Evaluation of the antiangiogenic and anti-parasitic activities of flavonoids from gardenia species and their modified analogues

LM Hoang; GG Chabot; P Grellier; L Quentin; V Dumontet; S Michel; B Deguin; R Grougnet

doi:10.1055/s-0032-1320514

Planta Medica, Table of Contents

Evaluation of the antiangiogenic and anti-parasitic activities of flavonoids from gardenia species and their modified analogues

LM Hoang ¹, GG Chabot ², P Grellier ³, L Quentin ², V Dumontet ⁴, S Michel ¹, B Deguin ¹, R Grougnet ¹

¹Laboratoire de Pharmacognosie, UMR/CNRS 8638
²Laboratoire de Pharmacologie Chimique, Génétique et Imagerie U1022 Inserm-UMR8151 CNRS, Faculté des Sciences Pharmaceutiques et Biologiques, Université Paris Descartes, 4, Avenue de l'Observatoire, F-75006 Paris
³Museum National d'Histoire Naturelle, FRE 3206 CNRS Molécules de Communication et Adaptation des Micro-organismes, 61 rue Buffon, F-75231 Paris
⁴Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, Labex LERMIT, 1, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France

Abstract

Dedicated to the memory of Pr François Tillequin

The structural similarity of methoxylated flavonoids with the antiangiogenic agent Combretastatin A4 makes them good candidates as potential inhibitors of tumour blood vessels. In addition, some of these secondary metabolites showed noticeable anti-parasite activities against Plasmodium and Trypanosome. In this context, six flavone derivatives, isolated from the glutinous exudate of flowering buds of two species from New-Caledonia Gardenia urvillei and Gardenia oudiepe, and their nine modified analogues were evaluated for antiangiogenic and anti-parasitic activities. Some structure-activity relationship are then proposed.