ArticleThe Journal of antimicrobial chemotherapy2013
Nelfinavir is effective in inhibiting the multiplication and aspartic peptidase activity of Leishmania species, including strains obtained from HIV-positive patients.
Article in The Journal of antimicrobial chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 33 citations in OpenAlex.
- Insights to the HIV-associated visceral leishmaniasis clinical outcome: lessons learned about immune mediated disorders.Frontiers in immunology · 2025Review
- Leishmania Infection among HIV-Infected Patients in a Southern Province of Thailand: A Cross-Sectional Study.The American journal of tropical medicine and hygiene · 2024Article
- Silver(I) 1,10-Phenanthroline Complexes Are Active againstJournal of fungi (Basel, Switzerland) · 2023Article
- Aspartic peptidase ofJournal of enzyme inhibition and medicinal chemistry · 2020Article
- In vitro effectivity of three approved drugs and their synergistic interaction against Leishmania infantum.Biomedica : revista del Instituto Nacional de Salud · 2020Article
- Miltefosine-Lopinavir Combination Therapy AgainstFrontiers in cellular and infection microbiology · 2019Article
- Docking simulation between HIV peptidase inhibitors and Trypanosoma cruzi aspartyl peptidase.BMC research notes · 2018Article
- Lopinavir, an HIV-1 peptidase inhibitor, induces alteration on the lipid metabolism of Leishmania amazonensis promastigotes.Parasitology · 2018Article
- Article
- The Dialogue of the Host-Parasite Relationship: Leishmania spp. and Trypanosoma cruzi Infection.BioMed research international · 2015Review
- Oral effectiveness of PMIC4, a novel hydroxyethylpiperazine analogue, in Leishmania amazonensis.International journal for parasitology. Drugs and drug resistance · 2014Article
- Decoding the anti-Trypanosoma cruzi action of HIV peptidase inhibitors using epimastigotes as a model.PloS one · 2014Article
- Aspartic peptidases of human pathogenic trypanosomatids: perspectives and trends for chemotherapy.Current medicinal chemistry · 2013Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectivesThere is a general lack of effective and non-toxic chemotherapeutic agents for leishmaniasis and there is as yet no study about the effect of HIV peptidase inhibitors (HIV PIs) on Leishmania/HIV-coinfected patients. In the present work, we performed a comparative analysis of the spectrum of action of HIV PIs on different Leishmania spp., including strains obtained from HIV-positive patients receiving or not receiving antiretroviral treatment.
methodsThe effects of nelfinavir and saquinavir on Leishmania proliferation were assessed by means of a colorimetric assay (MTT). Subsequently, the effect of nelfinavir on aspartic peptidase activity from Leishmania spp. was assessed by following the degradation of the fluorogenic substrate MCA-G-K-P-I-L-F-F-R-L-K-DNP-Arg-NH(2).
resultsNelfinavir was capable of significantly reducing the multiplication of many Leishmania reference strains and isolates obtained from HIV-positive patients receiving or not receiving antiretroviral treatment. Leishmania major growth was inhibited by ≈ 50%, while all other flagellates were strongly inhibited (at least 94%), except for a Leishmania chagasi strain obtained from an HIV-positive patient under treatment with highly active antiretroviral therapy (HAART). Culture of this isolate in the presence of nelfinavir induced a considerable reduction in the aspartic peptidase activity. In addition, nelfinavir was also capable of inhibiting the aspartic peptidase activity of all Leishmania strains tested.
conclusionsThe present data contribute to the study of the effect of HIV PIs on Leishmania infection and add new insights into the possibility of exploiting aspartic peptidases as promising targets in order to generate novel medications to treat leishmaniasis.
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