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目的针对钠-葡萄糖协同转运蛋白抑制剂(SGLT)靶点,通过尿糖检测方法筛选和评价糖苷类衍生物的降糖作用。方法 SD大鼠分别单次ig给予8个新型糖苷类衍生物30 mg/kg,在不同时段收集大鼠的尿液,己糖激酶法测定葡萄糖的量;尾静脉取血,血糖仪测血糖水平;同时对活性化合物进行大鼠糖耐量实验。结果新型糖苷类衍生物中N-糖苷类化合物TY702-1N和S-糖苷类化合物TY702-1S对大鼠ig葡萄糖水溶液后的排糖作用较弱,C-糖苷类化合物TY702-4C的排糖作用较强,且显示剂量相关性。结论就开发和研制作用强、药动学性质好的降糖药物而言,新型糖苷类衍生物TY702-4C是一个具有较好前景的先导化合物。
Aim To aim at the target of sodium-glucose cotransporter inhibitor (SGLT), the hypoglycemic effect of glycoside derivatives was screened and evaluated by urine sugar detection method. Methods SD rats were given a single ig eight new glycosides derivatives 30 mg / kg, at different time intervals to collect the urine of rats, hexokinase method for the determination of the amount of glucose; tail vein blood glucose and blood glucose measurement of blood glucose levels At the same time, the rats were subjected to glucose tolerance test. Results The N-glycoside TY702-1N and the S-glycoside TY702-1S of the novel glycoside derivatives had a weaker glucose-releasing effect on ig glucose aqueous solution and the glucose-evolving effect of the C-glycoside compound TY702-4C Strong, and show dose-dependent. Conclusions In terms of developing and developing hypoglycemic drugs with good pharmacokinetic properties, the novel glycoside derivative TY702-4C is a promising compound.