从巴拿马红树植物 Mora oleifera (Triana ex Hemsl.) Ducke 中分离出α-葡萄糖苷酶抑制剂

Pharmaceuticals Pub Date : 2024-07-04 DOI:10.3390/ph17070890
Lilia Chérigo, Javier Liao-Luo, Juan Fernández, Sergio Martínez-Luis
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摘要

巴拿马拥有广阔的红树林区域,是美洲生物多样性最丰富的国家之一。虽然红树植物长期以来一直被用于传统医药,但仍有一些未被研究的物种,其潜在的医药用途仍不为人知。本研究旨在从 Mora oleifera (Triana ex Hemsl.) Ducke 这种未被充分研究的红树林物种中提取生物活性化合物。通过生物测定指导下的粗提取物分馏,我们分离出七种活性化合物,分别为羽扇豆酮(1)、羽扇豆醇(2)、α-amyrin(3)、β-amyrin(4)、棕榈酸(5)、西固醇(6)和豆甾醇(7)。化合物的结构是通过光谱分析(包括 APCI-HR-MS 和 NMR)确定的。化合物 1-7 对α-葡萄糖苷酶的抑制作用呈浓度依赖性,IC50 值分别为 0.72、1.05、2.13、1.22、240.20、18.70 和 163.10 µM。它们的抑制活性超过了阳性对照阿卡波糖(IC50 241.6 µM)。动力学分析表明,所有化合物都是竞争性抑制剂。对接分析预测,所有三萜类化合物都与阿卡波糖在人类肠道α-葡萄糖苷酶(PDB:3TOP)中的相同位点结合。对油橄榄果实活性馏分的补充代谢组学分析表明,油橄榄果实中含有 64 种化合物,为了解该植物的化学成分提供了新的线索。这些研究结果表明,M. oleifera有望成为开发用于控制糖尿病患者血糖水平的化合物的重要植物来源。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Isolation of Alpha-Glucosidase Inhibitors from the Panamanian Mangrove Plant Mora oleifera (Triana ex Hemsl.) Ducke
Panama boasts an expansive mangrove area and stands as one of the most biodiverse countries in America. While mangrove plants have long been utilized in traditional medicine, there are still unstudied species whose potential medicinal applications remain unknown. This study aimed to extract bioactive compounds from Mora oleifera (Triana ex Hemsl.) Ducke, an understudied mangrove species. Through bioassay-guided fractionation of the crude extract, we isolated seven active compounds identified as lupenone (1), lupeol (2), α-amyrin (3), β-amyrin (4), palmitic acid (5), sitosterol (6), and stigmasterol (7). Compound structures were determined using spectroscopic analyses, including APCI-HR-MS and NMR. Compounds 1–7 displayed concentration-dependent inhibition of the alpha-glucosidase enzyme, with IC50 values of 0.72, 1.05, 2.13, 1.22, 240.20, 18.70, and 163.10 µM, respectively. Their inhibitory activity surpassed acarbose, the positive control (IC50 241.6 µM). Kinetic analysis revealed that all compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bonded to the same site as acarbose in human intestinal alpha-glucosidase (PDB: 3TOP). A complementary metabolomic analysis of M. oleifera active fractions revealed the presence of 64 compounds, shedding new light on the plant’s chemical composition. These findings suggest that M. oleifera holds promise as a valuable botanical source for developing compounds for managing blood sugar levels in individuals with diabetes.
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