车前子环烯醚萜苷类化合物与其抑制PTP1B的活性研究

Protein Tyrosine Phosphatase 1B Inhibitory Activity of Iridoid Glucosides Isolated from Plantago Asiatica

蛋白酪氨酸磷酸酯酶1B在胰岛素信号传达过程中起负调控作用,也是研究治疗2型糖尿病的重要靶点.利用生物活性导向分离方法从车前子中分离得到6个环烯醚萜苷类活性化合物.通过光谱和文献比较鉴定,6种化合为Desacetylhookerioside(1),Hookerioside(2),Alpinoside(3),Majoroside(4),Anagalloside(5)和10-hydroxymajoroside(6),其中化合物3和5可以有效抑制PTP1B的活性,其IC50值分别为(17.7±2.5)和(19.8±1.2)μM.

Protein tyrosine phosphatase 1B plays a major role in the negative regulation of insulin signaling,and thus considered as an attractive therapeutic target for diabetes.Bioassay-guided fractionation of the seeds of Plantago asiatica afforded six protein tyrosine phosphatase 1B inhibitory iridoid glucosides（1-5）.Six compounds were identified as Desacetylhookerioside（1）,Hookerioside（2）,Alpinoside（3）,Majoroside（4） Alpinoside（5） and 10-hydroxymajoroside（6） by comparison of their spectral data with those in the literature.Isolated compounds 3 and 5 inhibited PTP1B with IC50 values ranged from（17.7±2.5） to（19.8±1.2）μM.