食品科学2025，Vol.46Issue(2)：38-49,12.DOI:10.7506/spkx1002-6630-20240705-061
汉麻籽多肽靶向抑制胰脂肪酶/胆固醇酯酶的分子作用机制
Molecular Mechanism of Targeted Inhibition of Pancreatic Lipase and Cholesterol Esterase by Hempseed Peptides
摘要
Abstract
In this study,we systematically investigated the regulatory effects of two hempseed peptides(APAM and RLPA)on pancreatic lipase(PL)and cholesterol esterase(CE)activities and the molecular binding mechanism using enzyme kinetics,synergistic inhibition,fluorescence spectroscopy,isothermal titration calorimetry and molecular docking.The results showed that RLPA had stronger inhibitory activity on PL and CE with half maximal inhibitory concentration(IC50)values of(79.62±3.20)and(301.27±14.40)μmol/L,respectively.Kinetic analysis indicated that the inhibition mechanism of APAM on the two enzymes was competitive inhibition,whereas RLPA was a mixed-type inhibitor.Both APAM and RLPA synergistically inhibited PL and CE with orlistat at low concentrations,but the synergistic effect was weakened or even antagonized at high concentrations.Fluorescence spectroscopy results showed that both peptides could produce static quenching by binding to PL and CE,which changed the hydrophobic environment of aliphatic amino acids in the enzymes.Isothermal titration calorimetry demonstrated that the binding process between the peptides and the enzymes was spontaneous and exothermic,which was achieved mainly through hydrogen bonding and electrostatic interaction.Further analysis using molecular docking simulations showed that hydrogen bonding,salt bridges,and cation-π interactions played crucial roles in peptide-enzyme binding.This study enriches our understanding of the interaction mechanism of peptides with PL and CE,and provides a scientific basis for the development of functional foods based on hempseed protein.关键词
脂质消化酶/抑制机制/荧光光谱/等温滴定量热法/分子模拟Key words
lipid-digesting enzymes/inhibition mechanism/fluorescence spectroscopy/isothermal titration calorimetry/molecular modeling分类
轻工业引用本文复制引用
尹浩,朱将雄,赵海云,钟宇,王丹凤,邓云..汉麻籽多肽靶向抑制胰脂肪酶/胆固醇酯酶的分子作用机制[J].食品科学,2025,46(2):38-49,12.基金项目
云南省基础研究计划项目(202301AS070014) （202301AS070014）
"十四五"国家重点研发计划重点专项(2023YFF1104302-1) （2023YFF1104302-1）
