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.

• Authors: Renate R Baumgartner, Dirk Steinmann, Elke H Heiss, Atanas G Atanasov, Markus Ganzera, Hermann Stuppner, Verena M Dirsch
• Journal: Journal of natural products (J Nat Prod) Vol. 73 Issue 9 Pg. 1578-81 (Sep 24 2010) ISSN: 1520-6025 [Electronic] United States
• PMID: 20806783 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Hydrolyzable Tannins
• Hypoglycemic Agents
• Insulin
• pentagalloylglucose
• Protein Tyrosine Phosphatase, Non-Receptor Type 1

Topics

• Austria
• Carcinoma, Hepatocellular (metabolism)
• Diabetes Mellitus, Type 2 (drug therapy)
• Enzyme Assays
• Humans
• Hydrolyzable Tannins (chemistry, isolation & purification, pharmacology)
• Hypoglycemic Agents (chemistry, isolation & purification, pharmacology)
• Insulin (metabolism)
• Paeonia (chemistry)
• Plant Roots (chemistry)
• Plants, Medicinal (chemistry)
• Protein Tyrosine Phosphatase, Non-Receptor Type 1 (antagonists & inhibitors)