Abstract Inhibiting the activity of α-glucosidase and glycosylation of protein is an important way to treat diabetes mellitus and its complications. In this study, we investigated the anti-α-glucosidase activity, anti-glycation potential and structure of proanthocyanidins from fruit pulp of Clausena lansium (Lour.) Skeels. C. lansium fruit pulp proanthocyanidins showed a remarkable inhibition against α-glucosidase activity with IC50 vaule of 0.26 ± 0.01 μg/mL in a competitive manner, and quenched the fluorescence of α-glucosidase by forming proanthocyanidin-α-glucosidase complex. Furthermore, compared to positive agent aminoguanidine (AG), the proanthocyanidins were the more significant inhibitors of non-enzymatic glycation by strongly inhibiting the formation of α-dicarbonyl compounds and advanced glycation end products. In addition, the structure of the proanthocyanidins was characterized in detail. These compounds were mainly composed of prodelphinidins, and their gallates. The main extender units, gallocatechin epigallocatechin and their gallates, were critical factor of the strong anti-α-glucosidase and anti-glycation activity. Therefore, this study authenticated a efficient α-glucosidase inhibitors and antiglycation agents, which would contribute to the development of anti-diabetic drug.

中文翻译：

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来自 Clausena lansium (Lour.) Skeels 果肉的原花青素对 α-葡萄糖苷酶和非酶糖化的抑制潜力：活性和机制

摘要 抑制α-葡萄糖苷酶活性和蛋白质糖基化是治疗糖尿病及其并发症的重要途径。在这项研究中，我们研究了来自 Clausena lansium (Lour.) Skeels 果肉的原花青素的抗 α-葡萄糖苷酶活性、抗糖化潜力和结构。C. lansium 果肉原花青素对 α-葡萄糖苷酶活性有显着的抑制作用，IC50 值为 0.26 ± 0.01 μg/mL，以竞争方式，并通过形成原花青素-α-葡萄糖苷酶复合物来淬灭 α-葡萄糖苷酶的荧光。此外，与阳性试剂氨基胍 (AG) 相比，原花青素通过强烈抑制 α-二羰基化合物和晚期糖基化终产物的形成，是更重要的非酶糖化抑制剂。此外，详细表征了原花青素的结构。这些化合物主要由原飞燕草素及其没食子酸酯组成。主要的扩展单元，没食子儿茶素表没食子儿茶素及其没食子酸酯，是强抗α-葡萄糖苷酶和抗糖化活性的关键因素。因此，本研究验证了一种有效的α-葡萄糖苷酶抑制剂和抗糖化剂，这将有助于抗糖尿病药物的开发。