alexa In Vivo Evaluation of Leishmanicidal Activity of Benzop
ISSN: 2161-0444

Medicinal chemistry
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Research Article

In Vivo Evaluation of Leishmanicidal Activity of Benzophenone Derivatives by qPCR

Fabio Antonio Colombo1*, Rayssa Azara Reis1, Juliana Barbosa Nunes1, Danielle Ferreira Dias2, Marcelo Henrique dos Santos2, Claudio Viegas Junior3 and Marcos José Marques1

1Department of Pathology and Parasitology, Laboratory of Molecular Biology of Microorganisms, UNIFAL-MG, Rua Gabriel Monteiro da Silva, 700, 37130-000, Alfenas-MG, Brazil

2Laboratory of Phytochemistry and Medicinal Chemistry, UNIFAL-MG, Rua Gabriel Monteiro da Silva, 700, 37130-000, Alfenas-MG, Brazil

3Laboratory of Research in Medicinal Chemistry, Institute of Chemistry, UNIFAL-MG, Avenida Jovino Fernandes Sales, 2600, 37130-000, Alfenas-MG, Brazil

*Corresponding Author:
Fabio Antonio Colombo
Faculty of Pharmaceutical Sciences
Department of Pathology and Parasitology
University Federal of Alfenas
PO Box 37130-000, Alfenas, Brazil
Tel: +5503537019534
E-mail:
[email protected]

Received Date: May 04, 2017 Accepted Date: May 18, 2017 Published Date: May 25, 2017

Citation: Colombo FA, Reis RA, Nunes JB, Dias DF, dos Santos MH, et al. (2017) in vivo Evaluation of Leishmanicidal Activity of Benzophenone Derivatives by qPCR. Med Chem (Los Angeles) 7: 890-893. doi: 10.4172/2161-0444.1000448

Copyright: © 2017 Colombo FA, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

In many tropical areas, infections by Leishmania species are endemic and include visceral leishmaniasis (VL), which is often fatal if untreated. Outside India, VL treatment and control are based on long-term administration of highly toxic pentavalent antimonials. Previously, we described the synthesis and in vitro leishmanicidal activity of a series of nine benzophenone derivatives with low toxicity towards murine macrophages. Here in, we report the in vivo evaluation of the most promising active compounds of that series in an experimental model of established VL by L. (L). infantum chagasi in hamsters. Importantly, parasite DNA (amastigote form) quantification in infected tissues was performed by real time PCR, for improved detection accuracy and speed. Compounds 2-Hydroxy-4- O-(3,3-dimethyl)-allylbenzophenone (LFQM-117 (1)), 4-O-(3,3-Dimethyl)-allylbenzophenone (LFQM-120 (2)) and 4,4′-Di-methoxybenzophenone (LFQM-121 (3)) were administered as oral suspensions (50 mg/kg/day) for 10 days, after 50 days of parasite inoculation, and their efficacy was compared to pentavalent antimonial Glucantime (GLU). Compound 1 significantly reduced the number of parasites in the spleen (1.64 × 102 amastigotes/g, vs. 1.16 × 106 amastigotes/g in the untreated control), while compound 2 significantly reduced (p<0.05) the number of parasites in the liver (1.28 × 104 amastigotes/g, vs. 1.76 × 105 amastigotes/g in the untreated control) of infected animals. Glucantime was the most effective in the treatment of infected animals (1.15 × 101 and 3.20 × 102 amastigotes/g in the spleen and liver, respectively), but with higher toxicity then the most active compounds LFQM-117 (1) and LFQM-120 (2).

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