Protein tyrosine phosphatase 1B inhibitory activities of ursane- and lupane-type triterpenes from Sorbus pohuashanensis
Protein tyrosine phosphatase 1B inhibitory activities of ursane- and lupane-type triterpenes from Sorbus pohuashanensis
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DOI：
10.1007/s11418-013-0804-x
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发表时间：
2013-10
影响因子：
3.3
通讯作者：
Dongxia Li;Wei Li;K. Higai;K. Koike
中科院分区：
文献类型：
--
作者：
Dongxia Li;Wei Li;K. Higai;K. Koike
蛋白酪氨酸磷酸酶1B(PTP1B)是一种非跨膜蛋白酪氨酸磷酸酶，因其在负调控胰岛素和瘦素信号通路中的重要作用而成为治疗胰岛素抵抗疾病的分子靶点。6个熊果烷型三萜，3β-乙酰氧基-12-烯-28-OIC酸(1)，3-β-乙酸酯(2)，熊果酸(3)，熊果醛(4)，月桂酸(5)和3-β-乙酰氧基-URS-11-烯-28，13-内酯(6)，以及羽扇豆烷型三萜白桦酸(7)具有显著的PTP1B抑制活性，IC50值在3.5~54.8之间。μM动力学分析表明，化合物2、3和7为非竞争性PTP1B抑制剂，化合物1和6为混合型PTP1B抑制剂。
Protein tyrosine phosphatase 1B (PTP1B) is a non-transmembrane protein tyrosine phosphatase, and has received much attention as a molecular target for the treatment of insulin resistance diseases because of its critical roles in negatively regulating insulin- and leptin-signaling cascades. Six ursane-type triterpenes, 3β-acetoxy-urs-12-ene-28-oic acid (1), pomolic acid-3β-acetate (2), pomolic acid (3), ursolaldehyde (4), euscaphic acid (5) and 3β-acetoxy-urs-11-en-28,13-olide (6), and a lupane-type triterpene, betulinic acid (7), from the fruits ofSorbus pohuashanensis, exhibited significant PTP1B inhibitory activity, with IC50values ranging from 3.5 to 54.8 μM. Kinetics analyses revealed that compounds2, 3, and7are non-competitive PTP1B inhibitors, and compounds1and6are mixed-type PTP1B inhibitors.