Cherigo Lilia, Liao-Luo Javier, Fernández Juan, Martínez-Luis Sergio
Departamento de Química Orgánica, Facultad de Ciencias Naturales, Exactas y Tecnología, Universidad de Panamá, Ciudad de Panamá P.O. Box 3366, Panama.
Centro de Biodiversidad y Descubrimiento de Drogas, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Edificio 208, Ciudad del Saber, Apartado 0843-01103, Panama.
Pharmaceuticals (Basel). 2024 Jul 4;17(7):890. doi: 10.3390/ph17070890.
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 (Triana ex Hemsl.) Ducke, an understudied mangrove species. Through bioassay-guided fractionation of the crude extract, we isolated seven active compounds identified as lupenone (), lupeol (), α-amyrin (), β-amyrin (), palmitic acid (), sitosterol (), and stigmasterol (). Compound structures were determined using spectroscopic analyses, including APCI-HR-MS and NMR. Compounds displayed concentration-dependent inhibition of the alpha-glucosidase enzyme, with IC 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 (IC 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 active fractions revealed the presence of 64 compounds, shedding new light on the plant's chemical composition. These findings suggest that holds promise as a valuable botanical source for developing compounds for managing blood sugar levels in individuals with diabetes.
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。虽然红树林植物长期以来一直被用于传统医学,但仍有一些未被研究的物种,其潜在的药用价值尚不清楚。本研究旨在从一种研究较少的红树林物种——(Triana ex Hemsl.)Ducke中提取生物活性化合物。通过对粗提物进行生物测定指导的分级分离,我们分离出了七种活性化合物,分别鉴定为羽扇豆酮()、羽扇豆醇()、α-香树脂醇()、β-香树脂醇()、棕榈酸()、谷甾醇()和豆甾醇()。使用包括APCI-HR-MS和NMR在内的光谱分析确定了化合物的结构。这些化合物对α-葡萄糖苷酶表现出浓度依赖性抑制作用,IC值分别为0.72、1.05、2.13、1.22、240.20、18.70和163.10μM。它们的抑制活性超过了阳性对照阿卡波糖(IC 241.6μM)。动力学分析表明,所有化合物均作为竞争性抑制剂起作用。对接分析预测,所有三萜类化合物在人肠道α-葡萄糖苷酶(PDB:3TOP)中与阿卡波糖结合在同一位置。对活性馏分的补充代谢组学分析揭示了64种化合物的存在,为该植物的化学成分提供了新的线索。这些发现表明,该物种有望成为开发用于控制糖尿病患者血糖水平化合物的宝贵植物来源。