Jiang Pingzhe, Dong Zhen, Ma Baicheng, Ni Zaizhong, Duan Huikun, Li Xiaodan, Wang Bin, Ma Xiaofeng, Wei Qian, Ji Xiangzhen, Li Minggang
Key Laboratory for Bioactive Materials of the Ministry of Education, Institute of Molecular Biology, College of Life Science, Nankai University, 300071, Tianjin, China.
State Key Laboratory of Medicinal Chemical Biology, Nankai University, 300071, Tianjin, China.
Appl Biochem Biotechnol. 2016 Nov;180(5):841-851. doi: 10.1007/s12010-016-2137-1. Epub 2016 May 30.
Diabetes has been cited as the most challenging health problem in the twenty-first century. Accordingly, it is urgent to develop a new type of efficient and low-toxic antidiabetic medication. Since vanadium compounds have insulin-mimetic and potential hypoglycemic activities for type 1 and type 2 diabetes, a new trend has been developed using vanadium and organic ligands to form a new compound in order to increase the intestinal absorption and reduce the toxicity of vanadium compound. In the current investigation, a new organic vanadium compounds, vanadyl rosiglitazone, was synthesized and determined by infrared spectra. Vanadyl rosiglitazone and three other organic vanadium compounds were administered to the diabetic mice through oral administration for 5 weeks. The results of mouse model test indicated that vanadyl rosiglitazone could regulate the blood glucose level and relieve the symptoms of polydipsia, polyphagia, polyuria, and weight loss without side effects and was more effective than the other three organic vanadium compounds including vanadyl trehalose, vanadyl metformin, and vanadyl quercetin. The study indicated that vanadyl rosiglitazone presents insulin-mimetic activities, and it will be a good potential candidate for the development of a new type of oral drug for type 2 diabetes.
糖尿病被认为是21世纪最具挑战性的健康问题。因此，开发一种新型高效低毒的抗糖尿病药物迫在眉睫。由于钒化合物对1型和2型糖尿病具有胰岛素模拟和潜在的降血糖活性，利用钒与有机配体形成新化合物以增加肠道吸收并降低钒化合物毒性的新趋势已经出现。在当前的研究中，合成了一种新的有机钒化合物——罗格列酮钒，并通过红外光谱进行了测定。将罗格列酮钒和其他三种有机钒化合物通过口服给药给糖尿病小鼠5周。小鼠模型试验结果表明，罗格列酮钒可以调节血糖水平，缓解多饮、多食、多尿和体重减轻的症状，且无副作用，比其他三种有机钒化合物（包括海藻糖钒、二甲双胍钒和槲皮素钒）更有效。该研究表明，罗格列酮钒具有胰岛素模拟活性，它将是开发新型2型糖尿病口服药物的良好潜在候选物。
