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

• Published in: Journal of natural products (Washington, D.C.) D.C.), 2010-09, Vol.73 (9), p.1578-1581
• Main Authors: Baumgartner, Renate R, Steinmann, Dirk, Heiss, Elke H, Atanasov, Atanas G, Ganzera, Markus, Stuppner, Hermann, Dirsch, Verena M
• Format: Article
• Language: English
• Subjects: Austria; Biological and medical sciences; Carcinoma, Hepatocellular - metabolism; Diabetes Mellitus, Type 2 - drug therapy; Enzyme Assays; General pharmacology; Humans; Hydrolyzable Tannins - chemistry; Hydrolyzable Tannins - isolation & purification; Hydrolyzable Tannins - pharmacology; Hypoglycemic Agents - chemistry; Hypoglycemic Agents - isolation & purification; Hypoglycemic Agents - pharmacology; Insulin - metabolism; Medical sciences; Paeonia - chemistry; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Plant Roots - chemistry; Plants, Medicinal - chemistry; Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors
• ISSN: 0163-3864; 1520-6025
• DOI: 10.1021/np100258e

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.