Bioactivity-Guided Isolation of 1,2,3,4,6-Penta-O-galloyl-d-glucopyranose from Paeonia lactiflora Roots As a PTP1B Inhibitor

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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 (1) was isolated from the roots of Paeonia lactiflora as an inhibitor of PTP1B, with an IC50 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.

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