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目的:研究WX-JT复方对α-葡萄糖苷酶抑制作用,评价WX-JT复方长期给药对Ⅱ型糖尿病KK-Ay小鼠血糖相关指标影响。方法:①体外反转肠囊试验:采用大鼠小肠制备反转肠囊作为α-葡萄糖苷酶的来源,采用经α-淀粉酶消化后的淀粉溶液作为底物,与不同浓度阿卡波糖及WX-JT复方于37℃反应2 h,通过最终葡萄糖产生量计算受试药的α-葡萄糖苷酶抑制率。②正常小鼠淀粉耐量试验:正常ICR小鼠禁食20 h后单次ig给予3 g.kg-1淀粉溶液及45.24,90.48,180.96 mg.kg-1WX-JT复方,测定给予淀粉0,30,60,120 min后血糖,评价药物对血糖升高的抑制作用。③长期给药对Ⅱ型糖尿病小鼠血糖的影响:采用自发Ⅱ型糖尿病模型KK-Ay小鼠,分为模型对照组、阿卡波糖组、WX-JT复方低剂量组(180.96 mg.kg-1)和高剂量组(361.92 mg.kg-1),正常对照组采用C57 BL/6J小鼠。连续ig给药9周,定期测定空腹血糖和非空腹血糖值;试验结束前进行口服葡萄糖耐量试验(OGTT)和糖基化血红蛋白(HbA1c)测定。结果:7～189 mg.L-1WX-JT复方体外能浓度依赖地抑制α-葡萄糖苷酶活性,抑制率为16.6%～86%;90.48,180.96 mg.kg-1WX-JT复方明显降低正常小鼠淀粉耐量试验餐后30,60 min血糖;180.96,361.92 mg.kg-1WX-JT复方长期给药显著降低自发Ⅱ型糖尿病模型KK-Ay小鼠空腹血糖、非空腹血糖和糖化血红蛋白水平,改善口服葡萄糖耐量,并呈明显量效关系。结论:WX-JT复方具有明确的α-葡萄糖苷酶抑制作用,长期给药明显改善KK-Ay小鼠血糖相关指标,表明WX-JT复方通过抑制α-葡萄糖苷酶活性而发挥降血糖作用。
OBJECTIVE: To study the inhibitory effect of WX-JT on α-glucosidase and to evaluate the effect of long-term administration of WX-JT compound on blood glucose related indicators in type 2 diabetic KK-Ay mice. Methods: ① In vitro reversal of the intestinal sac test: The intestine of the intestine was used as a source of α-glucosidase in the small intestine of rats. The starch solution digested with α-amylase was used as the substrate, and different concentrations of acarbose And WX-JT complex at 37 ℃ for 2 h, the α-glucosidase inhibition rate of the tested drug was calculated from the final glucose production. (2) Starch tolerance test in normal mice: The normal ICR mice were fasted for 20 h and then given 3 g.kg-1 starch solution and 45.24, 90.48, 180.96 mg.kg-1WX-JT compound ig for one time. , 60,120 min after the blood glucose, evaluation of drugs on the inhibition of elevated blood sugar. (3) The effect of long-term administration on blood glucose in type 2 diabetic mice: KK-Ay mice were randomly divided into model control group, acarbose group, WX-JT low dose group (180.96 mg.kg -1) and high dose group (361.92 mg.kg-1). C57BL / 6J mice were used as normal control group. Continuous ig administration for 9 weeks, regular fasting blood glucose and non-fasting blood glucose values; oral glucose tolerance test (OGTT) and glycosylated hemoglobin (HbA1c) determination before the end of the test. Results: 7 ~ 189 mg.L-1WX-JT compound could inhibit a-glucosidase activity in vitro in a concentration-dependent manner with the inhibition rate of 16.6% -86%; 90.48,180.96 mg.kg-1WX-JT compound significantly decreased the normal Long-term administration of 180.96, 361.92 mg.kg-1WX-JT compound fasting blood glucose, fasting blood glucose, non-fasting blood glucose and glycosylated hemoglobin in spontaneous type 2 diabetic KK-Ay mice were significantly improved Oral glucose tolerance, and showed a significant dose-effect relationship. Conclusion: The WX-JT compound has a definite inhibitory effect on α-glucosidase, long-term administration significantly improved blood glucose related indicators KK-Ay mice, indicating that WX-JT compound by inhibiting α-glucosidase activity and hypoglycemic effect.