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In vitro and in vivo activity of major constituents from Pluchea carolinensis against Leishmania amazonensis

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Abstract

The search for new therapeutic agents from natural sources has been a constant for the treatment of diseases such as leishmaniasis. Herein, in vitro and in vivo pharmacological activities of pure major phenolic constituents (caffeic acid, chlorogenic acid, ferulic acid, quercetin, and rosmarinic acid) from Pluchea carolinensis against Leishmania amazonensis are presented. Pure compounds showed inhibitory activity against promastigotes (IC50 = 0.2–0.9 μg/mL) and intracellular amastigotes (IC50 = 1.3–2.9 μg/mL). Four of them were selected after testing against macrophages of BALB/c mice: caffeic acid, ferulic acid, quercetin, and rosmarinic acid, with selective indices of 11, 17, 10, and 20, respectively. Ferulic acid, rosmarinic acid, and caffeic acid controlled lesion size development and parasite burden in footpads from BALB/c experimentally infected mice, after five injections of compounds by intralesional route at 30 mg/kg every 4 days. Pure compounds from P. carolinensis demonstrated antileishmanial properties.

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Abbreviations

DMSO:

Dimethyl sulfoxide

HFBS:

Heat-inactivated fetal bovine serum

IC50 :

Concentration at which inhibition of the activity was 50 %

MTT:

3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide

PBS:

Phosphate-buffered saline

p.i.:

Post-infection

SD:

Standard deviation

SI:

Selectivity indices

TDR:

Tropical Diseases Research

WHO:

World Health Organization

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The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Antwerp University, Antwerp, Belgium

    Elly Montrieux, Louis Maes & Paul Cos

  2. Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, CCS, Bl. A, Ilha do Fundão, 21.941-590 Rio de Janeiro, RJ, Brazil

    Wilmer H. Perera

  3. Parasitology Department, Institute of Tropical Medicine “Pedro Kouri”, Havana City, Cuba

    Marley García & Lianet Monzote

Authors
  1. Elly Montrieux
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  2. Wilmer H. Perera
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  3. Marley García
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  4. Louis Maes
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  5. Paul Cos
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  6. Lianet Monzote
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Correspondence to Lianet Monzote.

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Montrieux, E., Perera, W.H., García, M. et al. In vitro and in vivo activity of major constituents from Pluchea carolinensis against Leishmania amazonensis . Parasitol Res 113, 2925–2932 (2014). https://doi.org/10.1007/s00436-014-3954-1

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  • DOI: https://doi.org/10.1007/s00436-014-3954-1

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