Wang Yunxiao, Wang Jifeng, Wang Shunxin, Cao Zengyuan, Gu Dongyu, Wang Yi, Tian Jing, Yang Yi
School of Biological Engineering, Dalian Polytechnic University, 1 Qinggongyuan, Dalian 116034, China.
College of Marine Science and Environment, Dalian Ocean University, 52 Heishijiao Street, Dalian 116023, China.
Food Funct. 2021 Nov 1;12(21):10806-10812. doi: 10.1039/d1fo01542g.
As a popular vegetable, has a wide range of bioactivities including lipase inhibitory activity. In the present study, an efficient and rapid method using a ligand-enzyme complex was established for screening of an active compound against lipase from . The ethyl acetate extract of showed good lipase inhibitory activity. After incubation with lipase, one of the compounds in the extract decreased significantly while comparing the HPLC chromatograms before and after incubation, which indicated that it may be the active compound bound to lipase. Then, the compound was isolated using a Sephadex LH-20 column and identified as 1,2,3,4,6-penta--galloyl-β-D-glucose. The activity test showed that the compound had good inhibitory activity against lipase, and its IC value was 118.8 ± 1.53 μg mL. The kinetic experiments indicated that 1,2,3,4,6-penta--galloyl-β-D-glucose inhibited lipase through mixed competitive and non-competitive inhibitions. Further docking results showed that the target compound could bind to the active site of lipase stably through seven hydrogen bonds, resulting in a docking energy of -8.31 kcal mol. The proposed method can not only screen the lipase inhibitors from quickly and effectively, but also provide an effective way for the rapid screening of active substances in natural food and plants.
作为一种常见蔬菜，[具体蔬菜名称未给出]具有广泛的生物活性，包括脂肪酶抑制活性。在本研究中，建立了一种使用配体 - 酶复合物的高效快速方法，用于筛选来自[具体来源未给出]的抗脂肪酶活性化合物。[具体蔬菜名称未给出]的乙酸乙酯提取物表现出良好的脂肪酶抑制活性。与脂肪酶孵育后，比较孵育前后的高效液相色谱图，提取物中的一种化合物显著减少，这表明它可能是与脂肪酶结合的活性化合物。然后，使用葡聚糖凝胶LH - 20柱分离该化合物，并鉴定为1,2,3,4,6 - 五 - [具体基团未给出] - 没食子酰基 - β - D - 葡萄糖。活性测试表明该化合物对脂肪酶具有良好的抑制活性，其IC值为118.8±1.53μg/mL。动力学实验表明，1,2,3,4,6 - 五 - [具体基团未给出] - 没食子酰基 - β - D - 葡萄糖通过混合竞争和非竞争抑制作用抑制脂肪酶。进一步的对接结果表明，目标化合物可通过七个氢键稳定地结合到脂肪酶的活性位点，对接能量为 - 8.31 kcal/mol。所提出的方法不仅可以快速有效地从[具体来源未给出]中筛选脂肪酶抑制剂，还为快速筛选天然食品和植物中的活性物质提供了一种有效途径。
