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

Renate R Baumgartner; Dirk Steinmann; Elke H Heiss; Atanas G Atanasov; Markus Ganzera; Hermann Stuppner; Verena M Dirsch

doi:10.1021/np100258e

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

J Nat Prod. 2010 Sep 24;73(9):1578-81. doi: 10.1021/np100258e.

Authors

Renate R Baumgartner¹, Dirk Steinmann, Elke H Heiss, Atanas G Atanasov, Markus Ganzera, Hermann Stuppner, Verena M Dirsch

Affiliation

¹ Department of Pharmacognosy, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.

PMID: 20806783
DOI: 10.1021/np100258e

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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