数字农科院2.0

Discovery, α-Glucosidase Inhibitory Activity, and Structural Optimization of the Alkaloids from Vanderbylia robiniophila SY636

文献类型： 外文期刊

作者： Yu, Guihong;Zhang, Jianing;Shang, Zhaomeng;Sun, Peng;Mo, Xuhua;Peng, Jixing;Yang, Song;Tan, Lingling

作者机构：

期刊名称： JOURNAL OF NATURAL PRODUCTS

ISSN： 0163-3864

年卷期： 2026 年

页码：

收录情况： SCIE（2025版）

摘要： alpha-Glucosidase inhibitory activity-guided isolation led to the discovery of ten alkaloids from the medicinal mushroom Vanderbylia robiniophila SY636, including six new compounds ((+)-1a, (-)-1b, (+)-2a, (-)-2b, 3, and (+)-4a) and four newly reported natural products ((-)-4b and 5-7). Compounds (+)-1a, (-)-1b, (+)-2a, and (-)-2b possess a unique lactam-furan ring system, whereas 3 features a rare tetrahydrobenzo[c]oxepine-furan ring system. (+)-1a, (-)-1b, (+)-4a, and (-)-4b exhibited notable alpha-glucosidase inhibitory activities, with IC50 values of 160-330 mu M (acarbose as the positive control, IC50 = 660 mu M). Guided by docking results of bioactive compounds with alpha-glucosidase, derivatives D1-D28 were designed and synthesized, among which D15 and D19 exhibited stronger activities (IC50 = 28 and 130 mu M). Molecular docking and kinetic studies suggested that D15 and D19 interact with alpha-glucosidase at a single binding site, exhibiting an uncompetitive or mixed type of inhibition mechanism. D19 also exhibited notable antioxidant activity (IC50 = 35 mu M), comparable to l-ascorbic acid, suggesting its dual role in combating the development of diabetes. This study provides a foundation for the development of natural medicines from V. robiniophila and offers valuable guidance for future structural optimization toward the discovery of more potent and safer antidiabetic agents.

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