Department of Oriental Medicine Biotechnology, College of Life Sciences, Kyung Hee University Global Campus, Yongin-si 17104, Korea.
Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai 90112, Thailand.
Nutrients. 2022 Aug 9;14(16):3249. doi: 10.3390/nu14163249.
Metabolic syndrome has become a global health care problem since it is rapidly increasing worldwide. The search for alternative natural supplements may have potential benefits for obesity and diabetes patients. fruit extract and its oligosaccharides, including gentiobiose, melibiose, and raffinose, were examined for their anti-insulin resistance and obesity-preventing effect in zebrafish larvae. The results show that oligosaccharides improved insulin resistance and high-fat-diet-induced obesity in zebrafish larvae, evidenced by enhanced β-cell recovery, decreased abdominal size, and reduced the lipid accumulation. The mechanism of the oligosaccharides, molecular docking, and enzyme activities of PTP1B were investigated. Three of the oligosaccharides had a binding interaction with the catalytic active sites of PTP1B, but did not show inhibitory effects in an enzyme assay. The catalytic residues of PTP1B were typically conserved and the cellular penetration of the cell membrane was necessary for the inhibitors. The results of the mechanism of action study indicate that fruit extract and its oligosaccharides affected gene expression changes in inflammation- (, , and ), lipogenesis- ( and ), and lipid-lowering ()-related genes. Therefore, fruit extract and its oligosaccharides may have a great potential for applications in metabolic syndrome drug development and dietary supplements.
代谢综合征在全球范围内迅速增加,已成为一个全球性的医疗保健问题。寻找替代天然补充剂可能对肥胖和糖尿病患者有潜在的益处。水果提取物及其寡糖,包括龙胆二糖、棉子糖和水苏糖,已在斑马鱼幼虫中被检查其抗胰岛素抵抗和预防肥胖的作用。结果表明,寡糖可改善胰岛素抵抗和高脂肪饮食诱导的肥胖,这表现在增强β细胞恢复、减小腹部大小和减少脂肪积累。研究了寡糖的作用机制、分子对接和 PTP1B 的酶活性。三种寡糖与 PTP1B 的催化活性部位具有结合相互作用,但在酶测定中没有显示抑制作用。PTP1B 的催化残基通常是保守的,抑制剂需要穿透细胞膜。作用机制研究的结果表明,水果提取物及其寡糖影响与炎症相关的基因表达变化(、和)、脂肪生成(和)和降低血脂()相关基因。因此,水果提取物及其寡糖可能在代谢综合征药物开发和膳食补充剂中有很大的应用潜力。