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Evaluation of licorice flavonoids as protein tyrosine phosphatase 1B inhibitors

Wei Li1, Songpei Li, Koji Higai

  • 1Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba 274-8510, Japan.

Bioorganic & Medicinal Chemistry Letters
|September 20, 2013
PubMed

Insights

New licorice flavonoids, including glycybenzofuran, show potential as PTP1B inhibitors. Glycybenzofuran demonstrates selective inhibition and cellular activity, suggesting its use as an anti-insulin-resistant drug candidate for diabetes and obesity.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Protein tyrosine phosphatase 1B (PTP1B) is a key regulator in insulin and leptin signaling pathways.
  • PTP1B also plays a role in cancer development, making its inhibitors attractive therapeutic targets for diabetes, obesity, and cancer.

Purpose of the Study:

  • To screen licorice flavonoids for novel PTP1B inhibitors.
  • To evaluate the inhibitory mechanisms, selectivity, and cellular activity of identified compounds in the insulin-signaling pathway.

Main Methods:

  • Screening of a licorice flavonoid compound library against PTP1B.
  • Assays to determine inhibitory modes, selectivity, and cellular effects on insulin signaling.
  • Analysis of Akt phosphorylation levels in response to insulin stimulation.

Main Results:

  • Several licorice flavonoids, including licoagrone, licoagrodin, licoagroaurone, and isobavachalcone, were identified as new PTP1B inhibitors.
  • These compounds exhibited varied inhibition modes, selectivities, and cellular activities.
  • Glycybenzofuran, a competitive PTP1B inhibitor, displayed high selectivity and significant cellular activity in the insulin-signaling pathway, specifically on insulin-stimulated Akt phosphorylation.

Conclusions:

  • Licorice flavonoids represent a promising source for novel PTP1B inhibitors.
  • Glycybenzofuran's potent PTP1B inhibition and favorable cellular activity profile suggest its potential as a therapeutic candidate for combating insulin resistance.
Keywords:
FlavonoidsGlycyrrhizaLicoriceProtein tyrosine phosphatase 1B

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