Planta Med 2008; 74(4): 401-406
DOI: 10.1055/s-2008-1034346
Pharmacology
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Competitive ELISA-Based Screening of Plant Derivatives for the Inhibition of VEGF Family Members Interaction with Vascular Endothelial Growth Factor Receptor 1

Salvatore Ponticelli1 , 4 , Alessandra Braca2 , 4 , Nunziatina De Tommasi3 , Sandro De Falco1
  • 1Angiogenesis Lab and Stem Cell Fate Lab, Istituto di Genetica e Biofisica ‘Adriano Buzzati-Traverso’, CNR, Napoli, Italy
  • 2Dipartimento di Chimica Bioorganica e Biofarmacia, Università di Pisa, Pisa, Italy
  • 3Dipartimento di Scienze Farmaceutiche, Università di Salerno, Fisciano (SA), Italy
  • 4These authors contributed equally to this work
Further Information

Publication History

Received: November 29, 2007 Revised: February 5, 2008

Accepted: February 6, 2008

Publication Date:
25 March 2008 (online)

Abstract

The activation of vascular endothelial growth factor receptor-1 (VEGFR-1, also known as Flt-1) is crucial in many physiological and pathological conditions, like angiogenesis, cancer, inflammation, hematopoiesis, bone marrow precursors/stem cells recruitment in tumor angiogenesis, and metastasis formation. Many recent reports indicate that molecules able to antagonize Flt-1 activity have gained a strong interest in the view of therapeutic approaches. In order to identify new compounds able to interfere in the Flt-1 recognition by VEGFs family members, we have developed a highly sensitive competitive ELISA-based screening to study plant extracts and derivatives. Several fractions of the n-butanol extract of Pteleopsis suberosa leaves and of the chloroform extract of Parinari campestris leaves demonstrated by a bioassay-guided fractionation an evident inhibition of VEGF-A or placental growth factor (PlGF) interaction with Flt-1, with an inhibition over 50 % in particular for the VEGF-A/Flt-1 interaction at a concentration of 100 μg/mL. This activity seems be due to the presence of a combination of compounds acting synergistically.

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Dr. Sandro De Falco

Angiogenesis Lab and Stem Cell Fate Lab

Institute of Genetics and Biophysics ‘Adriano Buzzati-Traverso’

CNR,

Via P. Castellino 111

80131 Naples

Italy

Phone: +39-081-613-2354

Fax: +39-081-613-2595

Email: defalco@igb.cnr.it