ArticleAntimicrobial agents and chemotherapy2001
Inhibition of fumarate reductase in Leishmania major and L. donovani by chalcones.
Article in Antimicrobial agents and chemotherapy, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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41 citing papers in PubMed, 200 citations in OpenAlex.
- Novel Benzofuranyl Chalcones With Antileishmanial Activity: Synthesis, Structure-Activity Relationships, and Computational Target Hypothesis Studies.ChemMedChem · 2026Article
- Insights of potential trypanocidal effect of the synthetic derivative (2E)-1-(4-aminophenyl)-3-(2,4-dichlorophenyl)prop-2-en-1-one: in vitro assay, MEV analysis, quantum study, molecular docking, molecular dynamics, MPO analysis, and predictive ADMET.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- Synthesis, characterization and evaluation of prenylated chalcones ethers as promising antileishmanial compounds.Molecular diversity · 2023Article
- Brazilian Amazon Red Propolis: Leishmanicidal Activity and Chemical Composition of a New Variety of Red Propolis.Metabolites · 2023Article
- Chalcone Derivative Induces Flagellar Disruption and Autophagic Phenotype inPathogens (Basel, Switzerland) · 2023Article
- Design, Rational Repurposing, Synthesis, In Vitro Evaluation, Homology Modeling and In Silico Study of Sulfuretin Analogs as Potential Antileishmanial Hit Compounds.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Total Synthesis of the Natural Chalcone Lophirone E, Synthetic Studies toward Benzofuran and Indole-Based Analogues, and Investigation of Anti-Leishmanial Activity.Molecules (Basel, Switzerland) · 2022Article
- Synthesis, Structural Characterizations, and Quantum Chemical Investigations on 1-(3-Methoxy-phenyl)-3-naphthalen-1-yl-propenone.ACS omega · 2021Article
- An Overview on the Therapeutics of Neglected Infectious Diseases-Leishmaniasis and Chagas Diseases.Frontiers in chemistry · 2021Review
- Recent researches in effective antileishmanial herbal compounds: narrative review.Parasitology research · 2020Review
- Licochalcone a Exhibits Leishmanicidal ActivityFrontiers in veterinary science · 2020Article
- Identification of Chalcone Derivatives as Inhibitors ofFrontiers in chemistry · 2020Article
- The effects of trans-chalcone and chalcone 4 hydrate on the growth of Babesia and Theileria.PLoS neglected tropical diseases · 2019Article
- Anti-Trichomonas vaginalis activity of chalcone and amino-analogues.Parasitology research · 2019Article
- Berberine chloride mediates its antileishmanial activity by inhibiting Leishmania mitochondria.Parasitology research · 2019Article
- Emerging therapeutic targets for treatment of leishmaniasis.Expert opinion on therapeutic targets · 2018Review
- QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.European journal of medicinal chemistry · 2017Article
- Computer-aided discovery of two novel chalcone-like compounds active and selective against Leishmania infantum.Bioorganic & medicinal chemistry letters · 2017Article
- The mitochondrial SIR2 related protein 2 (SIR2RP2) impacts Leishmania donovani growth and infectivity.PLoS neglected tropical diseases · 2017Article
- The Role of Natural Products in Drug Discovery and Development against Neglected Tropical Diseases.Molecules (Basel, Switzerland) · 2016Review
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5 authors at 4 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
Our previous studies have shown that chalcones exhibit potent antileishmanial and antimalarial activities in vitro and in vivo. Preliminary studies showed that these compounds destroyed the ultrastructure of Leishmania parasite mitochondria and inhibited the respiration and the activity of mitochondrial dehydrogenases of Leishmania parasites. The present study was designed to further investigate the mechanism of action of chalcones, focusing on the parasite respiratory chain. The data show that licochalcone A inhibited the activity of fumarate reductase (FRD) in the permeabilized Leishmania major promastigote and in the parasite mitochondria, and it also inhibited solubilized FRD and a purified FRD from L. donovani. Two other chalcones, 2,4-dimethoxy-4'-allyloxychalcone (24m4ac) and 2,4-dimethoxy-4'-butoxychalcone (24mbc), also exhibited inhibitory effects on the activity of solubilized FRD in L. major promastigotes. Although licochalcone A inhibited the activities of succinate dehydrogenase (SDH), NADH dehydrogenase (NDH), and succinate- and NADH-cytochrome c reductases in the parasite mitochondria, the 50% inhibitory concentrations (IC(50)) of licochalcone A for these enzymes were at least 20 times higher than that for FRD. The IC(50) of licochalcone A for SDH and NDH in human peripheral blood mononuclear cells were at least 70 times higher than that for FRD. These findings indicate that FRD, one of the enzymes of the parasite respiratory chain, might be the specific target for the chalcones tested. Since FRD exists in the Leishmania parasite and does not exist in mammalian cells, it could be an excellent target for antiprotozoal drugs.
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