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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...

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Autores principales: Khan, Azmat Ali, Ahmad, Rehan, Alanazi, Amer M., Alsaif, Nawaf, Abdullah, Maha, Wani, Tanveer A., Bhat, Mashooq A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2022
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.
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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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