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 vitrocytotoxic activity of the ethanol extract of the aerial parts ofCynara cardunculusL. against human...

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Bibliographic Details
Published in:	Saudi pharmaceutical journal Vol. 31; no. 1; pp. 125 - 134
Main Authors:	Hamza, Rasha A., Mostafa, Islam, Mohamed, Yasmin S., Dora, Gamal A., Ateya, Abdel-Monem, Abdelaal, Mahmoud, Fantoukh, Omer I., Alqahtani, Abdulaziz, Attia, Rasha A.
Format:	Journal Article
Language:	English
Published:	Saudi Arabia Elsevier B.V 01-01-2023 Elsevier
Subjects:	Asteraceae Cynara cardunculus Hepatocellular carcinoma In vivo antitumor Molecular docking Original Secondary metabolites In vivo antitumor Hepatocellular carcinoma Secondary metabolites Cynara cardunculus Molecular docking Asteraceae
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Summary:	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 vitrocytotoxic activity of the ethanol extract of the aerial parts ofCynara cardunculusL. 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 The co-author has passed away, March 2016.
ISSN:	1319-0164 2213-7475
DOI:	10.1016/j.jsps.2022.11.011