Since glucolipid metabolism disorders is often the mono-target therapy fails in managing blood glucose and lipid levels and the other complications, it is urgent and necessary to seek for the new potential drugs or functional food acting on multi-targets. The hypoglycemic and hypolipidemic dual activities of the root, stems and leaves of Desmodium caudatum, which is used for traditional Chinese medicine, was evaluated. Twelve extracts with different extraction conditions were prepared and extract 9 was find to exhibit potential inhibitory activities of fructose-1, 6-bisphosphatase (FBPase), α-glucosidase, and pancrelipase, as well as promote cellular glucose consumption and reduce cellular content of lipid. Five flavonoids were isolated and identified from extract 9, among which 8-prenylquercetin exhibited potent α-glucosidase (IC₅₀ = 4.38 μM) and FBPase (IC₅₀ = 3.62 μM) dual inhibitory activity, which were 75-fold higher than acarbose (IC₅₀ = 330.10 μM) and comparable with AMP (IC₅₀ = 2.92 μM). In addition, 8-prenylquercetin was able to promote glucose consumption and reduce lipid content. Besides, an efficient synthesis of the most potent 8-prenylquercetin was developed from inexpensive and commercially available rutin in 21% overall yield by 6 steps, which lay the foundation of preparation sufficient amount for follow-up study.

由于糖脂代谢紊乱往往是单靶点治疗无法控制血糖和血脂水平等并发症，因此寻找新的潜在药物或功能性食品作用于多靶点已迫在眉睫。大金钱草根茎叶的降糖降血脂双重作用, 用于中药, 进行了评价。制备了 12 种不同提取条件的提取物，发现提取物 9 对果糖 1、6-双磷酸酶 (FBPase)、α-葡萄糖苷酶和胰脂肪酶具有潜在的抑制活性，并促进细胞葡萄糖消耗并降低细胞内脂质含量. 从提取物 9 中分离鉴定出 5 种黄酮类化合物，其中 8-异戊二烯槲皮素表现出强效的 α-葡萄糖苷酶 (IC ₅₀  = 4.38 μM) 和 FBPase (IC ₅₀  = 3.62 μM) 双重抑制活性，比阿卡波糖 (IC) 高 75 倍。₅₀  = 330.10 μM)，与 AMP (IC ₅₀ = 2.92 微米）。此外，8-异戊二烯槲皮素能够促进葡萄糖消耗并降低脂质含量。此外，以廉价、市售的芦丁为原料，通过6个步骤高效合成了最有效的8-异戊二烯槲皮素，总产率为21%，为后续研究制备足量奠定了基础。