Abstract：
Eleven oleanane triterpenoids (1-11) including two new ones (1 and 2) were isolated from the roots and stems of Caulophyllum robustum. Their structures were established by extensive spectroscopic analysis, comparison with literature, and NMR calculations. Compounds 1 and 2 represent the first examples of 23-hydroxy-28-nor-oleanane and 21-hydroxy-olean-3-one triterpenoids, respectively. All isolates were evaluated for their PTP1B and α-glucosidase inhibitory activities in vitro. Among them, the triterpene aglycones 1-5 showed almost equivalent PTP1B inhibitory activities to oleanolic acid and ursolic acid, while 1, 2, and the triterpene saponins 6-11 showed significant α-glucosidase inhibitory activities. Furthermore, compounds 1 and 3 were proved to regulate the expression of proteins implicated the PTP1B/IRS-1/pIRS-1 signalling pathway to improve insulin resistance.
摘要：
从粗花菜的根和茎中分离出11种齐头香三萜（1-11），包括两个新的（1和2）。它们的结构是通过广泛的光谱分析确定的，与文学相比，和NMR计算。化合物1和2代表23-羟基-28-去甲齐烷和21-羟基-布尔-3-酮三萜类化合物的第一个实例，分别。在体外评估所有分离株的PTP1B和α-葡萄糖苷酶抑制活性。其中,三萜苷元1-5表现出与齐墩果酸和熊果酸几乎相当的PTP1B抑制活性，而1、2和三萜皂苷6-11显示出显着的α-葡萄糖苷酶抑制活性。此外，化合物1和3被证明可以调节涉及PTP1B/IRS-1/pIRS-1信号通路的蛋白质的表达，从而改善胰岛素抵抗。
