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Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.
- Source :
-
Journal of natural products [J Nat Prod] 2010 Sep 24; Vol. 73 (9), pp. 1578-81. - Publication Year :
- 2010
-
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.
- Subjects :
- Austria
Carcinoma, Hepatocellular metabolism
Diabetes Mellitus, Type 2 drug therapy
Enzyme Assays
Humans
Hydrolyzable Tannins chemistry
Hypoglycemic Agents chemistry
Insulin metabolism
Plant Roots chemistry
Hydrolyzable Tannins isolation & purification
Hydrolyzable Tannins pharmacology
Hypoglycemic Agents isolation & purification
Hypoglycemic Agents pharmacology
Paeonia chemistry
Plants, Medicinal chemistry
Protein Tyrosine Phosphatase, Non-Receptor Type 1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1520-6025
- Volume :
- 73
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Journal of natural products
- Publication Type :
- Academic Journal
- Accession number :
- 20806783
- Full Text :
- https://doi.org/10.1021/np100258e