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Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)

Hepatocellular carcinoma (HCC) is one of the leading causes of mortality worldwide; therefore, searching for an effective treatment for this illness is of great importance. In the present work, in vitro cytotoxic activity of the ethanol extract of the aerial parts of Cynara cardunculus L. against hu...

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Autores principales: Hamza, Rasha A., Mostafa, Islam, Mohamed, Yasmin S., Dora, Gamal A., Ateya, Abdel-Monem, Abdelaal, Mahmoud, Fantoukh, Omer I., Alqahtani, Abdulaziz, Attia, Rasha A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9845127/
https://www.ncbi.nlm.nih.gov/pubmed/36685304
http://dx.doi.org/10.1016/j.jsps.2022.11.011
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author Hamza, Rasha A.
Mostafa, Islam
Mohamed, Yasmin S.
Dora, Gamal A.
Ateya, Abdel-Monem
Abdelaal, Mahmoud
Fantoukh, Omer I.
Alqahtani, Abdulaziz
Attia, Rasha A.
author_facet Hamza, Rasha A.
Mostafa, Islam
Mohamed, Yasmin S.
Dora, Gamal A.
Ateya, Abdel-Monem
Abdelaal, Mahmoud
Fantoukh, Omer I.
Alqahtani, Abdulaziz
Attia, Rasha A.
author_sort Hamza, Rasha A.
collection PubMed
description Hepatocellular carcinoma (HCC) is one of the leading causes of mortality worldwide; therefore, searching for an effective treatment for this illness is of great importance. In the present work, in vitro cytotoxic activity of the ethanol extract of the aerial parts of Cynara cardunculus L. against human liver carcinoma cells (Hep G2) was tested. Additionally, the antitumor activity of the extract was confirmed using chemically induced rat liver carcinogenesis with diethylnitrosamine (DEN). Moreover, bioguided fractionation and column chromatographic separation of the active compounds were carried out. The extract of C. cardunculus showed a promising cytotoxic activity according to the protocols of the National Cancer Institute. Bioguided chromatographic separation of the ethanol extract of C. cardunculus led to the isolation of seven secondary metabolites including two sesquiterpene lactones as the principal active components of the methylene chloride soluble fraction, grosheimin (IC(50) = 7.49 µg/mL) and cynaropicrin (IC(50) = 13.9 µg/mL). The compounds were characterized by different spectroscopic techniques such as EI-MS, IR and NMR. Additionally, in silico analysis of the two active compounds revealed their ability to bind with caspase-3 via hydrogen bonds interactions to initiate apoptosis of cancer cells. The results shed the light on the significance of C. cardunculus as a potential source of antitumor agents.
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spelling pubmed-98451272023-01-19 Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis) Hamza, Rasha A. Mostafa, Islam Mohamed, Yasmin S. Dora, Gamal A. Ateya, Abdel-Monem Abdelaal, Mahmoud Fantoukh, Omer I. Alqahtani, Abdulaziz Attia, Rasha A. Saudi Pharm J Original Article Hepatocellular carcinoma (HCC) is one of the leading causes of mortality worldwide; therefore, searching for an effective treatment for this illness is of great importance. In the present work, in vitro cytotoxic activity of the ethanol extract of the aerial parts of Cynara cardunculus L. against human liver carcinoma cells (Hep G2) was tested. Additionally, the antitumor activity of the extract was confirmed using chemically induced rat liver carcinogenesis with diethylnitrosamine (DEN). Moreover, bioguided fractionation and column chromatographic separation of the active compounds were carried out. The extract of C. cardunculus showed a promising cytotoxic activity according to the protocols of the National Cancer Institute. Bioguided chromatographic separation of the ethanol extract of C. cardunculus led to the isolation of seven secondary metabolites including two sesquiterpene lactones as the principal active components of the methylene chloride soluble fraction, grosheimin (IC(50) = 7.49 µg/mL) and cynaropicrin (IC(50) = 13.9 µg/mL). The compounds were characterized by different spectroscopic techniques such as EI-MS, IR and NMR. Additionally, in silico analysis of the two active compounds revealed their ability to bind with caspase-3 via hydrogen bonds interactions to initiate apoptosis of cancer cells. The results shed the light on the significance of C. cardunculus as a potential source of antitumor agents. Elsevier 2023-01 2022-11-21 /pmc/articles/PMC9845127/ /pubmed/36685304 http://dx.doi.org/10.1016/j.jsps.2022.11.011 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
Hamza, Rasha A.
Mostafa, Islam
Mohamed, Yasmin S.
Dora, Gamal A.
Ateya, Abdel-Monem
Abdelaal, Mahmoud
Fantoukh, Omer I.
Alqahtani, Abdulaziz
Attia, Rasha A.
Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title_full Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title_fullStr Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title_full_unstemmed Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title_short Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)
title_sort bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (cynara cardunculus var. altilis)
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9845127/
https://www.ncbi.nlm.nih.gov/pubmed/36685304
http://dx.doi.org/10.1016/j.jsps.2022.11.011
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