A new insulin-enhancing agent: [N,N′-bis(4-hydroxysalicylidene)-o-phenylene-diamine]oxova nadium(IV) and its permeability and cytotoxicity

作者：Xie, Ming-jin^*; Li, Ling; Yang, Xiao-Da; Liu, Wei-ping; Yan, Shi-ping; Niu, Yan-fen; Meng, Zhao-hui

来源：European Journal of Medicinal Chemistry, 2010, 45(6): 2327-2335.

DOI：10.1016/j.ejmech.2010.02.010

• Insulin-enhancing
• Salen-type ligands
• Caco-2 cells

A new insulin-enhancing agent: [N,N'-bis(4-hydroxysalicylidene)-o-phenylene-diamine] oxovanadium (IV) (BPOV) was synthesized and characterized by X-ray crystallography. BPOV was administered intragastrically to STZ-diabetic rats for 4 weeks. The results showed that BPOV could significantly decrease the blood glucose level and ameliorated impaired glucose tolerance in STZ-diabetic rats. BPOV has been further tested on insulin, glycogen and serum lipid studies. The results suggested BPOV has glucose-lowering activity in diabetic rats, as well as improved the disorder of lipid metabolism in diabetes. BPOV had permeability above 10(-5) cm s(-1). It was suggested good lipophilic properties. The cytotoxicity of BPOV on Caco-2 cells was measured by MTT assay which suggested BPOV have higher effect on impairment of cellular associated with lower level capacity of cellular accumulation.

• 出版日期2010-6
• 单位昆明医科大学; 北京大学; 云南大学; 昆明贵金属研究所; 南开大学