Dimeric Polyphenols to Pave the Way for New Antimalarial Drugs

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2023 May 1

PMID 37122550

Authors

Gilles Degotte

Helene Pendeville

Carla Di Chio

Roberta Ettari

Bernard Pirotte

Michel Frederich

Pierre Francotte

Affiliations

Soon will be listed here.

Abstract

Because of the threat of resistant , new orally active antimalarials are urgently needed. Inspired by the structure of ellagic acid, exhibiting potent and antiplasmodial effects, polyphenolic structures possessing a similar activity-safety profile were synthesized. Indeed, most exhibited a marked effect (IC < 4 μM) on resistant , without any detrimental effects reported during the toxicity assays (hemolysis, cytotoxicity, ). In addition, they possessed a greater hydrosolubility (from 7 μM to 2.7 mM) compared to ellagic acid. Among them, 30 is the most promising for antimalarial purposes since it displayed a significant parasitaemia reduction after oral administration in mice (50 mg kg) compared to the orally ineffective ellagic acid. In conclusion, our investigations led to the identification of a promising scaffold, which could bring new insights for malaria treatment.

Citing Articles

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Di Chio C, Starvaggi J, Totaro N, Previti S, Natale B, Cosconati S Int J Mol Sci. 2024; 25(8).

PMID: 38673995 PMC: 11050014. DOI: 10.3390/ijms25084410.

Targeting Myeloperoxidase Activity and Neutrophil ROS Production to Modulate Redox Process: Effect of Ellagic Acid and Analogues.

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PMID: 37298992 PMC: 10254444. DOI: 10.3390/molecules28114516.

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