In vitro activity and mode of action of phenolic compounds on Leishmania donovani.
BACKGROUND:Leishmaniasis is a disease caused by the protozoan parasite, Leishmania. The disease remains a global threat to public health requiring effective chemotherapy for control and treatment. In this study, the effect of some selected phenolic compounds on Leishmania donovani was investigated....
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ftdoajarticles:oai:doaj.org/article:e3fa5ae1437d46d0a30c22c254b47557 2023-05-15T15:15:53+02:00 In vitro activity and mode of action of phenolic compounds on Leishmania donovani. Christine Achiaa Antwi Cynthia Mmalebna Amisigo Jonathan Partt Adjimani Theresa Manful Gwira 2019-02-01T00:00:00Z https://doi.org/10.1371/journal.pntd.0007206 https://doaj.org/article/e3fa5ae1437d46d0a30c22c254b47557 EN eng Public Library of Science (PLoS) http://europepmc.org/articles/PMC6405172?pdf=render https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0007206 https://doaj.org/article/e3fa5ae1437d46d0a30c22c254b47557 PLoS Neglected Tropical Diseases, Vol 13, Iss 2, p e0007206 (2019) Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 article 2019 ftdoajarticles https://doi.org/10.1371/journal.pntd.0007206 2022-12-31T00:11:25Z BACKGROUND:Leishmaniasis is a disease caused by the protozoan parasite, Leishmania. The disease remains a global threat to public health requiring effective chemotherapy for control and treatment. In this study, the effect of some selected phenolic compounds on Leishmania donovani was investigated. The compounds were screened for their anti-leishmanial activities against promastigote and intracellular amastigote forms of Leishmania donovani. METHODOLOGY/PRINCIPAL FINDINGS:The dose dependent effect and cytotoxicity of the compounds were determined by the MTT assay. Flow cytometry was used to determine the effect of the compounds on the cell cycle. Parasite morphological analysis was done by microscopy and growth kinetic studies were conducted by culturing cells and counting at 24 hours intervals over 120 hours. The cellular levels of iron in promastigotes treated with compounds was determined by atomic absorption spectroscopy and the effect of compounds on the expression of iron dependent enzymes was investigated using RT-qPCR. The IC50 of the compounds ranged from 16.34 μM to 198 μM compared to amphotericin B and deferoxamine controls. Rosmarinic acid and apigenin were the most effective against the promastigote and the intracellular amastigote forms. Selectivity indexes (SI) of rosmarinic acid and apigenin were 15.03 and 10.45 respectively for promastigotes while the SI of 12.70 and 5.21 respectively was obtained for intracellular amastigotes. Morphologically, 70% of rosmarinic acid treated promastigotes showed rounded morphology similar to the deferoxamine control. About 30% of cells treated with apigenin showed distorted cell membrane. Rosmarinic acid and apigenin induced cell arrest in the G0/G1 phase in promastigotes. Elevated intracellular iron levels were observed in promastigotes when parasites were treated with rosmarinic acid and this correlated with the level of expression of iron dependent genes. CONCLUSIONS/SIGNIFICANCE:The data suggests that rosmarinic acid exerts its anti-leishmanial effect via ... Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic PLOS Neglected Tropical Diseases 13 2 e0007206 |
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Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
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Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 Christine Achiaa Antwi Cynthia Mmalebna Amisigo Jonathan Partt Adjimani Theresa Manful Gwira In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
topic_facet |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
description |
BACKGROUND:Leishmaniasis is a disease caused by the protozoan parasite, Leishmania. The disease remains a global threat to public health requiring effective chemotherapy for control and treatment. In this study, the effect of some selected phenolic compounds on Leishmania donovani was investigated. The compounds were screened for their anti-leishmanial activities against promastigote and intracellular amastigote forms of Leishmania donovani. METHODOLOGY/PRINCIPAL FINDINGS:The dose dependent effect and cytotoxicity of the compounds were determined by the MTT assay. Flow cytometry was used to determine the effect of the compounds on the cell cycle. Parasite morphological analysis was done by microscopy and growth kinetic studies were conducted by culturing cells and counting at 24 hours intervals over 120 hours. The cellular levels of iron in promastigotes treated with compounds was determined by atomic absorption spectroscopy and the effect of compounds on the expression of iron dependent enzymes was investigated using RT-qPCR. The IC50 of the compounds ranged from 16.34 μM to 198 μM compared to amphotericin B and deferoxamine controls. Rosmarinic acid and apigenin were the most effective against the promastigote and the intracellular amastigote forms. Selectivity indexes (SI) of rosmarinic acid and apigenin were 15.03 and 10.45 respectively for promastigotes while the SI of 12.70 and 5.21 respectively was obtained for intracellular amastigotes. Morphologically, 70% of rosmarinic acid treated promastigotes showed rounded morphology similar to the deferoxamine control. About 30% of cells treated with apigenin showed distorted cell membrane. Rosmarinic acid and apigenin induced cell arrest in the G0/G1 phase in promastigotes. Elevated intracellular iron levels were observed in promastigotes when parasites were treated with rosmarinic acid and this correlated with the level of expression of iron dependent genes. CONCLUSIONS/SIGNIFICANCE:The data suggests that rosmarinic acid exerts its anti-leishmanial effect via ... |
format |
Article in Journal/Newspaper |
author |
Christine Achiaa Antwi Cynthia Mmalebna Amisigo Jonathan Partt Adjimani Theresa Manful Gwira |
author_facet |
Christine Achiaa Antwi Cynthia Mmalebna Amisigo Jonathan Partt Adjimani Theresa Manful Gwira |
author_sort |
Christine Achiaa Antwi |
title |
In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
title_short |
In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
title_full |
In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
title_fullStr |
In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
title_full_unstemmed |
In vitro activity and mode of action of phenolic compounds on Leishmania donovani. |
title_sort |
in vitro activity and mode of action of phenolic compounds on leishmania donovani. |
publisher |
Public Library of Science (PLoS) |
publishDate |
2019 |
url |
https://doi.org/10.1371/journal.pntd.0007206 https://doaj.org/article/e3fa5ae1437d46d0a30c22c254b47557 |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
PLoS Neglected Tropical Diseases, Vol 13, Iss 2, p e0007206 (2019) |
op_relation |
http://europepmc.org/articles/PMC6405172?pdf=render https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0007206 https://doaj.org/article/e3fa5ae1437d46d0a30c22c254b47557 |
op_doi |
https://doi.org/10.1371/journal.pntd.0007206 |
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PLOS Neglected Tropical Diseases |
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13 |
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2 |
container_start_page |
e0007206 |
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