Key Laboratory of Tropical Plant Resource and Sustainable Use, Xishuangbanna Tropical Botanical Garden, Chinese Academy of Sciences, Kunming 650223, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Molecules. 2022 May 24;27(11):3381. doi: 10.3390/molecules27113381.
Our research focused on the hypoglycemic capability and the possible mechanisms of extract and fractions from Polygoni Avicularis Herba (PAH) based on α-glucosidase, α-amylase inhibition assays, glucose uptake experiment, HPLC-MS analysis, and molecular docking experiment. In addition, DPPH, ABTS, and FRAP assays were used for determining the antioxidant capability. The results of total flavonoids and phenolics contents showed that ethyl acetate fraction (EAF) possessed the highest flavonoids and phenolics with values of 159.7 ± 2.5 mg rutin equivalents/g and 107.6 ± 2.0 mg galic acid equivalents/g, respectively. The results of in vitro hypoglycemic activity showed that all samples had effective α-glucosidase inhibition capacities, and EAF possessed the best inhibitory effect with IC50 value of 1.58 ± 0.24 μg/mL. In addition, n-butanol fraction (NBF) significantly promoted the glucose uptake rate of 3T3-L1 adipocytes. HPLC-MS analysis and molecular docking results proved the interactions between candidates and α-glucosidase. The results of antioxidation capacities showed that EAF possessed the best antioxidation abilities with DPPH, ABTS, and FRAP. In summary, the hypoglycemic activity of PAH might be related to the inhibition of α-glucosidase (EAF > PEF > NBF) and the promotion of glucose uptake in 3T3-L1 adipocytes (NBF). Simultaneously, the antioxidation capacity of PAH might be related to the abundant contents of flavonoids and other phenolics (EAF > PEF > NBF).
我们的研究集中在基于α-葡萄糖苷酶、α-淀粉酶抑制试验、葡萄糖摄取试验、HPLC-MS 分析和分子对接试验的虎杖提取物和馏分的降血糖能力及其可能机制。此外,还使用了 DPPH、ABTS 和 FRAP 测定法来测定抗氧化能力。总黄酮和总酚含量的结果表明,乙酸乙酯馏分(EAF)具有最高的黄酮类和酚类,其值分别为 159.7 ± 2.5 mg 芦丁当量/g 和 107.6 ± 2.0 mg 没食子酸当量/g。体外降血糖活性的结果表明,所有样品均具有有效的α-葡萄糖苷酶抑制能力,EAF 的抑制效果最好,IC50 值为 1.58 ± 0.24 μg/mL。此外,正丁醇馏分(NBF)显著促进了 3T3-L1 脂肪细胞的葡萄糖摄取率。HPLC-MS 分析和分子对接结果证明了候选物与α-葡萄糖苷酶之间的相互作用。抗氧化能力的结果表明,EAF 具有最好的抗氧化能力,DPPH、ABTS 和 FRAP 的抗氧化能力最强。综上所述,虎杖的降血糖活性可能与α-葡萄糖苷酶的抑制(EAF>PEF>NBF)和 3T3-L1 脂肪细胞中葡萄糖的摄取促进(NBF)有关。同时,虎杖的抗氧化能力可能与丰富的黄酮类和其他酚类物质有关(EAF>PEF>NBF)。