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Planta Med 2006; 72(12): 1127-1131
DOI: 10.1055/s-2006-946700
Original Paper
Pharmacology
© Georg Thieme Verlag KG Stuttgart · New York

Plant Phenolics Inhibit Neutrophil Elastase

Andrea Hrenn1 , Thomas Steinbrecher2 , Andreas Labahn2 , Joseph Schwager3 , Christoph M. Schempp4 , Irmgard Merfort1
  • 1Institute for Pharmaceutical Sciences, Department of Pharmaceutical Biology and Biotechnology, University of Freiburg, Freiburg, Germany
  • 2Institute for Physical Chemistry, University of Freiburg, Freiburg, Germany
  • 3DSM Nutritional Products, Kaiseraugst, Switzerland
  • 4Department of Dermatology, University of Freiburg, Freiburg, Germany
In memory of Professor Ernst Reinhard
Further Information

Publication History

Received: March 24, 2006

Accepted: June 1, 2006

Publication Date:
28 August 2006 (online)

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Abstract

Human neutrophil elastase (HNE) is a serine protease, which is present in its active form in inflamed tissue as well as in psoriatic lesions. In extension of our research on natural compounds as inhibitors of HNE or of its release, several phenolics of different size were tested. The ellagitannins agrimoniin and pedunculagin were the most potent direct HNE inhibitors (IC50 = 0.9 and 2.8 μM, respectively). Ligand docking calculations provided evidence that inhibition may occur in an unspecific manner. Agrimoniin also showed anti-proliferative effects in the ATP assay (IC50 = 3.2 μM), suggesting that this type of tannin could have beneficial effects in the treatment of diseases such as psoriasis. Tests with other phenolics combined with ligand docking experiments revealed that, besides the presence of ortho-dihydroxy groups, a specific lipophilic shape is necessary for an inhibitory activity. The phenolic genistein deserves special interest as an inhibitor of elastase release because its effect was remarkably potent (IC50 = 0.6 μM).

Key words

Human neutrophil elastase - proliferation - phenolics - genistein - tannins - agrimoniin - resveratrol - ligand docking

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Prof. Dr. I. Merfort

Institute for Pharmaceutical Sciences

Department of Pharmaceutical Biology and Biotechnology

University of Freiburg

Stefan-Meier-Str. 19

79104 Freiburg

Germany

Phone: +49-761-203-8373

Fax: +49-761-203-8383

Email: irmgard.merfort@pharmazie.uni-freiburg.de

    www.thieme-connect.de/ejournals/toc/plantamedica