Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake
W Zhang, D Hong, Y Zhou, Y Zhang, Q Shen… - … et Biophysica Acta (BBA …, 2006 - Elsevier
W Zhang, D Hong, Y Zhou, Y Zhang, Q Shen, J Li, L Hu, J Li
Biochimica et Biophysica Acta (BBA)-General Subjects, 2006•ElsevierProtein 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 Ki of 283 nM. As competitive inhibitors of …
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 Ki of 283 nM. As competitive inhibitors of …
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 Ki 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 α and ε, 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.
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