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Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates

Steven C Zammit1, Alison J Cox, Renae M Gow

  • 1School of Chemistry, Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Parkville, VIC 3010, Australia.

Bioorganic & Medicinal Chemistry Letters
|November 3, 2009
PubMed

Insights

Tranilast derivatives show promise in treating diabetic nephropathy by reducing kidney fibrosis. A novel compound significantly lowered albuminuria in diabetic rats, indicating potential for improved kidney function.

Area of Science:

  • Pharmacology
  • Nephrology
  • Medicinal Chemistry

Background:

  • Tranilast, an anti-inflammatory agent, has demonstrated antifibrotic properties in the kidney.
  • Diabetic nephropathy is characterized by progressive kidney fibrosis and dysfunction.
  • Optimizing tranilast's structure is crucial for enhancing its efficacy against kidney fibrosis.

Purpose of the Study:

  • To conduct a structure-activity relationship study of cinnamoyl anthranilates.
  • To identify tranilast derivatives with improved antifibrotic activity and reduced toxicity.
  • To evaluate the potential of these derivatives in treating diabetic nephropathy.

Main Methods:

  • Synthesis of a series of cinnamoyl anthranilate derivatives.
  • Assessment of antifibrotic activity using TGF-beta-stimulated collagen production in renal mesangial cells.
  • In vivo evaluation of a lead compound in a rat model of progressive diabetes.

Main Results:

  • Several tranilast derivatives exhibited enhanced antifibrotic potency compared to the parent compound.
  • Some derivatives demonstrated reduced cellular toxicity.
  • 3-Methoxy-4-propargyloxycinnamoyl anthranilate significantly reduced albuminuria in diabetic rats.

Conclusions:

  • Novel cinnamoyl anthranilates possess superior antifibrotic properties and lower toxicity than tranilast.
  • 3-Methoxy-4-propargyloxycinnamoyl anthranilate shows significant potential for treating diabetic nephropathy.
  • This study provides a basis for developing innovative therapies for diabetic kidney disease.

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