Background: With the aim of discovering new natural active extracts against malaria parasites, Icacina senegalensis was selected after an ethnopharmacological survey conducted on plants used in traditional malaria treatment in Senegal.
Methods: Different concentrations of the plant extract and fractions were tested on synchronized Plasmodium falciparum cultures at the ring stage using the parasite lactate dehydrogenase assay. Their haemolytic activity and in vitro cytoxicity were evaluated. The chromatographic profiles of active fractions were also established.
Results: The plant extract and fractions revealed anti-plasmodial activity (IC50 < 5 μg/mL) with no toxicity (Selectivity indexes >10). The dichloromethane fraction showed stronger anti-plasmodial activity than the total extract.
Conclusion: Anti-plasmodial activity and toxicity of I. senegalensis are reported for the first time and showed promising results in malaria field research.
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http://dx.doi.org/10.1186/1475-2875-10-85 | DOI Listing |
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFMolecules
November 2024
School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332, USA.
Agunmu (ground herbal medicine) is a form of West African traditional medicine consisting of a cocktail of herbs. The goal of this study is to evaluate a formulation of Agunmu made from , , , , and , sold in the open market and commonly used for the treatment of malaria by the locals, for its antimalarial effects and to determine the active principles that may contribute to the antimalarial effect. The ethanolic extract obtained from this formulation (Ag-Iba) was analyzed, using TLC, LC-MS, and Tandem-MS techniques, to determine its phytochemical properties.
View Article and Find Full Text PDFFuture Med Chem
December 2024
Department of Chemistry, Guru Nanak Dev University, Amritsar, India.
The aim of this study is to synthesize indolo[2,3-]quinoxaline-4-aminoquinoline-based hybrids and evaluate their effectiveness against chloroquine-susceptible (3D7) and resistant (W2) strains, with expected inhibition of chloroquine resistance transporter (CRT) and heme. The hybrids were synthesized and evaluated against both susceptible and resistant strains. Molecular docking and studies were conducted to assess the binding affinities for the CRT protein.
View Article and Find Full Text PDFMalar J
September 2024
Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, College of Health Sciences, Addis Ababa University, P.O Box.1176, Addis Ababa, Ethiopia.
Background: Over the past years, there has been a growing concern that a considerable amount of anti-malarial supply in the underdeveloped world particularly in the private sector, is of poor quality. The World Health Organization (WHO) has received about 1500 reports that mentions instances of substandard and falsified products since 2013. The majority of the reports concerned antibiotics and anti-malarials.
View Article and Find Full Text PDFPhytomedicine
October 2024
In vivo Testing facility, Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, Uttar Pradesh 226015, India; AcSIR, Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Background: Malaria, characterised by inflammation and multi-organ complications, needs novel chemotherapeutics due to the rise of drug-resistant malaria parasites, which is a serious health issue. Naringin (NGN), a flavanone glycoside (naringenin 7-O-neohesperidose), has a broad spectrum of pharmacological activities but its effect against malaria, alone and in combination, was not deeply investigated.
Purpose: To assess the pharmacological efficacy of NGN alone and in combination with chloroquine (CQ) against a Plasmodium strain resistant to CQ and to elucidate its potential mode of action.
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