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β-Nitrostyrenes as Potential Anti-leishmanial Agents
Development of new therapeutic approach to treat leishmaniasis has become a priority. In the present study, the antileishmanial effect of β-nitrostyrenes was investigated against in vitro promastigotes and amastigotes. A series of β-nitrostyrenes have been synthesized by using Henry reaction and wer...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5007854/ https://www.ncbi.nlm.nih.gov/pubmed/27635124 http://dx.doi.org/10.3389/fmicb.2016.01379 |
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author | Shafi, Syed Afrin, Farhat Islamuddin, Mohammad Chouhan, Garima Ali, Intzar Naaz, Faatima Sharma, Kalicharan Zaman, Mohammad S. |
author_facet | Shafi, Syed Afrin, Farhat Islamuddin, Mohammad Chouhan, Garima Ali, Intzar Naaz, Faatima Sharma, Kalicharan Zaman, Mohammad S. |
author_sort | Shafi, Syed |
collection | PubMed |
description | Development of new therapeutic approach to treat leishmaniasis has become a priority. In the present study, the antileishmanial effect of β-nitrostyrenes was investigated against in vitro promastigotes and amastigotes. A series of β-nitrostyrenes have been synthesized by using Henry reaction and were evaluated for their antimicrobial activities by broth microdilution assay and in vitro antileishmanial activities against Leishmania donovani promastigotes by following standard guidelines. The most active compounds were futher evaluated for their in vitro antileishmanial activities against intracellular amastigotes. Among the tested β-nitrostyrenes, compounds 7, 8, 9, 12, and 17 exhibited potential activities (MICs range, 0.25–8 μg/mL) against clinically significant human pathogenic fungi. However, the microbactericidal concentrations (MBCs) and the microfungicidal concentrations (MFCs) were found to be either similar or only two-fold greater than the MICs. Anti-leishmanial results demonstrated that compounds 9, 12, 14, and 18 were found to be most active among the tested samples and exhibited 50% inhibitory concentration (IC(50)) by 23.40 ± 0.71, 37.83 ± 3.74, 40.50 ± 1.47, 55.66 ± 2.84 nM against L. donovani promastigotes and 30.5 ± 3.42, 21.46 ± 0.96, 26.43 ± 2.71, and 61.63 ± 8.02 nM respectively against intracellular L. donovani promastigotes amastigotes respectively which are comparable with standard AmB (19.60 ± 1.71 nM against promastigotes and 27.83 ± 3.26 nM against amastigotes). Compounds 9, 12, 14, and 18 were found to have potent in vitro leishmanicidal activity against L. donovani and found to be non-toxic against mammalian macrophages even at a concentration of 25 μM. Nitric oxide (NO) estimation studies reveals that these compounds are moderately inducing NO levels. |
format | Online Article Text |
id | pubmed-5007854 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-50078542016-09-15 β-Nitrostyrenes as Potential Anti-leishmanial Agents Shafi, Syed Afrin, Farhat Islamuddin, Mohammad Chouhan, Garima Ali, Intzar Naaz, Faatima Sharma, Kalicharan Zaman, Mohammad S. Front Microbiol Microbiology Development of new therapeutic approach to treat leishmaniasis has become a priority. In the present study, the antileishmanial effect of β-nitrostyrenes was investigated against in vitro promastigotes and amastigotes. A series of β-nitrostyrenes have been synthesized by using Henry reaction and were evaluated for their antimicrobial activities by broth microdilution assay and in vitro antileishmanial activities against Leishmania donovani promastigotes by following standard guidelines. The most active compounds were futher evaluated for their in vitro antileishmanial activities against intracellular amastigotes. Among the tested β-nitrostyrenes, compounds 7, 8, 9, 12, and 17 exhibited potential activities (MICs range, 0.25–8 μg/mL) against clinically significant human pathogenic fungi. However, the microbactericidal concentrations (MBCs) and the microfungicidal concentrations (MFCs) were found to be either similar or only two-fold greater than the MICs. Anti-leishmanial results demonstrated that compounds 9, 12, 14, and 18 were found to be most active among the tested samples and exhibited 50% inhibitory concentration (IC(50)) by 23.40 ± 0.71, 37.83 ± 3.74, 40.50 ± 1.47, 55.66 ± 2.84 nM against L. donovani promastigotes and 30.5 ± 3.42, 21.46 ± 0.96, 26.43 ± 2.71, and 61.63 ± 8.02 nM respectively against intracellular L. donovani promastigotes amastigotes respectively which are comparable with standard AmB (19.60 ± 1.71 nM against promastigotes and 27.83 ± 3.26 nM against amastigotes). Compounds 9, 12, 14, and 18 were found to have potent in vitro leishmanicidal activity against L. donovani and found to be non-toxic against mammalian macrophages even at a concentration of 25 μM. Nitric oxide (NO) estimation studies reveals that these compounds are moderately inducing NO levels. Frontiers Media S.A. 2016-09-01 /pmc/articles/PMC5007854/ /pubmed/27635124 http://dx.doi.org/10.3389/fmicb.2016.01379 Text en Copyright © 2016 Shafi, Afrin, Islamuddin, Chouhan, Ali, Naaz, Sharma and Zaman. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Microbiology Shafi, Syed Afrin, Farhat Islamuddin, Mohammad Chouhan, Garima Ali, Intzar Naaz, Faatima Sharma, Kalicharan Zaman, Mohammad S. β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title | β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title_full | β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title_fullStr | β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title_full_unstemmed | β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title_short | β-Nitrostyrenes as Potential Anti-leishmanial Agents |
title_sort | β-nitrostyrenes as potential anti-leishmanial agents |
topic | Microbiology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5007854/ https://www.ncbi.nlm.nih.gov/pubmed/27635124 http://dx.doi.org/10.3389/fmicb.2016.01379 |
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