目的设计合成双(a-呋喃甲酸)氧钒(VO-FA)的衍生物,并进行降糖活性比较.方法采用元素分析、红外光谱、紫外光谱、质谱和核磁共振氢谱初步确证化合物的结构,并进行降糖作用研究,观察样品灌胃给药对四氧嘧啶性糖尿病小鼠血糖水平的影响.结果合成的2个VO-FA衍生物中,双(5-溴-a-呋喃甲酸)氧钒(VO-FABr)没有降糖作用,双(a-四氢呋喃甲酸)氧钒(VO-HFA)的降糖活性则低于VO-FA,且两者的毒性均大于VO-FA.结论在VO-FA分子的呋喃环上打开环内双键或引入溴均降低其生物学活性,而增加毒性.
Objective To design and synthesize derivatives of bis (a -furancarboxylato) oxovanadium (IV) (VO -FA), and to compare their hypoglycemic effects with VO -FA in alloxan -diabetic mice. Methods The chemical structure of the derivatives was determined by elemental analysis, IR, UV, MS and H NMR spectra. The Effects of the derivatives on the blood glucose concentrations were investigated in alloxan - induced diabetic mice. Results During the experiment, his ( a - tetrahydrofurancarboxylato) oxovanadium (Ⅳ) ( VO - HFA) reduced the blood glucose in alloxan - diabetic mice, but was less active than the parent compound VO - FA. Bis (5 - bromo - a - furancarboxylato) oxovanadium (Ⅳ) ( VO - FABr) had no hypoglycemic effect. Both derivatives were more toxic than VO - FA. Conclusion Hydrogen addition of C = C in the ring or introduction of bromine will lower hypoglycemic activity and increase toxicity of the parent compound.