Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta
Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta
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DOI：
10.1080/14756360802693312
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发表时间：
2009-08-01
影响因子：
5.6
通讯作者：
Ahn, Jong Seog
中科院分区：
文献类型：
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作者：
Na, Minkyun;Kim, Bo Yeon;Ahn, Jong Seog
蛋白酪氨酸磷酸酶1B（PTP 1B）似乎是开发2型糖尿病和肥胖症新药的一个有吸引力的靶点。在我们的初步试验中，一个甲醇提取物的干树皮的花楸。（蔷薇科植物）表现出较强的PTP 1B抑制活性。甲醇提取物的生物测定引导的分级分离导致两种羽扇烷型三萜，羽扇豆酮（1）和羽扇豆醇（2）的分离。化合物I和2抑制PTP 1B，IC 50值分别为13.7 +/- 2.1和5.6 +/- 0.9 μ M。动力学研究表明，化合物1和2都是PTP 1B的非竞争性抑制剂，其降低V-max值，而对K-m值没有影响。
Protein tyrosine phosphatase 1B (PTP1B) appears to be an attractive target for the development of new drugs for type 2 diabetes and obesity. In our preliminary test, a MeOH extract of the stem barks of Sorbus commixta Hedl. (Rosaceae) showed strong PTP1B inhibitory activity. Bioassay-guided fractionation of the MeOH extract resulted in the isolation of two lupane-type triterpenes, lupenone (1) and lupeol (2). Compounds I and 2 inhibited PTP1B with IC50 values of 13.7 +/- 2.1 and 5.6 +/- 0.9 mu M, respectively. Kinetic studies revealed that both the compounds 1 and 2 are non-competitive inhibitors of PTP1B that decrease V-max values with no effect on K-m values.