摘要
本文主要探讨了2’,4’-二羟基-6’-甲氧基-3’,5’-二甲基查耳酮(2’,4’-dihydroxy-6’-methoxy-3’,5’-dimethylchalcone,DMC)对胰脂肪酶(Pancreatic Lipase,PL)的抑制作用及作用机理。以4-硝基苯丁酸酯为底物,采用对硝基苯酚法检测DMC对PL活性的影响,采用紫外光谱法、荧光光谱法以及分子对接法研究DMC与PL的相互作用。结果表明:DMC对PL有抑制作用,半数抑制浓度为50.01±3.56μmol/L,酶动力研究表明DMC是PL的竞争型抑制剂;光谱实验结果显示DMC的加入使PL发生了荧光猝灭,猝灭类型为动态猝灭;同步荧光及三维荧光实验表明DMC不会改变PL构象;热力学参数ΔG<0,两者的相互作用是自发进行,ΔH<0,ΔS<0,表明DMC与PL的相互作用力主要为氢键和范德华力;分子对接实验进一步验证了以上结果。由此可见,DMC具有作为PL抑制剂的潜能。
To investigate the inhibitory activity and interaction between DMC and pancreatic lipase,the p NPB was selected as the substrate to investigate the inhibition effect of DMC on pancreatic lipase.The interaction between DMC and pancreas lipase(PL)was also studied by ultraviolet spectroscopy,fluorescence spectroscopy and molecular docking.Pancreatic lipase inhibition assay showed that DMC exhibited competitive inhibitor against pancreatic lipase with IC50 value of 50.01±3.56μmol/L.The interaction mechanisms between DMC and pancreatic lipase were studied by fluorescence spectra.Experimental results showed that DMC quenched the fluorescence of pancreatic lipase mainly through dynamic quenching mode while increasing the DMC concentration.The synchronous fluorescence spectra and three-dimensional fluorescence spectroscopy indicated that pancreatic lipase microenvironment was not changed by DMC.The thermodynamic parametersΔG<0 showed that the combination was a spontaneous reaction,andΔH<0,ΔS<0 showed that the main forces were hydrogen bond or van der Waals force.Molecular docking studies further verified the above results.Thus,DMC has potential as a PL inhibitor.
作者
李婷
向灿辉
王文君
LI Ting;XIANG Can-hui;WANG Wen-jun(Department of Bioengineering,Zhuhai Campus of Zunyi Medical University,Zhuhai 519041,China)
出处
《食品工业科技》
CAS
北大核心
2020年第15期65-70,共6页
Science and Technology of Food Industry
基金
贵州省科技厅基金(黔科合J字(2014)2174)
贵州省科技计划项目(黔科合基础[2019]1345号)。
