Strong inhibitory activities and action modes of lipopeptides on lipase

文献类型： 外文期刊

第一作者： Chen, Mei-chun

作者： Chen, Mei-chun;Wang, Jie-ping;Chen, Yan-ping;Zhu, Yu-jing;Liu, Bo;Liu, Tian-tian;Chen, Qing-xi

作者机构：

关键词： Lipopeptides; inhibitory activities; lipase; action mode

期刊名称：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY （ 影响因子：5.051； 五年影响因子：4.598 ）

ISSN： 1475-6366

年卷期： 2020 年 35 卷 1 期

页码：

收录情况： SCI

摘要： Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a Bacillus velezensis strain FJAT-52631 that could coproduce iturins, fengycins, and surfactins. Results showed that the FJAT-52631 crude lipopeptide, purified fengycin, iturin, and surfactin standards exhibited strong inhibition activities against lipase with dose-dependence manners (half maximal inhibitory concentration (IC50) = 0.011, 0.005, 0.056, and 0.005 mg/mL, respectively). Moreover, fengycin and surfactin had the comparable activities with orlistat, but iturin not. It was revealed that the inhibition mechanism and type of the lipopeptides were reversible and competitive. The quenching mechanism of lipase was static and only one binding site between lipase and lipopoeptide was inferred from the fluorescence analysis. The docking analysis displayed that fengycin and surfactin could directly interact with the active amino acid residues (Ser or Asp) of lipase, but not with iturin. Our work suggests that the B. velezensis lipopeptides would have great potential to act as lipase inhibitors.

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