Literature DB >> 26902763

Transmission-Blocking Potential of MEFAS, a Hybrid Compound Derived from Artesunate and Mefloquine.

Julia Penna-Coutinho1, Maria Jesús Almela2, Celia Miguel-Blanco2, Esperanza Herreros2, Paula M Sá3, Núbia Boechat3, Antoniana Ursine Krettli4.   

Abstract

Most antimalarial drugs target asexual parasites without reducing gametocyte formation or development. Drugs with dual roles, i.e., those that can target both asexual parasites and gametocytes, would improve the control of malaria. In the current study, MEFAS, a hybrid drug derived from mefloquine and artesunate that has been shown to be an active blood schizonticidal drug, was assessed to determine its ability to block the infectivity of Plasmodium falciparum gametocytes. MEFAS was 280 and 15 times more effective than mefloquine alone and artesunate alone, respectively.
Copyright © 2016, American Society for Microbiology. All Rights Reserved.

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Year:  2016        PMID: 26902763      PMCID: PMC4862484          DOI: 10.1128/AAC.02216-15

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  17 in total

1.  Complete in vitro maturation of Plasmodium falciparum gametocytes.

Authors:  T Ifediba; J P Vanderberg
Journal:  Nature       Date:  1981-11-26       Impact factor: 49.962

2.  Male and female Plasmodium falciparum mature gametocytes show different responses to antimalarial drugs.

Authors:  Michael J Delves; Andrea Ruecker; Ursula Straschil; Jöel Lelièvre; Sara Marques; María José López-Barragán; Esperanza Herreros; Robert E Sinden
Journal:  Antimicrob Agents Chemother       Date:  2013-04-29       Impact factor: 5.191

3.  Imaging-based high-throughput screening assay to identify new molecules with transmission-blocking potential against Plasmodium falciparum female gamete formation.

Authors:  Celia Miguel-Blanco; Joël Lelièvre; Michael J Delves; Ana I Bardera; Jesús L Presa; María José López-Barragán; Andrea Ruecker; Sara Marques; Robert E Sinden; Esperanza Herreros
Journal:  Antimicrob Agents Chemother       Date:  2015-03-23       Impact factor: 5.191

4.  Thiostrepton and derivatives exhibit antimalarial and gametocytocidal activity by dually targeting parasite proteasome and apicoplast.

Authors:  Makoah N Aminake; Sebastian Schoof; Ludmilla Sologub; Monika Leubner; Marc Kirschner; Hans-Dieter Arndt; Gabriele Pradel
Journal:  Antimicrob Agents Chemother       Date:  2011-01-18       Impact factor: 5.191

5.  Revisiting the circulation time of Plasmodium falciparum gametocytes: molecular detection methods to estimate the duration of gametocyte carriage and the effect of gametocytocidal drugs.

Authors:  Teun Bousema; Lucy Okell; Seif Shekalaghe; Jamie T Griffin; Sabah Omar; Patrick Sawa; Colin Sutherland; Robert Sauerwein; Azra C Ghani; Chris Drakeley
Journal:  Malar J       Date:  2010-05-24       Impact factor: 2.979

6.  Human malaria parasites in continuous culture.

Authors:  W Trager; J B Jensen
Journal:  Science       Date:  1976-08-20       Impact factor: 47.728

Review 7.  Hybrid drugs for malaria.

Authors:  J J Walsh; A Bell
Journal:  Curr Pharm Des       Date:  2009       Impact factor: 3.116

8.  Synthesis, antimalarial activity, and intracellular targets of MEFAS, a new hybrid compound derived from mefloquine and artesunate.

Authors:  Fernando de Pilla Varotti; Ana Cristina C Botelho; Anderson Assunção Andrade; Renata C de Paula; Elaine M S Fagundes; Alessandra Valverde; Lúcia M U Mayer; Jorge Souza Mendonça; Marcus V N de Souza; Núbia Boechat; Antoniana Ursine Krettli
Journal:  Antimicrob Agents Chemother       Date:  2008-08-18       Impact factor: 5.191

9.  Methemoglobinemia and adverse events in Plasmodium vivax malaria patients associated with high doses of primaquine treatment.

Authors:  Jaime Carmona-Fonseca; Gonzalo Alvarez; Amanda Maestre
Journal:  Am J Trop Med Hyg       Date:  2009-02       Impact factor: 2.345

10.  Recombinant Pfs25 protein of Plasmodium falciparum elicits malaria transmission-blocking immunity in experimental animals.

Authors:  P J Barr; K M Green; H L Gibson; I C Bathurst; I A Quakyi; D C Kaslow
Journal:  J Exp Med       Date:  1991-11-01       Impact factor: 14.307

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  3 in total

1.  Commercial drugs containing flavonoids are active in mice with malaria and in vitro against chloroquine-resistant Plasmodium falciparum.

Authors:  Julia Penna-Coutinho; Anna Cc Aguiar; Antoniana Ursine Krettli/
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Review 2.  The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.

Authors:  Luiz C S Pinheiro; Lívia M Feitosa; Marilia O Gandi; Flávia F Silveira; Nubia Boechat
Journal:  Molecules       Date:  2019-11-13       Impact factor: 4.411

3.  Antiplasmodial activities of dyes against Plasmodium falciparum asexual and sexual stages: Contrasted uptakes of triarylmethanes Brilliant green, Green S (E142), and Patent Blue V (E131) by erythrocytes.

Authors:  Louis-Jérôme Leba; Jean Popovici; Yannick Estevez; Stéphane Pelleau; Eric Legrand; Lise Musset; Christophe Duplais
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2017-08-02       Impact factor: 4.077

  3 in total

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