Zhou Qinru, Lei Xinyu, Niu Jing, Chen Yan, Shen Xiangchun, Zhang Nenling
The State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, People's Republic of China.
High Efficacy Application of Natural Medicinal Resources Engineering Center of Guizhou Province, High Educational Key Laboratory of Guizhou Province for Natural Medicinal Pharmacology and Drug Ability, Key Laboratory of Optimal Utilization of Natural Medicinal Resources, Guizhou Medical University, Guiyang, People's Republic of China.
Nat Prod Res. 2023 Oct-Nov;37(19):3267-3275. doi: 10.1080/14786419.2022.2068544. Epub 2022 Apr 25.
From the petroleum ether and ethyl acetate portions of the 95% ethanol extract of Bur., a new hemiacetal chromone racemate, named (±)-ficunomone (), together with twenty-two known flavonoids (-) were isolated. The new structure was elucidated by NMR, HRESIMS, and X-ray single-crystal diffraction analysis, and the known structures were determined by comparison of spectroscopic data with those reported from literatures. All the compounds were assayed for their inhibitory activities against yeast -glucosidase, seven flavonoids could inhibit -glucosidase, among which compounds and exhibited the highest inhibitory activity, with IC values at 5.12 ± 0.10 and 3.43 ± 0.15 μM respectively. Preliminary structure and relationship activity of all the compounds was analysed. Kinetic analysis of compounds and indicated that they are both uncompetitive inhibitors. Molecular docking studies revealed that they bound to amino acid residues of the -glucosidase activity pocket.
从Bur.的95%乙醇提取物的石油醚和乙酸乙酯部分中,分离出一种新的半缩醛色酮外消旋体,命名为(±)-ficunomone (),以及22种已知的黄酮类化合物(-)。通过核磁共振、高分辨电喷雾电离质谱和X射线单晶衍射分析阐明了新结构,并通过将光谱数据与文献报道的数据进行比较确定了已知结构。对所有化合物进行了抗酵母α-葡萄糖苷酶抑制活性测定,7种黄酮类化合物可抑制α-葡萄糖苷酶,其中化合物和表现出最高的抑制活性,IC值分别为5.12±0.10和3.43±0.15μM。分析了所有化合物的初步结构与活性关系。化合物和的动力学分析表明它们都是非竞争性抑制剂。分子对接研究表明它们与α-葡萄糖苷酶活性口袋的氨基酸残基结合。