【摘要】 目的:对10个磺酰脲衍生物金属配合物的降血糖作用进行初步筛选。方法:正常小鼠灌胃给药后,剪尾取血,用葡萄糖氧化酶-过氧化物酶(GOD-PAP)法测定血糖,以甲苯磺丁脲(D860)作为阳性对照药物,分析它们的降血糖作用,探讨其作用机理及化学结构与降血糖作用的构效关系。结果:实验表明,ZnL2.2H2O、NdL3.2H2O、SmL3.2H2O、Zn(HL’)2.2NO3、Eu(HL’)3.3NO3、HL、HL’等7个化合物,均具有降低正常小鼠血糖的活性,而EuL3.2H2O、Nd(HL’)3.3NO3、Sm(HL’)3.3NO3降糖活性不明显。结论:HL在2h对正常小鼠的降血糖活性强于D860,提示对甲苯磺酰脲1位取代基为脂环基(环己基)时,其降血糖活性高于直链脂基(丁基),更高于杂环基团(4-安替比林基)。更多还原

【Abstract】 AIM:To screen the hypoglycemic activity of diferent sulphonylureas derivative ligand and their metal complexes. METHODS:The mice were administered intragastrically,the blood samples were obtained from tail vein. The serum glucose levels were determined by glucose-oxidase-peroxidase (GOD-PAP) method. The hypoglycemic activities were analyzed by the mean of tolbutamide as a positive control drug,and its mechanism and structure-activity relationship between chemical structure and hypoglycemic activity were studied. RESUITS:The results showed that ZnL2·2H2O,NdL3·2H2O,SmL3·2H2O,Zn(HL’)2·2NO3,Eu(HL’)3·3NO3,HL and HL’ all reduced the blood sugar in normal mice,while EuL3·2H2O,Nd(HL’)3·3NO3 and Sm(HL’)3·3NO3 had no obvious hypoglycemic activity. CONCLUSION:The hypoglycemic activity of HL is stronger than that of tolbutamide in normal mice at 2 h,indicating that when the first substituent of tosylurea is the alicyclic group (cyclohexyl),its hypoglycemic activity may be higher than the straight-chain lipid group (butyl),and much higher than the heterocyclic group (4-antipyrine).更多还原