Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Anti-proliferative activity of leaves of Launaea capitata Asteraceae: Phytochemical, cytotoxicity and in silico studies

Hany Ezzat Khalil^1,2 , Turki Saeed Aldakheel³, Anas AlAhmed¹, Promise Madu Emeka¹, Mahmoud Kandeel^4,5

¹Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa ??31982; ²Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt; ³John Hopkins Aramco Healthcare, Dhahran; ⁴Department of Physiology, Biochemistry and Pharmacology, College of Veterinary Medicine, King Faisal University, Al-Ahsa 31982, Saudi Arabia; ⁵Department of Pharmacology, Faculty of Veterinary Medicine, Kafrelsheikh University, Kafr Elsheikh 33516, Egypt.

For correspondence:- Hany Khalil Email: heahmed@kfu.edu.sa Tel:+966563724624

Accepted: 24 September 2020 Published: 30 October 2020

Citation: Khalil HE, Aldakheel TS, AlAhmed A, Emeka PM, Kandeel M. Anti-proliferative activity of leaves of Launaea capitata Asteraceae: Phytochemical, cytotoxicity and in silico studies. Trop J Pharm Res 2020; 19(10):2129-2136 doi: 10.4314/tjpr.v19i10.17

© 2020 The authors.
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Abstract

Purpose: To investigate the phytochemical contents of Launaea capitata (L. capitate) and its ‎potential cytotoxic activity. Also, to examine its molecular modeling by docking of the isolated ‎compounds.

Methods: ‎ L. capitata was methanol-extracted and successively fractionated followed by determination of the total phenolic and flavonoid contents. Major constituents were isolated and purified. ‎3-(4, 5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide‎ (MTT) cytotoxicity assays were conducted for all fractions. In silico studies were conducted using four anticancer target kinases, namely, protein kinase B (PKB/AKT), phosphatidylinositol 3-kinase (PI3K), protein kinase C (PKC), and rapidly accelerated fibrosarcoma kinases (RAFK).

Results: The results showed that total phenolic constituents ranged from 0.150 ± 0.004 to 60.229 ± 0.822 mg Gallic Acid Equivalent/g of dry extract, while the total flavonoid content varied from 0.004 ± 0.002 to 18.129 ± 1.599 mg quercetin equivalent/g of ‎dry extract‎. Furthermore, the ethyl acetate fraction contained the highest amount of phenolic and flavonoid contents, which seemed to constitute the most effective anti-proliferative fraction. The plant’s major constituent was apigenin-7-O-glycoside and was isolated from the ethyl acetate fraction. The MTT cytotoxicity assay revealed the anti-proliferative activity of ethyl acetate and butanol fractions, and apigenin-7-O-glycoside with half-maximal concentration (IC₅₀) comparable to that of doxorubicin. In silico studies revealed that apigenin-7-O-glycoside showed a better binding score and ligand efficiency when compared with standard ligands/inhibitors for AKT/PKB and PI3K, suggesting potential multiple targets for its anti-cancer activities.

Conclusion: L. capitata contains considerable amounts of phenolic and flavonoid components. Its major constituent, apigenin-7-O-glycoside is a potential lead compound for developing new anticancer compounds.

Keywords: Launaea capitata, Total phenolics, Total flavonoids, Docking, Cytotoxicity