Protein tyrosine phosphatase 1B (PTP1B) is a key element in the negative regulation of the insulin signaling pathway and may play an important role in diabetes and obesity. We identified ursolic acid, a natural pentacyclic triterpenoid that occurs widely in traditional Chinese medicinal herbs, as an inhibitor of PTP1B by screening an extract library of the traditional Chinese medicinal herbs used a diabetes clinic. By modifying urosolic acid, we designed and synthesized a derivative with a K(i) of 283 nM. As competitive inhibitors of PTP1B, ursolic acid and its derivative also inhibit T-cell protein tyrosine phosphatase and src homology phosphatase-2 but not leucocyte antigen-related phosphatase or protein tyrosine phosphatase alpha and epsilon, which are all possibly involved in the insulin pathway. The ursolic acid derivative enhanced insulin receptor phosphorylation in CHO/hIR cells and stimulate glucose uptake in L6 myotubes.

译文

:蛋白酪氨酸磷酸酶1B(PTP1B)是胰岛素信号通路负调节的关键因素,可能在糖尿病和肥胖症中起重要作用。通过筛选用于糖尿病门诊的传统中草药提取物库,我们确定了熊果酸(一种普遍存在于传统中草药中的天然五环三萜类化合物)作为PTP1B抑制剂。通过修饰熊果酸,我们设计并合成了K(i)为283 nM的衍生物。作为PTP1B的竞争性抑制剂,熊果酸及其衍生物还抑制T细胞蛋白酪氨酸磷酸酶和src同源性磷酸酶2,但不抑制白细胞抗原相关的磷酸酶或蛋白酪氨酸磷酸酶α和epsilon,这些都可能与胰岛素途径有关。熊果酸衍生物增强CHO / hIR细胞中胰岛素受体的磷酸化,并刺激L6肌管中的葡萄糖摄取。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录