块根糙苏中黄酮类化合物的降糖活性研究

Hypoglycemic activity study on flavonoids in Phlomis tuberosa L.

目的:研究块根糙苏中黄酮类化合物的降糖活性。方法:四氧嘧啶诱导小鼠糖尿病模型筛选块根糙苏的降糖活性部位。利用多种分离分析技术从活性部位中共分离得到5个黄酮类化合物(木犀草素1、芹菜素2、槲皮素-4’-O-β-D-萄糖苷3、异鼠李素-3-O-β-D-葡萄糖苷4、槲皮素-3-O-β-D-萄糖苷5),其中3～5为首次从该属植物中分离得到。通过α-葡萄糖苷酶体外抑制活性实验验证活性部位中5个黄酮的降糖活性。结果:5个黄酮化合物表现出较强的α-葡萄糖苷酶抑制活性,IC50分别为427.8,502.7,803.4,698.8,768.2μmol/L,均强于阳性药阿卡波糖(IC50为3 760.0μmol/L)。结论:块根糙苏中黄酮类化合物具有降糖活性,提示具有潜在的抗糖尿病功效;为进一步开发高效、新型的抗糖尿病药物提供了先导化合物。

Objective: To study the hypoglycemic activity of flavonoids in Phlomis tuberosa L.. Methods: The alloxaninduced mouse model of diabetes was used to screen the hypoglycemic active site of Phlomis tuberosa L.. Five flavonoids(luteolin 1, apigenin 2, quercetin-4’-O-β-D-glucoside 3, isorhamnetin-3-O-β-D-glucoside 4, quercetin-3-O-β-D-glucoside 5) were isolated from the active site by various separation and analysis techniques, where in 3-5 was isolated from this genus for the first time. The hypoglycemic activity of five flavonoids in the active site was verified by the α-glucosidase inhibitory activity in vitro. Results: Five flavonoids showed strongα-glucosidase inhibitory activity with IC50 of 427.8, 502.7, 803.4, 698.8, and 768.2 μmol/L, respectively, which were stronger than the positive drug acarbose(IC50 of 3 760.0μmol/L). Conclusion: The flavonoids in Phlomis tuberosa L. have hypoglycemic activity, suggesting a potential anti-diabetic effect, which provides leading compounds for the further development of highly effective and novel antidiabetic drugs.