Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.
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.
Baumgartner
Renate R
RR
Department of Pharmacognosy, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.
Steinmann
Dirk
D
Heiss
Elke H
EH
Atanasov
Atanas G
AG
Ganzera
Markus
M
Stuppner
Hermann
H
Dirsch
Verena M
VM
D001317:Austria; D006528:Carcinoma, Hepatocellular / Q000378:metabolism; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D057075:Enzyme Assays; D006801:Humans; D047348:Hydrolyzable Tannins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007328:Insulin / Q000378:metabolism; D029596:Paeonia / Q000737:chemistry*; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*
D047348:Hydrolyzable Tannins; D007004:Hypoglycemic Agents; D007328:Insulin; C435084:pentagalloylglucose; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1