Organic Chemistry; Drug Discovery; Pharmaceutical Science; pharmacognosy; malaria
Abstract :
[en] Casearia coriacea Vent., an endemic plant from the Mascarene Islands, was investigated following its antiplasmodial potentialities highlighted during a previous screening. Three clerodane diterpene compounds were isolated and identified as being responsible for the antiplasmodial activity of the leaves of the plant: caseamembrin T (1), corybulosin I (2), and isocaseamembrin E (3), which exhibited half maximal inhibitory concentrations (IC50) of 0.25 to 0.51 µg/mL. These compounds were tested on two other parasites, Leishmania mexicana mexicana and Trypanosoma brucei brucei, to identify possible selectivity in one of them. Although these products possess both antileishmanial and antitrypanosomal properties, they displayed selectivity for the malaria parasite, with a selectivity index between 6 and 12 regarding antitrypanosomal activity and between 25 and 100 regarding antileishmanial activity. These compounds were tested on three cell lines, breast cancer cells MDA-MB-231, pulmonary adenocarcinoma cells A549, and pancreatic carcinoma cells PANC-1, to evaluate their selectivity towards Plasmodium. This has not enabled us to establish selectivity for Plasmodium, but has revealed the promising activity of compounds 1–3 (IC50 < 2 µg/mL), particularly against pancreatic carcinoma cells (IC50 < 1 µg/mL). The toxicity of the main compound, caseamembrin T (1), was then evaluated on zebrafish embryos to extend our cytotoxicity study to normal, non-cancerous cells. This highlighted the non-negligible toxicity of caseamembrin T (1).
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Ledoux, Allison ; Université de Liège - ULiège > Département de pharmacie > Pharmacognosie
Hamann, Carla ; Université de Liège - ULiège > Unités de recherche interfacultaires > Centre Interdisciplinaire de Recherche sur le Médicament (CIRM)
Bonnet, Olivier ; Université de Liège - ULiège > Unités de recherche interfacultaires > Centre Interdisciplinaire de Recherche sur le Médicament (CIRM)
Jullien, Kateline ; Université de Liège - ULiège > Faculté de Médecine > Master sc. pharma., à fin.
Quetin-Leclercq, Joëlle ; Pharmacognosy Research Group, Louvain Drug Research Institute, LDRI, Université Catholique de Louvain, UCLouvain, Avenue E. Mounier, B1 72.03, B-1200 Brussels, Belgium
Tchinda, Alembert; Laboratory of Pharmacognosy, Center of Interdisciplinary Research on Medicines, CIRM, University of Liège, Avenue Hippocrate 15, 4000 Liège, Belgium
Smadja, Jacqueline; Laboratoire de Chimie des Substances Naturelles et des Sciences des Aliments, Université de Réunion, Avenue René Cassin 15, BP 7151, 97715 Saint-Denis, La Réunion, France
Gauvin-Bialecki, Anne ; Laboratoire de Chimie des Substances Naturelles et des Sciences des Aliments, Université de Réunion, Avenue René Cassin 15, BP 7151, 97715 Saint-Denis, La Réunion, France
Maquoi, Erik ; Université de Liège - ULiège > Département des sciences cliniques > Labo de biologie des tumeurs et du développement
Frederich, Michel ; Université de Liège - ULiège > Département de pharmacie > Pharmacognosie
Language :
English
Title :
Bioactive Clerodane Diterpenoids from the Leaves of Casearia coriacea Vent
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