Sylvain G Alson1,2, Olivia Jansen1, Ewa Cieckiewicz1, Hajatiana Rakotoarimanana2, Herintsoa Rafatro2, Gilles Degotte1,3, Pierre Francotte3, Michel Frederich1. 1. Laboratoire de pharmacognosie, Centre Interdisciplinaire de Recherches sur les Médicaments (CIRM), Université de Liège, Liège, Belgium. 2. Laboratoire d'Évaluation Pharmaco Clinique (LEPC), Institut Malgache de Recherches Appliquées (IMRA), Fondation Albert et Suzanne Rakoto-Ratsimamanga, Antananarivo, Madagascar. 3. Laboratoire de Chimie Pharmaceutique, Centre Interdisciplinaire de Recherches sur les Médicaments (CIRM), Université de Liège, Liège, Belgium.
Abstract
OBJECTIVES: To explore the in-vitro and in-vivo antimalarial potential of caffeic acid and derivatives. METHODS: Two common phenolic acids (caffeic acid and chlorogenic acid) were evaluated for in-vitro and in-vivo antiplasmodial activity in comparison with some semi-synthetic derivatives that were synthesized. An in-vitro assay based on plasmodial lactate dehydrogenase activity, and the classical in-vivo 5-day suppressive test from Peters on an artemisinin-resistant Plasmodium berghei strain was used. Parasitic stage sensitivity to ethyl caffeate was determined in this work. KEY FINDINGS: Phenolic acid esters derivatives showed better antiplasmodial activity than corresponding phenolic acids. The derivative with the highest in-vitro activity being caffeic acid ethyl ester, exhibiting an IC50 = 21.9 ± 9.4 μm. Ethyl caffeate and methyl caffeate were then evaluated for antimalarial activity in vivo and ethyl caffeate showed a growth inhibition of 55% at 100 mg/kg. Finally, it seems that ethyl caffeate blocks the growth of young parasitic forms. CONCLUSIONS: Our study provides evidence for an antimalarial potential of caffeic acid derivatives which are common in several medicinal plants traditionally used against malaria. It also demonstrates the possibility to use such derivatives in the treatment of malaria.
OBJECTIVES: To explore the in-vitro and in-vivo antimalarial potential of caffeic acid and derivatives. METHODS: Two common phenolic acids (caffeic acid and chlorogenic acid) were evaluated for in-vitro and in-vivo antiplasmodial activity in comparison with some semi-synthetic derivatives that were synthesized. An in-vitro assay based on plasmodial lactate dehydrogenase activity, and the classical in-vivo 5-day suppressive test from Peters on an artemisinin-resistant Plasmodium berghei strain was used. Parasitic stage sensitivity to ethyl caffeate was determined in this work. KEY FINDINGS:Phenolic acid esters derivatives showed better antiplasmodial activity than corresponding phenolic acids. The derivative with the highest in-vitro activity being caffeic acid ethyl ester, exhibiting an IC50 = 21.9 ± 9.4 μm. Ethyl caffeate and methyl caffeate were then evaluated for antimalarial activity in vivo and ethyl caffeate showed a growth inhibition of 55% at 100 mg/kg. Finally, it seems that ethyl caffeate blocks the growth of young parasitic forms. CONCLUSIONS: Our study provides evidence for an antimalarial potential of caffeic acid derivatives which are common in several medicinal plants traditionally used against malaria. It also demonstrates the possibility to use such derivatives in the treatment of malaria.
Authors: Susiany P Lopes; Lina M Yepes; Yunierkis Pérez-Castillo; Sara M Robledo; Damião P de Sousa Journal: Molecules Date: 2020-07-11 Impact factor: 4.411
Authors: Xiaoming Wang; Xiaoyan Chang; Xiaomei Luo; Meifeng Su; Rong Xu; Jun Chen; Yi Ding; Yue Shi Journal: Front Pharmacol Date: 2019-07-25 Impact factor: 5.810