Jiangxi Key Laboratory of Natural Products and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China.
Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences/Key Laboratory of Functional Foods, Guangdong Key Laboratory of Agricultural Products Processing, Guangzhou 510610, China.
Molecules. 2022 Nov 4;27(21):7583. doi: 10.3390/molecules27217583.
Chalcone-1-deoxynojirimycin heterozygote (DC-5), a novel compound which was designed and synthesized in our laboratory for diabetes treatment, showed an extremely strong in vitro inhibitory activity on α-glucosidase in our previous studies. In the current research, its potential in vivo anti-diabetic effects were further investigated by integration detection and the analysis of blood glucose concentration, blood biochemical parameters, tissue section and gut microbiota of the diabetic rats. The results indicated that oral administration of DC-5 significantly reduced the fasting blood glucose and postprandial blood glucose, both in diabetic and normal rats; meanwhile, it alleviated the adverse symptoms of elevated blood lipid level and lipid metabolism disorder in diabetic rats. Furthermore, DC-5 effectively decreased the organ coefficient and alleviated the pathological changes of the liver, kidney and small intestine of the diabetic rats at the same time. Moreover, the results of 16S rDNA gene sequencing analysis suggested that DC-5 significantly increased the ratio of Firmicutes to Bacteroidetes and improved the disorder of gut microbiota in diabetic rats. In conclusion, DC-5 displayed a good therapeutic effect on the diabetic rats, and therefore had a good application prospect in hypoglycemic drugs and foods.
查尔酮-1-去氧野尻霉素杂合体 (DC-5) 是一种新型化合物,由我们实验室设计合成,用于治疗糖尿病,在之前的研究中显示出对 α-葡萄糖苷酶极强的体外抑制活性。在当前的研究中,通过整合检测以及对糖尿病大鼠血糖浓度、血液生化参数、组织切片和肠道微生物群的分析,进一步研究了其潜在的体内抗糖尿病作用。结果表明,DC-5 口服给药可显著降低糖尿病和正常大鼠的空腹血糖和餐后血糖;同时,它缓解了糖尿病大鼠血脂水平升高和脂质代谢紊乱的不良症状。此外,DC-5 还能有效降低糖尿病大鼠的器官系数,减轻其肝脏、肾脏和小肠的病理变化。此外,16S rDNA 基因测序分析的结果表明,DC-5 可显著增加厚壁菌门与拟杆菌门的比值,改善糖尿病大鼠肠道微生物群的紊乱。总之,DC-5 对糖尿病大鼠有良好的治疗效果,因此在降血糖药物和食品方面具有良好的应用前景。