Biomedical Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Central 6th, 1-1-1 Higashi, Tsukuba, Ibaraki, 305-8566, Japan.
Artisan Labo, 3-29-7 Nohmidai, Kanazawa, Yokohama, Kanagawa, 236-0056, Japan.
Pharm Res. 2018 Dec 6;36(1):23. doi: 10.1007/s11095-018-2553-8.
Straight-chain polysaccharides have a greater potential of selectively adsorbing hydrophobic bile salts than resin-based bile salt sequesters because of ionic and hydrophobic interactions; hence, they may possess antidiabetic activity. The feasibility of using cationic polysaccharides made from euglenoid β-1,3-glucan (referred to as paramylon) as potential antidiabetic agents was examined by using in vitro and animal experiments.
Cationic straight-chain polysaccharides were synthesized from euglenoid polysaccharide and glycidyltrimethylammonium chloride. The effects of administration of the synthetic polysaccharide on metabolic syndrome-related indicators were examined in high-fat diet-induced obesity mice. The degree of adsorption of bile salts by the polysaccharides was evaluated using spectroscopic analysis.
Administration of the cationic paramylon derivatives significantly reduced body and mesenteric fat weight in high-fat diet-induced obesity mice. A noteworthy effect was that glucagon-like peptide-1 (GLP-1) secretion was approximately three times higher in diet-induced obesity mice receiving cationic paramylon derivatives than in those receiving cellulose as a control.
Our results indicate that these cationic paramylon derivatives are potential GLP-1 secretagogues suitable for further study.
直链多糖由于离子和疏水相互作用，比基于树脂的胆汁盐螯合剂更有潜力选择性地吸附疏水性胆汁盐；因此，它们可能具有抗糖尿病活性。通过使用来源于眼虫 β-1,3-葡聚糖（称为 paramylon）的阳离子多糖作为潜在的抗糖尿病剂的可行性，通过体外和动物实验进行了检查。
将阳离子直链多糖从眼虫多糖和缩水甘油三甲基氯化铵合成。在高脂肪饮食诱导的肥胖小鼠中，检查了合成多糖对代谢综合征相关指标的影响。使用光谱分析评估了多糖对胆汁盐的吸附程度。
给予阳离子 paramylon 衍生物可显著降低高脂肪饮食诱导肥胖小鼠的体重和肠系膜脂肪重量。值得注意的是，接受阳离子 paramylon 衍生物的饮食诱导肥胖小鼠的胰高血糖素样肽-1（GLP-1）分泌量比接受纤维素作为对照的小鼠高约三倍。
我们的结果表明，这些阳离子 paramylon 衍生物是适合进一步研究的潜在 GLP-1 分泌激动剂。
