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Parasitology Research

, Volume 112, Issue 4, pp 1523–1527 | Cite as

Biological assay of a novel quinoxalinone with antimalarial efficacy on Plasmodium yoelii yoelii

  • Norma Rivera
  • Yovani Marrero Ponce
  • Vicente J. Arán
  • Cecilia Martínez
  • Filiberto Malagón
Original Paper

Abstract

Compound 1-methyl-7-nitro-4-(5-(piperidin-1-yl)pentyl)-3,4-dihydroquinoxalin-2(1H)-one (VAM2-6) was evaluated against a blood-induced infection with chloroquine-sensitive Plasmodium yoelii yoelii lethal strain in CD1 mice in a 4-day test scheme. LD50 of the compound was 56.51 mg/kg and LD10 was 20.58 mg/kg (taken as the highest dose). Animals were treated by oral gavage of 20, 10, and 5 mg/kg. Mice in the untreated control group showed a progressively increasing parasitemia leading to mouse death on 6 days post-infection; in this group, all mice showed parasites in the blood on the fifth day of sampling; the mean parasitemia on that day was 19.4 %. A 4-day dosage of 20 mg/kg of VAM2-6 showed a 97 % chemosuppression of total parasitemia on the fifth day, a 28 days survival time, and 20 % of cured animals. A 4-day dosage of 10 and 5 mg/kg showed 85 and 37 %, respectively, chemosuppression of total parasitemia on the fifth day; but all mice died from days 6 to 9 post-infection with increasing parasitemia. Mice treated with chloroquine at 5 mg/kg survived during the experiment. The results obtained in this study showed that the infection outcome of P. yoelii yoelii-infected mice is affected by VAM2-6 compound by slowing down the parasite replication, retarding the patency time, and increasing their survival time. Although compound VAM2-6 was active at higher doses than chloroquine, these results leaves a door open to the study of its structure in order to improve its antimalarial activity.

Keywords

Malaria Quinoline Chloroquine Antimalarial Drug Quinoxaline 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgments

This research was partially supported by Department of Microbiology and Parasitology, Faculty of Medicine, UNAM and project PAPIIT-DGAPA IN-229611, UNAM. The Spanish Ministry of Science and Innovation (MICINN, ref. SAF2009-10399) is also gratefully acknowledged for partially supporting this paper. We also appreciate the technical assistance of Enrique Pinzón Estrada.

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Copyright information

© Springer-Verlag Berlin Heidelberg 2013

Authors and Affiliations

  • Norma Rivera
    • 1
  • Yovani Marrero Ponce
    • 2
  • Vicente J. Arán
    • 3
  • Cecilia Martínez
    • 1
  • Filiberto Malagón
    • 1
  1. 1.Laboratorio de Malariología, Departamento de Microbiología y Parasitología, Facultad de MedicinaUniversidad Nacional Autónoma de MéxicoMéxicoMexico
  2. 2.Unit of Computer-Aided Molecular “Biosilico” Discovery and Bioinformatic Research, Faculty of Chemistry-PharmacyUniversidad Central “Marta Abreu” de Las VillasSanta ClaraCuba
  3. 3.Instituto de Química Médica, CSICMadridSpain

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