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卫矛属植物中具有α-葡萄糖苷酶抑制活性的三萜类化合物。

α-Glucosidase inhibitory triterpenoids from Euonymus fortunei.

机构信息

Department of Natural Medicine and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266071, PR China.

Department of Natural Medicine and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266071, PR China.

出版信息

Bioorg Chem. 2021 Jun;111:104980. doi: 10.1016/j.bioorg.2021.104980. Epub 2021 May 11.

Abstract

α-Glucosidase plays an important role in catalyzing the hydrolytic cleavage of disaccharides into monosaccharides. In this study, a phytochemical investigation of the potential α-glucosidase inhibitory fraction from the aerial parts of Euonymus fortunei led to the isolation and identification of two new tetracyclic triterpenoids, fortunenones A and B (1-2), together with 11 known triterpenoids (3-13). Fortunenones A and B are rare C triterpenoids possessing a 24,24-dimethyl group. The partial isolated compounds were evaluated their effects on α-glucosidase, of which echinochlorin D (5), lupenone (7), wilforlide B (12), and wilforlide A (13) exhibited remarkable inhibitory effects with the half inhibitory concentration ranged from 207.2 × 10 M to 388.3 × 10 M compared with the positive control, acarbose. An enzyme kinetics analysis by Lineweaver-Burk plots revealed that the inhibition types of the four active compounds were all mixed inhibition. Molecular docking further revealed that hydrophobic interactions and hydrogen bonds play an important role in the inhibition of α-glucosidase activity. Our results demonstrate the potential of E. fortunei extract and its constituents to inhibit α-glucosidase.

摘要

α-葡萄糖苷酶在催化二糖水解为单糖方面起着重要作用。在这项研究中,对卫矛科植物南蛇藤地上部分具有潜在α-葡萄糖苷酶抑制作用的化学成分进行了研究,分离并鉴定了两种新的四环三萜福酮 A 和 B(1-2),以及 11 种已知的三萜(3-13)。福酮 A 和 B 是罕见的 C 型三萜,具有 24,24-二甲基。对部分分离得到的化合物进行了α-葡萄糖苷酶抑制活性评价,其中,echinochlorin D(5)、羽扇豆酮(7)、wilforlide B(12)和 wilforlide A(13)具有显著的抑制作用,半抑制浓度范围为 207.2×10^-6 M 至 388.3×10^-6 M,与阳性对照阿卡波糖相当。Lineweaver-Burk 作图的酶动力学分析表明,四种活性化合物的抑制类型均为混合抑制。分子对接进一步表明,疏水相互作用和氢键在抑制α-葡萄糖苷酶活性中起着重要作用。我们的研究结果表明,南蛇藤提取物及其成分具有抑制α-葡萄糖苷酶的潜力。

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