Hanan G. Sary, Nahla A. Ayoub, Abdel Nasser B. Singab, Mickey Vinodh, Khaled Y. Orabi


Objective: In a previous study, Centaurea aegyptiaca ethanol and ethyl acetate extracts showed potent cytotoxic effects against laryngeal (HEP2) and hepatic (HEPG2) carcinoma cell lines. Additionally, two novel compounds were isolated and identified. The aim of this study is to continue isolating and identifying another compound (s) that may, also, be responsible for this potent biological activity.

Methods: C. aegyptiaca dried aerial parts were extracted with ethanol and ethyl acetate. Both extracts were chromatographed separately to afford seven guaianolides that were identified using different spectroscopic methods. Moreover, compounds 1-7 were evaluated for their cytotoxicity (IC50, µM) against HEP2 and HEPG2 cells in comparison to the normal fibroblasts (BHK) using sulforhodamine B assay. Doxorubicin was used as a positive control.

Results: Seven sesquiterpene lactones, centaurepensin, also known as chlorohyssopifolin A (1), 8α-hydroxy-11α, 13-dihydrozaluzanin C (2), chlorohyssopifolin B (3), desacylcynaropicrin (4), chlorohyssopifolin C, acroptilin (5), subluteolide (6), and solstitiolide (7) were isolated from C. aegyptiaca extracts and identified. This is the first report on the occurrence of 2, 4, 5 and 6 in C. aegyptiaca. Compounds 1-4 and 6 exhibited selective cytotoxic effects against HEP2 and HEPG2 cells. However, compounds 1 and 7 showed the highest activities against HEP2 with IC50 values of 10.6±0.02 and 10.9±0.03 µM, respectively. Moreover, compound 3 was the most potent one against HEPG2 cells with IC50value of 13.8±0.05 µM.

Conclusions: Chemical investigation of C. aegyptiaca ethanol and ethyl acetate extracts led to the isolation and identification of seven guaianolides. These compounds exhibited good cytotoxic activities against HEP2 and HEPG2 cell lines.


Centaurea aegyptiaca, Sesquiterpene, Guaianolides, Cytotoxic activity, Sulforhodamine B assay

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Centaurea aegyptiaca, Sesquiterpene, Guaianolides, Cytotoxic activity, Sulforhodamine B assay





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International Journal of Pharmacy and Pharmaceutical Sciences
Vol 10, Issue 4, 2018 Page: 1-6

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Authors & Affiliations

Hanan G. Sary
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Health Sciences Center, Kuwait University, Safat 13110, Kuwait

Nahla A. Ayoub
Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt

Abdel Nasser B. Singab
Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt

Mickey Vinodh
Research Sector Project Units, Faculty of Science, Kuwait University, Safat 13060, Kuwait

Khaled Y. Orabi
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Health Sciences Center, Kuwait University, Safat 13110, Kuwait

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