[关键词]
[摘要]
目的 考察藏药美多罗米抗糖尿病药效物质基础。方法 多舌飞蓬Erigeron multiradiatus为美多罗米原植物之一。利用萃取、大孔树脂柱色谱法对多舌飞蓬的化学成分进行提取分离,通过体外醛糖还原酶抑制反应探讨其药效部位。制备链脲佐菌素致糖尿病大鼠模型,将糖尿病大鼠随机分成4组,模型组(蒸馏水),依帕司他(10 mg/kg)阳性对照组和多舌飞蓬提取物II低、高剂量(200、400 mg/kg)组,各组ig相应药物,每天1次,连续给药11周。观察大鼠一般状态,检测体质量、血糖、尿糖、血流动力学及心功能参数等的变化。结果 多舌飞蓬提取物I和提取物II对醛糖还原酶活性均有抑制作用,IC50分别为0.64、0.12 mg/mL。与模型组相比,提取物II高剂量组大鼠体质量增加,血糖水平降低,心率提高,左心室平均舒张末期压(LEVDP)及最大上升速率(+dp/dtmax)升高(P<0.05、0.01、0.001)。结论 提取物II具有明显的醛糖还原酶抑制活性,能够改善血流动力学行为,保护心脏功能,为美多罗米抗糖尿病药效物质基础。
[Key word]
[Abstract]
Objective To study the antidiabetic constituents of Tibetan Medicine “Meiduoluomi”. Methods Erigeron multiradiatus (EM) is one of the crude materials. The chemical constituents in EM were extracted and isolated by extraction and macroporous resin column. The inhibitory activities of the extracts against aldose reductase (AR) were evaluated in vitro to make sure the active fragments. Diabetic rats induced by streptozotocin were randomly divided into four groups: model (distilled water), positive control (epalrestat 10 mg/kg), EM II low- and high-dosage (200, 400 mg/kg) groups. The rats were ig administered once daily for 11 weeks. The rat normal sign, body weight, urine glucose, blood glucose, hemodynamics, and cardiac function parameters were determined. Results Both EM I and EM II showed the inhibitory activities against AR with IC50 values of 0.64 and 0.12 mg/mL, respectively. Compared with diabetic group, body weight, heart rate, left ventricular end diastolic pressure average (LEVDP) and the left ventricular maximum rate of pressure development (+dp/dtmax) in EM II group were significantly improved, while blood glucose was decreased (P < 0.05, 0.01, 0.001). Conclusion EM II demonstrates the obvious inhibitory activity on AR, and could improve the hemodynamics and protect heart function, which may be the antidiabetic active constituents of “Meiduoluomi”.
[中图分类号]
[基金项目]
国家科技支撑计划课题(2012BAI27B07);澳门特别行政区科学技术发展基金(073/2011/A3)