密花香薷体外对代谢综合征相关酶抑制活性研究

Inhibitory Activity of Elsholtzia densa on Metabolic Syndrome Related Enzymes in Vitro

目的:探讨密花香薷粗提物体外对酶抑制的作用,初步阐明其对代谢综合征的药效物质基础。方法:体外测定密花香薷粗提物及其不同萃取部位对多种酶活性的抑制率,与阳性对照比较IC50值,高效液相色谱法测定密花香薷中主成分含量。分子对接计算主成分与酶抑制作用相关目标基因的结合能。结果:密花香薷粗提物对α-淀粉酶、黄嘌呤氧化酶、胰脂肪酶、乙酰胆碱酯酶均有一定的抑制作用,IC_(50)值分别为0.199 mg/mL、0.254 mg/mL、0.258mg/mL、0.057 mg/mL。密花香薷乙酸乙酯部分对酶抑制作用最强,其中含量最高为绿原酸57.40 mg/g和槲皮素37.51 mg/g。分子对接发现绿原酸、槲皮素与以上代谢综合征酶抑制作用相关目标基因结合作用良好。结论:密花香薷粗提物对代谢综合征相关多种酶有一定的抑制活性,初步认为密花香薷治疗代谢综合征的药效物质基础可能为绿原酸与槲皮素。

Objective:The effect of crude extract of Elsholtzia densa was discussed on enzyme inhibitors in vitro,and the material basis of its effect on metabolic syndrome was preliminarily elucidated.Methods:The inhibitory rate of Elsholtzia densa extract and its different extraction parts on various enzyme activi‑ties was determined in vitro.IC50 value was compared with positive control.The content of principal com‑ponent was determined by high performance liquid chromatography.The binding energies of target genes related to principal component and enzyme inhibition were calculated by molecular docking.Results:The crude extract of Elsholtzia densa showed some inhibitory effects on xanthine oxidase,α-amylase,pancre‑atic lipase and acetylcholinesterase with IC_(50) values of 0.199 mg/mL,0.254 mg/mL,0.258 mg/mL and 0.057 mg/mL,respectively.The ethyl acetate part of Elsholtzia densa had the strongest inhibitory effect on enzyme,and the highest content of chlorogenic acid was 57.40 mg/g and quercetin was 37.51 mg/g.Molecular docking showed that chlorogenic acid and quercetin had good binding effect on the target genes related to the above metabolic syndrome enzyme inhibition.Conclusion:Elsholtzia densa had certain inhib‑itory activity on various enzymes related to metabolic syndrome.It was initially thought that chlorogenic acid and quercetin might be the basis of its pharmacodynamic substance in the treatment of metabolic syndrome.