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DOI: 10.1055/s-0031-1298242
© Georg Thieme Verlag KG Stuttgart · New York
Ratanhiaphenol III from Ratanhiae Radix is a PTP1B Inhibitor
Publikationsverlauf
received November 7, 2011
revised January 16, 2012
accepted January 18, 2012
Publikationsdatum:
03. Februar 2012 (online)
![](https://www.thieme-connect.de/media/plantamedica/201207/lookinside/thumbnails/10.1055-s-0031-1298242-1.jpg)
Abstract
The inhibition of protein tyrosine phosphatase 1B (PTP1B) is considered a valid strategy to combat insulin resistance and type II diabetes. We show here that a dichloromethane extract of Ratanhiae radix (RR_ex) dose-dependently inhibits human recombinant PTP1B in vitro and enhances insulin-stimulated glucose uptake in murine myocytes. By determination of the PTP1B inhibiting potential of 11 recently isolated lignan derivatives from RR_ex, the observed activity of the extract could be partly assigned to ratanhiaphenol III. This compound inhibited PTP1B in vitro with an IC50 of 20.2 µM and dose-dependently increased insulin receptor phosphorylation as well as insulin-stimulated glucose uptake in cultured myotubes. This is the first report to reveal an antidiabetic potential for a constituent of rhatany root, traditionally used against inflammatory disorders, by showing its capability of inhibiting PTP1B.
Key words
PTP1B inhibition - Ratanhiae radix - Krameria lappacea - Krameriaceae - ratanhiaphenol III
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Dr. Elke Heiss
Department of Pharmacognosy
University of Vienna
Althanstrasse 14
1090 Vienna
Austria
Telefon: +43 14 27 75 59 93
Fax: +43 14 27 75 59 69
eMail: elke.heiss@univie.ac.at