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Related Experiment Videos

Kinase inhibitors from Polygonum cuspidatum

G S Jayatilake1, H Jayasuriya, E S Lee

  • 1Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.

Journal of Natural Products
|October 1, 1993
PubMed
Summary

Resveratrol, a compound from Polygonum cuspidatum, inhibits protein-tyrosine kinase (p56lck). Its structure requires free hydroxyl groups on both phenyl rings for this kinase inhibition activity.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Natural Products Chemistry

Background:

  • Polygonum cuspidatum is a medicinal plant with potential therapeutic properties.
  • Protein-tyrosine kinases (PTKs) play crucial roles in cellular signaling pathways.
  • Dysregulation of PTKs is implicated in various diseases, making them important drug targets.

Purpose of the Study:

  • To identify bioactive compounds from Polygonum cuspidatum using bioassay-directed fractionation.
  • To investigate the inhibitory activity of isolated compounds against protein-tyrosine kinase (p56lck).
  • To elucidate the structure-activity relationship of resveratrol and its derivatives regarding kinase inhibition.

Main Methods:

  • Bioassay-directed fractionation of Polygonum cuspidatum extract.

Related Experiment Videos

  • Purification and isolation of resveratrol and related glucosides.
  • Enzyme inhibition assays to determine IC50 values for protein-tyrosine kinase (p56lck) and protein kinase C.
  • Comparative analysis of inhibitory activities of different resveratrol isomers and derivatives.

    • Main Results:

    • Resveratrol was identified as a potent inhibitor of bovine thymus p56lck.
    • Both trans and cis isomers of resveratrol demonstrated comparable inhibitory activity.
    • Free hydroxyl groups on both phenyl rings of resveratrol are essential for protein-tyrosine kinase inhibition.
    • Protein kinase C inhibition requires two free hydroxyl groups on a single phenyl ring.

    Conclusions:

    • Resveratrol is a significant inhibitor of p56lck, highlighting its potential pharmacological value.
    • The specific hydroxyl group configuration is critical for resveratrol's kinase inhibitory mechanisms.
    • Understanding these structure-activity relationships can guide the development of novel kinase inhibitors.