中国免疫学杂志2017，Vol.33Issue(7)：1000-1004,5.DOI:10.3969/j.issn.1000-484X.2017.07.009
多酚氧化酶抑制剂高良姜素抗黑色素瘤机制研究
Inhibitory effect of galangin on polyphenol oxidase and study of mechanism
摘要
Abstract
Objective:To investigated the activity inhibition and inhibitory type of polyphenol oxidase (PPO) induced by galangin and the interaction mechanism of galangin with polyphenol oxidase was preliminarily indicated,and prove the related mechanism of galangin on proliferation of on human melanoma A375 cells.Methods: The activity inhibition and inhibitory type of PPO induced by galangin were investigated by spectrophotometric method,and interation mechanism of galangin with PPO was preliminarily indicated by fluorescence quenching and molecular docking,and chelating copper ions with the inhibitory mechanism of galangin on polyphenol oxidase was measured.Results: Galangin was a competitive inhibitor,the IC50 and Ki on PPO were obtained to be (47.86±3.33) and (24.83±1.45)μmol/L,respectively.Fluorescence spectrum indicated the fluorescence of PPO was quenched effectively by galangin and the binding constant Ka was obtained to be (4.67±0.43)×104 L/mol.Chelating copper ions and molecular simulation further showed that galangin was combined with active center of copper ions,and formed hydrogen bonds with catalytic site His259.Luteolin could induce the apoptosis of A375 cells significantly,and the tyrosinase activity and melanin synthesis were decreased.Conclusion: Galangin as a competitive polyphenol oxidase inhibitor and reduced the activity of polyphenol oxidase.which provides the theoretical basis for the clinical anti skin cancer.关键词
高良姜素/多酚氧化酶/抑制作用/荧光光谱/螯合金属铜离子/人恶性黑色素瘤细胞株A375/凋亡Key words
Galangin/Polyphenol oxidase/Inhibitory effect/Fluorescence spectrum/Chelating copper ions/Human melanoma A375 cells/Apoptosis分类
医药卫生引用本文复制引用
杨镓宁,邓菲,潘宁..多酚氧化酶抑制剂高良姜素抗黑色素瘤机制研究[J].中国免疫学杂志,2017,33(7):1000-1004,5.基金项目
本文为四川省卫计委科研课题(No.140084). （No.140084）
