从 L. 中分离出作为 α-葡萄糖苷酶抑制剂的异香豆素和类黄酮
Isolation of Isocoumarins and Flavonoids as α-Glucosidase Inhibitors from L.
机构信息
Division of Applied Biosciences, College of Agriculture & Life Sciences Kyungpook National University, Daegu 41566, Korea.
出版信息
Molecules. 2020 May 31;25(11):2572. doi: 10.3390/molecules25112572.
L. (AP) showed potent α-glucosidase inhibitory (AGI) activity, but it is uncertain what phytochemicals play a key factor. The phytochemical study of AP based on AGI activity led to the isolation of four isocoumarins; agrimonolide (), agrimonolide-6--β-d-glucopyranoside (), desmethylagrimonolide (), desmethylagrimonolide-6--β-d-glucopyranoside (), and four flavonoids; luteolin (), quercetin (), vitexin (), and isovitexin (). The four isocoumarins were isolated as α-glucosidase inhibitors for the first time. Isocoumarins, compound 1 (agrimonolide) and 3 (desmethylagrimonolide) showed strong α-glucosidase inhibitory activities with IC values of 24.2 and 37.4 µM, respectively. Meanwhile, isocoumarin and flavonoid glycosides showed weak AGI activity. In the kinetic analysis, isocoumarins, compounds 1 and 3 showed non-competitive inhibition, whereas flavonoid, compound showed competitive inhibition.
L.（AP）表现出很强的α-葡萄糖苷酶抑制（AGI）活性，但哪种植物化学物质起关键作用还不确定。基于 AGI 活性的 AP 的植物化学研究导致分离出四种异香豆素；agrimonolide ()、agrimonolide-6--β-d-吡喃葡萄糖苷 ()、desmethylagrimonolide ()、desmethylagrimonolide-6--β-d-吡喃葡萄糖苷 ()，以及四种类黄酮；木犀草素 ()、槲皮素 ()、牡荆素 () 和异牡荆素 ()。这四种异香豆素首次被分离为α-葡萄糖苷酶抑制剂。异香豆素化合物 1（agrimonolide）和 3（desmethylagrimonolide）表现出很强的α-葡萄糖苷酶抑制活性，IC 值分别为 24.2 和 37.4 µM。同时，异香豆素和类黄酮糖苷表现出较弱的 AGI 活性。在动力学分析中，异香豆素化合物 1 和 3 表现出非竞争性抑制，而类黄酮化合物 表现出竞争性抑制。
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