging the cavity and finally inhibiting the activity of XO.
文章编号：201821011 中图分类号： 文献标志码：
基金项目:
| Author Name | Affiliation |
| YE Su-mei | Shanghai Aurora Vocational College，Shanghai 201908，China |
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