ArticleAntimicrobial agents and chemotherapy2009
In vitro susceptibilities of Leishmania donovani promastigote and amastigote stages to antileishmanial reference drugs: practical relevance of stage-specific differences.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 120 papers, 1 of them a synthesis that pooled it.
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120 citing papers in PubMed, 1 synthesis or guideline pooled it, 229 citations in OpenAlex.
- A Systematic Review of Curcumin and its Derivatives as Valuable Sources of Antileishmanial Agents.Acta parasitologica · 2021Pooled it
- Novel Synthetic Chalcones Display Potent Anti-ACS omega · 2026Article
- Assessing Designed Model Membrane-Targeting Peptides Found as Potential Molecular Scaffolds against Cutaneous Leishmaniasis.ACS omega · 2026Article
- Systems-Driven Identification and Experimental Validation of Actinomycetes-Derived Secondary Metabolites as Promising Antileishmanial Agents TargetingACS medicinal chemistry letters · 2026Article
- A Dual-Reporter Fluorescence-Luminescence Assay for Drug Screening in Promastigote and Intracellular Amastigote Stages ofMolecules (Basel, Switzerland) · 2026Article
- A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 2: from molecule to confirmed hit.The Journal of antimicrobial chemotherapy · 2026Review
- In vitro drug susceptibility of Leishmania donovani from visceral leishmaniasis patients with and without HIV coinfection in Northwestern Ethiopia.Scientific reports · 2025Article
- In Vitro and Ultrastructural Evaluation of the Cytotoxic and Antileishmanial Activities of Thiosemicarbazone Compounds Against Promastigotes and Axenic Amastigotes ofTropical medicine and infectious disease · 2025Article
- Dual immunomodulatory and antileishmanial potential of TLR7/8 agonists againstInfection and immunity · 2025Article
- Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library.Molecules (Basel, Switzerland) · 2025Article
- Antiparasitic and Antifungal Activities of Cetyl-Maritima, a NewAntibiotics (Basel, Switzerland) · 2025Article
- Evaluation of Beauvericin's activity and mode of action against all life stages ofFrontiers in cellular and infection microbiology · 2025Article
- Susceptibility ofTropical medicine and infectious disease · 2024Article
- Identification of Novel Antileishmanial Chemotypes By High-Throughput Virtual and In Vitro Screening.Acta parasitologica · 2024Article
- Antimony susceptibleMicrobiology spectrum · 2024Article
- Dual Antitubercular and Antileishmanial Profiles of Quinoxaline Di-Pharmaceuticals (Basel, Switzerland) · 2024Article
- Induced pluripotent stem cell-derived human macrophages as an infection model for Leishmania donovani.PLoS neglected tropical diseases · 2024Article
- Imidazo[1,2-ACS omega · 2023Article
- Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Improved synthesis of deoxyalpinoid B and quantification of antileishmanial activity of deoxyalpinoid B and sulforaphane.Bioorganic & medicinal chemistry · 2023Article
60 more citing papers are in PubMed but not listed here.
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6 authors at 1 institution in 1 country.
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Abstract
The in vitro susceptibilities of the reference strain Leishmania donovani MHOM/ET/67/L82 to sodium stibogluconate, amphotericin B, miltefosine, and the experimental compound PX-6518 were determined for extracellular log-phase promastigotes, established axenic amastigotes, fresh spleen-derived amastigotes, and intracellular amastigotes in primary mouse peritoneal macrophages. Susceptibility to amphotericin B did not differ across the various axenic models (50% inhibitory concentrations [IC50], 0.6 to 0.7 microM), and amphotericin B showed slightly higher potency against intracellular amastigotes (IC50, 0.1 to 0.4 microM). A similar trend was observed for miltefosine, with comparable efficacies against the extracellular (IC50, 0.4 to 3.8 microM) and intracellular (IC50, 0.9 to 4.3 microM) stages. Sodium stibogluconate, used either as Pentostam or as a crystalline substance, was inactive against all axenic stages (IC50, >64 microg SbV/ml) but showed good efficacy against intracellular amastigotes (IC50, 22 to 28 microg SbV/ml); the crystalline substance was about two to three times more potent (IC50, 9 to 11 microg SbV/ml). The activity profile of PX-6518 was comparable to that of sodium stibogluconate, but at a much higher potency (IC50, 0.1 microg/ml). In conclusion, the differential susceptibility determines which in vitro models are appropriate for either drug screening or resistance monitoring of clinical field isolates. Despite the more complex and labor-intensive protocol, the current results support the intracellular amastigote model as the gold standard for in vitro Leishmania drug discovery research and for evaluation of the resistance of field strains, since it also includes host cell-mediated effects. Axenic systems can be recommended only for compounds for which no cellular mechanisms are involved, for example, amphotericin B and miltefosine.
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