Planta Med 2012; 78 - PA14
DOI: 10.1055/s-0032-1320329

Evaluation of natural products as potential angiogenesis modulators

S Dimitrakoudi 1, A Angelis 1, N Aligiannis 1, A Karamitri 2, M Michailidou 1, E Loutrari 1, S Topouzis 2, A Papapetropoulos 2, AL Skaltsounis 1
  • 1Department of Pharmacognosy & Natural Products Chemistry, Faculty of Pharmacy, University of Athens, Panepistimiopolis Zografou, Athens, 15771, Greece
  • 2Laboratory for Molecular Pharmacology, Department of Pharmacy, University of Patra, Rio/Patra, 26504, Greece

Small molecules derived from species of the Greek flora were evaluated as lead preclinical candidates. The aim was to identify potential innovative compounds and molecular targets in the rapidly growing therapeutic field of angiogenesis-related diseases (solid tumors and ischemic heart disease). Specifically, 170 compounds with structurally diverse scaffolds and decoration patterns were screened for their anti- or pro-angiogenetic properties by endothelial cell-based functional assays. The initial screening in an immortalized HUVEC (human umbilical vein endothelial cells) cell line (EA.hy926) at 10µM and 100µM, showed that flavonoids, alkaloids and phenolic compounds exhibited both pro- and anti-angiogenic activity, while terpenes, coumarins, xanthones and anthraquinones provoked inhibition of angiogenesis. The most active inducer was the alkaloid 4-{(E)-2-[4-(dimethylamino)phenyl]-1-ethenyl}-1-ethylpyridinium chloride, while the phenylpropanes, bisphenol and 1-(4-hydroxyphenyl)-3-(4-methoxyphenyl)propane, and the isoflavon 5,4'-dihydroxy-7-methoxyisoflavon showed strong inhibition. Based on these data, a collection of 200 plant extracts obtained from Greek flora was compiled and evaluated in order to discover new natural compounds as promising angiogenetic modulators.