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Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines
Thiosemicarbazones have received noteworthy attention due to their numerous pharmacological activities. Various thiosemicarbazone derivatives have been reported to play a key role as potential chemotherapeutic agents for the management of cancer. Herein, we aimed to establish the anticancer efficacy...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9257852/ https://www.ncbi.nlm.nih.gov/pubmed/35812146 http://dx.doi.org/10.1016/j.jsps.2022.03.011 |
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author | Khan, Azmat Ali Ahmad, Rehan Alanazi, Amer M. Alsaif, Nawaf Abdullah, Maha Wani, Tanveer A. Bhat, Mashooq A. |
author_facet | Khan, Azmat Ali Ahmad, Rehan Alanazi, Amer M. Alsaif, Nawaf Abdullah, Maha Wani, Tanveer A. Bhat, Mashooq A. |
author_sort | Khan, Azmat Ali |
collection | PubMed |
description | Thiosemicarbazones have received noteworthy attention due to their numerous pharmacological activities. Various thiosemicarbazone derivatives have been reported to play a key role as potential chemotherapeutic agents for the management of cancer. Herein, we aimed to establish the anticancer efficacy of novel thiosemicarbazone derivative C4 against colon cancer in vitro. The MTT viability assay identified C4 as a promising anticancer compound in a panel of cancer cell lines with the most potent activity against colon cancer cells. Further, anticancer potential of C4 was evaluated against HT-29 and SW620 colon cancer cell lines considering the factors like cell adhesion and migration, oxidative stress, cell cycle arrest, and apoptosis. Our results showed that C4 significantly inhibited the migration and adhesion of colon cancer cells. C4 significantly increased the intracellular reactive oxygen species (ROS) and induced apoptotic cell death. Cell cycle analysis revealed that C4 interfered in the cell cycle distribution and arrested the cells at the G2/M phase of the cell cycle. Consistent with these results C4 also down-regulated the Bcl-XL and Bcl-2 and up-regulated the caspase-3 expression. These findings introduced C4 as the potential anticancer agent against colon cancer. |
format | Online Article Text |
id | pubmed-9257852 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-92578522022-07-07 Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines Khan, Azmat Ali Ahmad, Rehan Alanazi, Amer M. Alsaif, Nawaf Abdullah, Maha Wani, Tanveer A. Bhat, Mashooq A. Saudi Pharm J Original Article Thiosemicarbazones have received noteworthy attention due to their numerous pharmacological activities. Various thiosemicarbazone derivatives have been reported to play a key role as potential chemotherapeutic agents for the management of cancer. Herein, we aimed to establish the anticancer efficacy of novel thiosemicarbazone derivative C4 against colon cancer in vitro. The MTT viability assay identified C4 as a promising anticancer compound in a panel of cancer cell lines with the most potent activity against colon cancer cells. Further, anticancer potential of C4 was evaluated against HT-29 and SW620 colon cancer cell lines considering the factors like cell adhesion and migration, oxidative stress, cell cycle arrest, and apoptosis. Our results showed that C4 significantly inhibited the migration and adhesion of colon cancer cells. C4 significantly increased the intracellular reactive oxygen species (ROS) and induced apoptotic cell death. Cell cycle analysis revealed that C4 interfered in the cell cycle distribution and arrested the cells at the G2/M phase of the cell cycle. Consistent with these results C4 also down-regulated the Bcl-XL and Bcl-2 and up-regulated the caspase-3 expression. These findings introduced C4 as the potential anticancer agent against colon cancer. Elsevier 2022-06 2022-03-31 /pmc/articles/PMC9257852/ /pubmed/35812146 http://dx.doi.org/10.1016/j.jsps.2022.03.011 Text en © 2022 The Author(s) https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Original Article Khan, Azmat Ali Ahmad, Rehan Alanazi, Amer M. Alsaif, Nawaf Abdullah, Maha Wani, Tanveer A. Bhat, Mashooq A. Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title | Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title_full | Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title_fullStr | Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title_full_unstemmed | Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title_short | Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
title_sort | determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9257852/ https://www.ncbi.nlm.nih.gov/pubmed/35812146 http://dx.doi.org/10.1016/j.jsps.2022.03.011 |
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