In vitro additive interaction between ketoconazole and antimony against intramacrophage Leishmania (Leishmania) amazonensis amastigotes

Leishmaniasis is a group of diseases caused by protozoa of Leishmania genus. The currently available treatments for this disease are expensive, present high toxicity and are associated to difficulties of healing and parasite resistance. Therefore, the development of strategies for leishmaniasis trea...

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Bibliographic Details
Published in:PloS one 2017-06, Vol.12 (6), p.e0180530-e0180530
Main Authors: Nunes, Débora Cristina de Oliveira, Bispo-da-Silva, Luiz Borges, Napolitano, Danielle Reis, Costa, Mônica Soares, Figueira, Márcia Moura Nunes Rocha, Rodrigues, Renata Santos, Rodrigues, Veridiana de Melo, Yoneyama, Kelly Aparecida Geraldo
Format: Article
Language:English
Subjects:
Amastigotes
Animals
Antifungal agents
Antimony
Antimony - administration & dosage
Antimony - pharmacology
Biocompatibility
Biology and Life Sciences
Care and treatment
Cytotoxicity
Diseases
Dosage
Dosage and administration
Drug resistance
Drug Synergism
Drug therapy
Drugs
Effectiveness
Experiments
Female
Healing
In vitro methods and tests
In Vitro Techniques
In vivo methods and tests
Ketoconazole
Ketoconazole - administration & dosage
Ketoconazole - pharmacology
Leishmania - drug effects
Leishmaniasis
Medicine and Health Sciences
Mice
Mice, Inbred BALB C
Parasite resistance
Parasites
Parasitic diseases
Penicillin
Pharmaceutical industry
Physical Sciences
Protozoa
Therapy
Toxicity
Vector-borne diseases
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Summary:Leishmaniasis is a group of diseases caused by protozoa of Leishmania genus. The currently available treatments for this disease are expensive, present high toxicity and are associated to difficulties of healing and parasite resistance. Therefore, the development of strategies for leishmaniasis treatment is indispensable and includes reposition of existing drugs, as well as drug combination therapy. The aim of this study was to assess the nature of ketoconazole and antimony association on the cytotoxic effect against Leishmania (Leishmania) amazonensis amastigotes. The calculated mean sum of fractional 50% inhibitory concentration ([Formula: see text]ΣFIC50) was 2.54 and 1.43 for free and intracellular amastigotes, respectively, values that suggest an additive interaction between ketoconazole and antimony concerning to Leishmania toxicity only in the intramacrophage parasite form. Despite the clinical efficacy of ketoconazole-antimony combination has been shown in the literature, our study is the first to describe the nature of ketoconazole-antimony interaction against L. (L.) amazonensis amastigotes. Moreover, our results point out the need for future in vivo studies to confirm the nature of ketoconazole-antimony interaction and also to determine possible effective dosage regimens related to ketoconazole administration in association with the optimal lower dose of antimony.
ISSN:1932-6203
1932-6203
DOI:10.1371/journal.pone.0180530