阿莫酸萨考 A-K，来自Amomum tsao-ko 的二芳基庚烷类化合物及其对α-葡萄糖苷酶的抑制活性。
Amomutsaokols A-K, diarylheptanoids from Amomum tsao-ko and their α-glucosidase inhibitory activity.
机构信息
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming, 650201, PR China; University of Chinese Academy of Sciences, Beijing, 100049, PR China.
College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300071, PR China.
出版信息
Phytochemistry. 2020 Sep;177:112418. doi: 10.1016/j.phytochem.2020.112418. Epub 2020 Jul 15.
Eleven undescribed diarylheptanoids, amomutsaokols A‒K (1-11), together with 13 known ones (13-24), were isolated from the active fraction of the fruits of Amomum tsao-ko. The structures of the undescribed compounds were determined by extensive 1D and 2D NMR, HRESIMS and ECD calculations. Compounds 3-5, 7, 8, 12, 14 and 19 showed obviously α-glucosidase inhibitory activity with IC values ranging from 12.9 to 48.8 μM. An enzyme kinetic analysis indicated that compounds 8 and 9 were α-glucosidase noncompetitive inhibitors with K values of 18.5 and 213.0 μM, respectively. This study supported diarylheptanoids as the active constituents of A. tsao-ko with α-glucosidase inhibitory effects.
从益智果实的活性部位分离得到了 11 个未被描述的二芳基庚烷类化合物，分别命名为 amomutsaokols A-K（1-11），以及 13 个已知化合物（13-24）。通过广泛的 1D 和 2D NMR、HRESIMS 和 ECD 计算确定了未知化合物的结构。化合物 3-5、7、8、12、14 和 19 对 α-葡萄糖苷酶表现出明显的抑制活性，IC 值范围为 12.9-48.8 μM。酶动力学分析表明，化合物 8 和 9 是 α-葡萄糖苷酶的非竞争性抑制剂，K 值分别为 18.5 和 213.0 μM。本研究支持二芳基庚烷类化合物是具有α-葡萄糖苷酶抑制作用的益智果实的活性成分。
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