Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.

Abstract

The inhibition of protein tyrosine phosphatase 1B (PTP1B) is of substantial interest for the treatment of type-2 diabetes mellitus. Using an in vitro enzyme assay with human recombinant PTP1B 1,2,3,4,6-penta-O-galloyl-D-glucopyranose was isolated from the roots of Paeonia lactiflora as an inhibitor of PTP1B, with an IC(50) value of 4.8 μM. Additionally, 1 was shown to act as an insulin sensitizer in human hepatoma cells (HCC-1.2) at a concentration of 10 μM. Thus, a potential new mechanism of action is provided explaining the antidiabetic properties of P. lactiflora.

DOI: 10.1021/np100258e

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@article{Baumgartner2010BioactivityguidedIO, title={Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.}, author={Renate Rita Baumgartner and Dirk Steinmann and Elke Hannelore Heiss and Atanas G Atanasov and Markus Ganzera and Hermann Stuppner and Verena M. Dirsch}, journal={Journal of natural products}, year={2010}, volume={73 9}, pages={1578-81} }