Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
College of Biological Science and Engineering, Xiamen University, Xiamen, China.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):897-905. doi: 10.1080/14756366.2020.1734798.
Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a 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 (IC) = 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 lipopeptides would have great potential to act as lipase inhibitors.
脂肽已被报道具有抗肥胖作用。在本研究中，我们获得了一株能够同时产生伊枯草菌素、丰原素和表面活性剂的菌株 FJAT-52631。结果表明，FJAT-52631 粗脂肽、纯化丰原素、伊枯草菌素和表面活性剂标准品均表现出较强的脂肪酶抑制活性，呈剂量依赖性（半抑制浓度（IC）分别为 0.011、0.005、0.056 和 0.005mg/mL）。此外，丰原素和表面活性剂的活性与奥利司他相当，但伊枯草菌素没有。结果表明，脂肽的抑制机制和类型为可逆和竞争型。荧光分析显示，脂肪酶的猝灭机制为静态，并且推断出脂肽与脂肪酶之间只有一个结合位点。对接分析表明，丰原素和表面活性剂可以直接与脂肪酶的活性氨基酸残基（Ser 或 Asp）相互作用，但与伊枯草菌素没有相互作用。我们的工作表明，这些脂肽可能具有作为脂肪酶抑制剂的巨大潜力。
