八月瓜种子的化学成分及其α-葡萄糖苷酶抑制活性

Chemical Composition and α-Glucosidase Inhibitory Activity of the Seeds of Akebia trifoliata

摘要:

该研究探讨了药食两用八月瓜种子［Akebia trifoliata (Thunb.) Koidz. Seeds］的化学成分及其α-葡萄糖苷酶抑制活性。将八月瓜种子经水和95%乙醇提取，不同极性溶剂萃取后，分别测试各部位的α-葡萄糖苷酶抑制活性，发现95%乙醇提取物的正丁醇部位为α-葡萄糖苷酶抑制活性部位（IC50为18.16 μg/mL），采用硅胶柱色谱、HP20SS柱色谱和半制备HPLC等手段对正丁醇部位进行分离纯化。从八月瓜种子正丁醇部位中分离得到14个化合物，通过与文献波谱数据对比，分别鉴定为：Hederacholichiside F (1)、Saponin E (2)、Mutong Sponin B (3)、Saponin PJ1 (4)、Saponin PH (5)、Yuzhizioside Ⅳ (6)、Akebia Saponin D (7)、Saponin B (8)、HN-Saponin F (9)、Yuzhizioside Ⅳ a (10)、Icariside D (11)、Phenethyl rutinoside (12)、Calceolariolside B (13) 和Isoquercitrin (14)。化合物9、10、11、12、14为首次从八月瓜中分离得到。化合物2、7、10、14对α-葡萄糖苷酶具有一定程度的抑制活性，其IC50分别为17.48、35.62、35.79、44.78 μg/mL。化合物6、13的抑制活性最为显著，其IC50分别为4.27、2.95 μg/mL，活性优于阳性药阿卡波糖（IC50为6.02 μg/mL）。

Abstract:

In this study, the chemical constituents and α-glucosidase inhibitory activity of medicine and food dualuse Akebia trifoliata (Thunb.) Koidz. Seeds were studied. The seeds of Akebia trifoliata were extracted with water and 95% ethanol, then extracted with different polar solvents. The α-glucosidase inhibitory activity of each of these extract fractions was determined. It was found that the n-butanol fraction of the 95% ethanol extract could inhibit the active site of the α-glucosidase (IC50 was 18.16 μg/mL). The n-butanol fraction was separated and purified by silica gel column chromatography, HP20SS column chromatography and semi-preparative HPLC. Fourteen compounds were isolated from the n-butanol fraction of Akebia trifoliata seeds, and after the comparison with the spectral data in the literature, they were identified as Hederacholichiside F (1), Saponin E (2), Mutong Sponin B (3), Saponin PJ1 (4), Saponin PH (5), Yuzhiziosiside IV (6), Akebia Saponin D (7), Saponin B (8), HN-Saponin F (9), Yuzhizioside Ⅳa (10), Icariside D (11), Phenethyl rutinoside (12), Calceolariolside B (13) and Isoquercitrin (14). Compounds 9, 10, 11, 12 and 14 were isolated from Akebia trifoliata for the first time. Compounds 2, 7, 10 and 14 had certain inhibitory activities against α-glucosidase with IC50 values being 17.48, 35.62, 35.79 and 44.78 μg/mL, respectively. Compounds 6 and 13 showed the most significant inhibitory activities, with IC50 values being 4.27 μg/mL and 2.95 μg/mL, respectively, which were superior to that of acarbose (IC50: 6.02 μg/mL).