ArticlePLoS neglected tropical diseases2012
In vitro and in vivo activity of a palladacycle complex on Leishmania (Leishmania) amazonensis.
Article in PLoS neglected tropical diseases, 2012. 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, 48 citations in OpenAlex.
- Platinum Group Metals against Parasites: State of the Art and Future Perspectives.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- New Insights into the Mechanism of Action of the Cyclopalladated Complex (CP2) inAntimicrobial agents and chemotherapy · 2022Article
- In Vitro Antileishmanial and Antischistosomal Activities of Anemonin Isolated from the Fresh Leaves ofMolecules (Basel, Switzerland) · 2021Article
- Amentoflavone as an Ally in the Treatment of Cutaneous Leishmaniasis: Analysis of Its Antioxidant/Prooxidant Mechanisms.Frontiers in cellular and infection microbiology · 2021Article
- Protective Cellular Immune Response Induction for Cutaneous Leishmaniasis by a New Immunochemotherapy Schedule.Frontiers in immunology · 2020Article
- Axenic amastigote cultivation and in vitro development of Leishmania orientalis.Parasitology research · 2019Article
- Cysteine proteases in protozoan parasites.PLoS neglected tropical diseases · 2018Review
- Efficacy of FourMedicines (Basel, Switzerland) · 2018Article
- Leishmanicidal and Immunomodulatory Activities of the Palladacycle Complex DPPE 1.1, a Potential Candidate for Treatment of Cutaneous Leishmaniasis.Frontiers in microbiology · 2018Article
- In Vitro antileishmania activity of sesquiterpene-rich essential oils from Nectandra species.Pharmaceutical biology · 2017Article
- VOSalophen: a vanadium complex with a stilbene derivative-induction of apoptosis, autophagy, and efficiency in experimental cutaneous leishmaniasis.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2017Article
- Efficacy of a Binuclear Cyclopalladated Compound Therapy for Cutaneous Leishmaniasis in the Murine Model of Infection with Leishmania amazonensis and Its Inhibitory Effect on Topoisomerase 1B.Antimicrobial agents and chemotherapy · 2017Article
- Treatment ofFrontiers in microbiology · 2017Article
- Antileishmanial Activity and Structure-Activity Relationship of Triazolic Compounds Derived from the Neolignans Grandisin, Veraguensin, and Machilin G.Molecules (Basel, Switzerland) · 2016Article
- Immucillins Impair Leishmania (L.) infantum chagasi and Leishmania (L.) amazonensis Multiplication In Vitro.PloS one · 2015Article
- In vitro activity of the hydroethanolic extract and biflavonoids isolated from Selaginella sellowii on Leishmania (Leishmania) amazonensis.Memorias do Instituto Oswaldo Cruz · 2014Article
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
- In-silico Leishmania target selectivity of antiparasitic terpenoids.Molecules (Basel, Switzerland) · 2013Article
- In vitro Evaluation of the Potent Antileishmanial Activity ofIranian journal of pharmaceutical research : IJPRArticle
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundAntitumor cyclopalladated complexes with low toxicity to laboratory animals have shown leishmanicidal effect. These findings stimulated us to test the leishmanicidal property of one palladacycle compound called DPPE 1.2 on Leishmania (Leishmania) amazonensis, an agent of simple and diffuse forms of cutaneous leishmaniasis in the Amazon region, Brazil. METHODOLOGY/PRINCIPAL
findingsPromastigotes of L. (L.) amazonensis and infected bone marrow-derived macrophages were treated with different concentrations of DPPE 1.2. In in vivo assays foot lesions of L. (L.) amazonensis-infected BALB/c mice were injected subcutaneously with DPPE 1.2 and control animals received either Glucantime or PBS. The effect of DPPE 1.2 on cathepsin B activity of L. (L.) amazonensis amastigotes was assayed spectrofluorometrically by use of fluorogenic substrates. The main findings were: 1) axenic L. (L.) amazonensis promastigotes were destroyed by nanomolar concentrations of DPPE 1.2 (IC50 = 2.13 nM); 2) intracellular parasites were killed by DPPE 1.2 (IC50 = 128.35 nM), and the drug displayed 10-fold less toxicity to macrophages (CC50 = 1,267 nM); 3) one month after intralesional injection of DPPE 1.2 infected BALB/c mice showed a significant decrease of foot lesion size and a reduction of 97% of parasite burdens when compared to controls that received PBS; 4) DPPE 1.2 inhibited the cysteine protease activity of L. (L.) amazonensis amastigotes and more significantly the cathepsin B activity. CONCLUSIONS/SIGNIFICANCE: The present results demonstrated that DPPE 1.2 can destroy L. (L.) amazonensis in vitro and in vivo at concentrations that are non toxic to the host. We believe these findings support the potential use of DPPE 1.2 as an alternative choice for the chemotherapy of leishmaniasis.
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