ArticleAntimicrobial agents and chemotherapy2011
The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenase.
Article in Antimicrobial agents and chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 75 citations in OpenAlex.
- Plant-derived products as anti-leishmanials which target mitochondria: a review.Expert reviews in molecular medicine · 2025Review
- Immunotherapy and immunochemotherapy in combating visceral leishmaniasis.Frontiers in medicine · 2023Review
- Parasitological and immunological evaluation of a quinoline derivative salt incorporated into a polymeric micelle formulation against Leishmania infantum infection.Parasitology research · 2022Article
- Naphthoquinone as a New Chemical Scaffold for Leishmanicidal Inhibitors ofBiomedicines · 2022Article
- The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates.Molecules (Basel, Switzerland) · 2022Review
- Biological Evaluation and Mechanistic Studies of Quinolin-(1Antimicrobial agents and chemotherapy · 2021Article
- New Trends for Antimalarial Drugs: Synergism between Antineoplastics and Antimalarials on Breast Cancer Cells.Biomolecules · 2020Article
- Mode of action of a formulation containing hydrazones and saponins against leishmania spp. Role in mitochondria, proteases and reinfection process.International journal for parasitology. Drugs and drug resistance · 2020Article
- Current challenges in treatment options for visceral leishmaniasis in India: a public health perspective.Infectious diseases of poverty · 2016Review
- Experimental resistance to drug combinations in Leishmania donovani: metabolic and phenotypic adaptations.Antimicrobial agents and chemotherapy · 2015Article
- Mechanisms of action of substituted β-amino alkanols on Leishmania donovani.Antimicrobial agents and chemotherapy · 2015Article
- Plant-derived compounds in treatment of leishmaniasis.Iranian journal of veterinary research · 2015Review
- Induction of mitochondrial dysfunction and oxidative stress in Leishmania donovani by orally active clerodane diterpene.Antimicrobial agents and chemotherapy · 2014Article
- 4-amino bis-pyridinium derivatives as novel antileishmanial agents.Antimicrobial agents and chemotherapy · 2014Article
- Alkyl galactofuranosides strongly interact with Leishmania donovani membrane and provide antileishmanial activity.Antimicrobial agents and chemotherapy · 2014Article
- The double-edged sword in pathogenic trypanosomatids: the pivotal role of mitochondria in oxidative stress and bioenergetics.BioMed research international · 2014Review
- Drug resistance in leishmaniasis: Newer developments.Tropical parasitology · 2014Review
- Article
- Visceral leishmaniasis treatment: What do we have, what do we need and how to deliver it?International journal for parasitology. Drugs and drug resistance · 2012Review
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Authors and funding
6 authors at 2 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
The 8-aminoquinoline analogue sitamaquine (SQ) is an oral antileishmanial drug currently undergoing phase 2b clinical trials for the treatment of visceral leishmaniasis. In the present study, we investigated the mechanism of action of this drug in Leishmania donovani promastigotes. SQ causes a dose-dependent inhibition of complex II (succinate dehydrogenase) of the respiratory chain in digitonin-permeabilized promastigotes, together with a drop in intracellular ATP levels and a decrease of the mitochondrial electrochemical potential. This is associated with increases of reactive oxygen species and intracellular Ca(2+) levels, a higher percentage of the population with sub-G(1) DNA content, and exposure of phosphatidylserine. Taken together, these results support a lethal mechanism for SQ that involves inhibition of the respiratory chain complex II, which in turn triggers oxidative stress and finally leads to an apoptosis-like death of Leishmania parasites.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.