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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| Format: | Article |
| Language: | English |
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Elsevier
2023-01-01
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| Series: | Saudi Pharmaceutical Journal |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016422002808 |
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| author | Rasha A. Hamza Islam Mostafa Yasmin S. Mohamed Gamal A. Dora Abdel-Monem Ateya Mahmoud Abdelaal Omer I. Fantoukh Abdulaziz Alqahtani Rasha A. Attia |
| author_facet | Rasha A. Hamza Islam Mostafa Yasmin S. Mohamed Gamal A. Dora Abdel-Monem Ateya Mahmoud Abdelaal Omer I. Fantoukh Abdulaziz Alqahtani Rasha A. Attia |
| author_sort | Rasha A. Hamza |
| collection | DOAJ |
| 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 (IC50 = 7.49 µg/mL) and cynaropicrin (IC50 = 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. |
| first_indexed | 2024-04-10T23:13:00Z |
| format | Article |
| id | doaj.art-1459b7ee98924886a65f8ea77bfc28d7 |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-04-10T23:13:00Z |
| publishDate | 2023-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-1459b7ee98924886a65f8ea77bfc28d72023-01-13T04:15:49ZengElsevierSaudi Pharmaceutical Journal1319-01642023-01-01311125134Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis)Rasha A. Hamza0Islam Mostafa1Yasmin S. Mohamed2Gamal A. Dora3Abdel-Monem Ateya4Mahmoud Abdelaal5Omer I. Fantoukh6Abdulaziz Alqahtani7Rasha A. Attia8Department of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, EgyptDepartment of Pharmacology, Faculty of Pharmacy, Cairo University, Cairo, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, EgyptDepartment of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; Corresponding authors.Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmacognosy, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, Egypt; Corresponding authors.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 (IC50 = 7.49 µg/mL) and cynaropicrin (IC50 = 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.http://www.sciencedirect.com/science/article/pii/S1319016422002808Hepatocellular carcinomaAsteraceaeCynara cardunculusSecondary metabolitesMolecular dockingIn vivo antitumor |
| spellingShingle | Rasha A. Hamza Islam Mostafa Yasmin S. Mohamed Gamal A. Dora Abdel-Monem Ateya Mahmoud Abdelaal Omer I. Fantoukh Abdulaziz Alqahtani Rasha A. Attia Bioguided isolation of potential antitumor agents from the aerial parts of cultivated cardoon (Cynara cardunculus var. altilis) Saudi Pharmaceutical Journal Hepatocellular carcinoma Asteraceae Cynara cardunculus Secondary metabolites Molecular docking In vivo antitumor |
| 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 | Hepatocellular carcinoma Asteraceae Cynara cardunculus Secondary metabolites Molecular docking In vivo antitumor |
| url | http://www.sciencedirect.com/science/article/pii/S1319016422002808 |
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