The demand for plant‐derived antidiabetic nutraceuticals is increasing. In this study, the effects of three common caffeoylquinic acids (CQAs) (chlorogenic acid, isochlorogenic acid A, and cynarin) on α‐glucosidase activity and glucose consumption in HepG2 cells were systematically compared. Their α‐glucosidase inhibitory activities followed the order of isochlorogenic acid A > chlorogenic acid > cynarin. The fluorescence analysis indicated that they exerted the inhibitory role by forming the complex with α‐glucosidase at the molar ratio of 1:1. Isochlorogenic acid A possessed the highest binding capacity, followed by chlorogenic acid and cynarin. The effect of caffeoyl group distribution on the α‐glucosidase inhibitory activity was clarified by the molecular docking results. In the HepG2 cells, isochlorogenic acid A also showed the best glucose consumption with negligible cytotoxicity, which might be related to its reactive oxygen species scavenging capacity in cells. Our results confirm its potential application as the antidiabetic nutraceutical.

中文翻译：

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三种常见的咖啡酰奎尼酸作为潜在的降糖营养品：HepG2细胞中α-葡萄糖苷酶抑制活性和葡萄糖消耗的评估。

对源自植物的抗糖尿病营养品的需求正在增加。在这项研究中，系统地比较了三种常见的咖啡酰奎尼酸（CQAs）（绿原酸，异绿原酸A和cynarin）对HepG2细胞中α-葡萄糖苷酶活性和葡萄糖消耗的影响。它们的α-葡萄糖苷酶抑制活性遵循异绿原酸A>绿原酸> cynarin的顺序。荧光分析表明，它们通过与α-葡萄糖苷酶以1：1的摩尔比形成复合物而发挥抑制作用。异绿原酸A具有最高的结合能力，其次是绿原酸和cynarin。分子对接结果明确了咖啡酰基分布对α-葡萄糖苷酶抑制活性的影响。在HepG2细胞中 异绿原酸A还显示出最佳的葡萄糖消耗，而细胞毒性可忽略不计，这可能与其在细胞中清除活性氧的能力有关。我们的结果证实了其作为抗糖尿病营养保健品的潜在应用。