Literature DB >> 21739037

The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil.

Eliane de Morais-Teixeira1, Quesia Souza Damasceno, Mariana Kolos Galuppo, Alvaro José Romanha, Ana Rabello.   

Abstract

The in vitro leishmanicidal activity of miltefosine® (Zentaris GmbH) was assessed against four medically relevant Leishmania species of Brazil: Leishmania (Leishmania) amazonensis, Leishmania (Viannia) braziliensis, Leishmania (Viannia) guyanensis and Leishmania (Leishmania) chagasi. The activity of miltefosine against these New World species was compared to its activity against the Old World strain, Leishmania (Leishmania) donovani, which is known to be sensitive to the effects of miltefosine. The IC50 and IC90 results suggested the New World species harboured similar in vitro susceptibilities to miltefosine; however, miltefosine was approximately 20 times more active against the Old World L. (L.) donovani than against the New World L. (L.) chagasi species. The selectivity index varied from 17.2-28.9 for the New World Leishmania species and up to 420.0 for L. (L.) donovani. The differences in susceptibility to miltefosine suggest that future clinical trials with this drug should include a laboratory pre-evaluation and a dose-defining step.

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Year:  2011        PMID: 21739037     DOI: 10.1590/s0074-02762011000400015

Source DB:  PubMed          Journal:  Mem Inst Oswaldo Cruz        ISSN: 0074-0276            Impact factor:   2.743


  21 in total

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2.  Mechanism of Action of Miltefosine on Leishmania donovani Involves the Impairment of Acidocalcisome Function and the Activation of the Sphingosine-Dependent Plasma Membrane Ca2+ Channel.

Authors:  Andrea K Pinto-Martinez; Jessica Rodriguez-Durán; Xenon Serrano-Martin; Vanessa Hernandez-Rodriguez; Gustavo Benaim
Journal:  Antimicrob Agents Chemother       Date:  2017-12-21       Impact factor: 5.191

3.  Alkyl galactofuranosides strongly interact with Leishmania donovani membrane and provide antileishmanial activity.

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Journal:  Antimicrob Agents Chemother       Date:  2014-01-27       Impact factor: 5.191

4.  An alternative in vitro drug screening test using Leishmania amazonensis transfected with red fluorescent protein.

Authors:  Marcele N Rocha; Célia M Corrêa; Maria N Melo; Stephen M Beverley; Olindo Assis Martins-Filho; Ana Paula Madureira; Rodrigo P Soares
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5.  Development of a semi-automated image-based high-throughput drug screening system.

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6.  Generation of luciferase-expressing Leishmania infantum chagasi and assessment of miltefosine efficacy in infected hamsters through bioimaging.

Authors:  Juliana Q Reimão; Jordana C Oliveira; Cristiana T Trinconi; Paulo C Cotrim; Adriano C Coelho; Silvia R B Uliana
Journal:  PLoS Negl Trop Dis       Date:  2015-02-13

7.  Computational study to discover potent phytochemical inhibitors against drug target, squalene synthase from Leishmania donovani.

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Journal:  Heliyon       Date:  2021-05-31

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Journal:  Front Cell Infect Microbiol       Date:  2021-06-04       Impact factor: 5.293

9.  Antileishmanial activity of the estrogen receptor modulator raloxifene.

Authors:  Juliana Q Reimão; Danilo C Miguel; Noemi N Taniwaki; Cristiana T Trinconi; Jenicer K U Yokoyama-Yasunaka; Silvia R B Uliana
Journal:  PLoS Negl Trop Dis       Date:  2014-05-08

10.  In vitro and in vivo miltefosine susceptibility of a Leishmania amazonensis isolate from a patient with diffuse cutaneous leishmaniasis.

Authors:  Adriano C Coelho; Cristiana T Trinconi; Carlos H N Costa; Silvia R B Uliana
Journal:  PLoS Negl Trop Dis       Date:  2014-07-17
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