In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis.
Rifampicin, discovered more than 50 years ago, represents the last novel class of antibiotics introduced for the first-line treatment of tuberculosis. Drugs in this class form part of a 6-month regimen that is ineffective against MDR and XDR TB, and incompatible with many antiretroviral drugs. Inves...
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doaj-e703023b58f14816a09d1ac4dbcf45822020-11-25T02:47:04ZengPublic Library of Science (PLoS)PLoS ONE1932-62032013-01-0185e6424210.1371/journal.pone.0064242In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis.Fernando R PavanGustavo V PoelhsitzLucas V P da CunhaMarilia I F BarbosaSergio R A LeiteAlzir A BatistaSang H ChoScott G FranzblauMariana S de CamargoFlávia A ResendeEliana A VarandaClarice Q F LeiteRifampicin, discovered more than 50 years ago, represents the last novel class of antibiotics introduced for the first-line treatment of tuberculosis. Drugs in this class form part of a 6-month regimen that is ineffective against MDR and XDR TB, and incompatible with many antiretroviral drugs. Investments in R&D strategies have increased substantially in the last decades. However, the number of new drugs approved by drug regulatory agencies worldwide does not increase correspondingly. Ruthenium complexes (SCAR) have been tested in our laboratory and showed promising activity against Mycobacterium tuberculosis. These complexes showed up to 150 times higher activity against MTB than its organic molecule without the metal (free ligand), with low cytotoxicity and high selectivity. In this study, promising results inspired us to seek a better understanding of the biological activity of these complexes. The in vitro biological results obtained with the SCAR compounds were extremely promising, comparable to or better than those for first-line drugs and drugs in development. Moreover, SCAR 1 and 4, which presented low acute toxicity, were assessed by Ames test, and results demonstrated absence of mutagenicity.http://europepmc.org/articles/PMC3665843?pdf=render |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Fernando R Pavan Gustavo V Poelhsitz Lucas V P da Cunha Marilia I F Barbosa Sergio R A Leite Alzir A Batista Sang H Cho Scott G Franzblau Mariana S de Camargo Flávia A Resende Eliana A Varanda Clarice Q F Leite |
spellingShingle |
Fernando R Pavan Gustavo V Poelhsitz Lucas V P da Cunha Marilia I F Barbosa Sergio R A Leite Alzir A Batista Sang H Cho Scott G Franzblau Mariana S de Camargo Flávia A Resende Eliana A Varanda Clarice Q F Leite In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. PLoS ONE |
author_facet |
Fernando R Pavan Gustavo V Poelhsitz Lucas V P da Cunha Marilia I F Barbosa Sergio R A Leite Alzir A Batista Sang H Cho Scott G Franzblau Mariana S de Camargo Flávia A Resende Eliana A Varanda Clarice Q F Leite |
author_sort |
Fernando R Pavan |
title |
In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. |
title_short |
In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. |
title_full |
In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. |
title_fullStr |
In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. |
title_full_unstemmed |
In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis. |
title_sort |
in vitro and in vivo activities of ruthenium(ii) phosphine/diimine/picolinate complexes (scar) against mycobacterium tuberculosis. |
publisher |
Public Library of Science (PLoS) |
series |
PLoS ONE |
issn |
1932-6203 |
publishDate |
2013-01-01 |
description |
Rifampicin, discovered more than 50 years ago, represents the last novel class of antibiotics introduced for the first-line treatment of tuberculosis. Drugs in this class form part of a 6-month regimen that is ineffective against MDR and XDR TB, and incompatible with many antiretroviral drugs. Investments in R&D strategies have increased substantially in the last decades. However, the number of new drugs approved by drug regulatory agencies worldwide does not increase correspondingly. Ruthenium complexes (SCAR) have been tested in our laboratory and showed promising activity against Mycobacterium tuberculosis. These complexes showed up to 150 times higher activity against MTB than its organic molecule without the metal (free ligand), with low cytotoxicity and high selectivity. In this study, promising results inspired us to seek a better understanding of the biological activity of these complexes. The in vitro biological results obtained with the SCAR compounds were extremely promising, comparable to or better than those for first-line drugs and drugs in development. Moreover, SCAR 1 and 4, which presented low acute toxicity, were assessed by Ames test, and results demonstrated absence of mutagenicity. |
url |
http://europepmc.org/articles/PMC3665843?pdf=render |
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