Research Article

Quercetin against MCF7 and CAL51 breast cancer cell lines: apoptosis, gene expression and cytotoxicity of nano-quercetin

Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim, 51452, Saudi Arabia

Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo, 11371, Egypt

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Ghassan M Sulaiman

*Author for correspondence: Tel.: +964 790 278 1890;

E-mail Address: ghassan.m.sulaiman@uotechnology.edu.iq

https://orcid.org/0000-0001-6388-3849

Division of Biotechnology, Department of Applied Sciences, University of Technology, Baghdad,10066, Iraq

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Sahar S Anwar

Division of Biotechnology, Department of Applied Sciences, University of Technology, Baghdad,10066, Iraq

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Amer T Tawfeeq

Department of Molecular Biology, Iraqi Center for Cancer and Medical Genetics Research, Mustansiriyah University, PO Box 14022, Baghdad, Iraq

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Riaz A Khan

**Author for correspondence:

E-mail Address: ri.khan@qu.edu.sa

https://orcid.org/0000-0003-0185-0149

Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim, 51452, Saudi Arabia

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Salman A A Mohammed

Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Qassim, 51452, Saudi Arabia

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Mohsen S Al-Omar

Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim, 51452, Saudi Arabia

Medicinal Chemistry and Pharmacognosy Department, Faculty of Pharmacy, JUST, Irbid, 22110, Jordan

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Mansour Alsharidah

Department of Physiology, College of Medicine, Qassim University, Qassim, 51452, Kingdom of Saudi Arabia

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Osamah Al Rugaie

Department of Basic Medical Sciences, College of Medicine and Medical Sciences, Qassim University, Unaizah, PO Box 991, Qassim, 51911, Saudi Arabia

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Ahmed A Al-Amiery

Unit of Applied Sciences Research, Department of Applied Science, University of Technology, Baghdad,10066, Iraq

Department of Chemical and Process Engineering, University of Kebangsaan Malaysia (UKM), Bangi, Selangor, 43000, Malaysia

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Published Online:25 Aug 2021https://doi.org/10.2217/nnm-2021-0070

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Abstract

Aims: To evaluate the anti breast-cancer activity, biocompatibility and toxicity of poly(d,l)-lactic-co-glycolic acid (PLGA)-encapsulated quercetin nanoparticles (Q-PLGA-NPs). Materials & methods: Quercetin was nano-encapsulated by an emulsion–diffusion process, and the nanoparticles were fully characterized through Fourier transform infrared spectroscopy, x-ray diffractions, FESEM and zeta-sizer analysis. Activity against CAL51 and MCF7 cell lines were assessed by DNA fragmentation assays, fluorescence microscopy, and acridine-orange, and propidium-iodide double-stainings. Biocompatibility towards red blood cells and toxicity towards mice were also explored. Results: The Q-PLGA-NPs exhibited apoptotic activity against the cell lines. The murine in vivo studies showed no significant alterations in the liver and kidney's functional biomarkers, and no apparent abnormalities, or tissue damages were observed in the histological images of the liver, spleen, lungs, heart and kidneys. Conclusion: The study established the preliminary in vitro efficacy and in vivo safety of Q-PLGA-NPs as a potential anti-breast cancer formulation.

Lay abstract

Quercetin is a flavonoid, a type of chemical, antioxidant in nature, found in many fruits and vegetables. It is known to have anticancer properties. In this study, quercetin was encased into nano-sized particles of biologically compatible and bio-degradable synthetic polymer, named PLGA (poly-[D,L]-lactic-co-glycolic acid). The effects of the quercetin nanoparticles/nano-quercetin were tested against two types of breast cancer cell lines in the laboratory. The quercetin-loaded nanoparticles were able to kill the breast cancer cells, suggesting they could be able to kill the cancer cells in the body. Also, when given to mice, the quercetin nanoparticles did not appear to damage any organ, or change the functions of the liver, and kidneys, thereby suggesting that they are not toxic. Further work is required to assess how well they could be used to treat breast cancer in people.

Graphical abstract

Keywords:

Papers of special note have been highlighted as: • of interest; •• of considerable interest

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Vol. 16, No. 22

Supplemental Materials

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History

Received 22 February 2021

Accepted 9 July 2021

Published online 25 August 2021

Published in print September 2021

Information

Keywords

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at: www.futuremedicine.com/doi/suppl/10.2217/nnm-2021-0070

Author contributions

Conceptualization: G Sulaiman, S Anwar, R Khan, and A Tawfeeq. Methodology: G Sulaiman, S Mohammed, M Al-Omar, H Mohammed, and R Khan. Software: G Sulaiman, R Khan, M Alsharidah, O Rugaie, and S Anwar. Validation, R Khan, H Mohammed, S Mohammed, M Alsharidah, O Rugaie, and A Al-Amiery. Formal analysis: G Sulaiman, S Anwar, and R Khan. Investigation: A Tawfeeq, S Anwar, G Sulaiman, R Khan, S Mohammed, M Al-Omar, H Mohammed, and A Al-Amiery. Resources: G Sulaiman, S Anwar, M Alsharidah, O Rugaie, and A Tawfeeq. Data curation: S Mohammed, M Al-Omar, R Khan, and H Mohammed. Writing (original draft preparation): G Sulaiman, R Khan, H Mohammed, and S Mohammed; writing (review and editing): M Al-Omar, R Khan, H Mohammed, S Mohammed, M Alsharidah, and G Sulaiman. Visualization: M Al-Omar, H Mohammed, R Khan, and S Mohammed. Supervision: G Sulaiman. Project administration: G Sulaiman, and A Tawfeeq. Funding acquisition: S Mohammed, H Mohammed, and G Sulaiman. All authors have read and agreed to the published version of the manuscript.

Acknowledgments

The authors extend their appreciation to the Deputyship for Research and Innovation, Ministry of Education, Saudi Arabia for funding this research work through the project number (QU-IF-1-2-2). The authors also thank the technical supports of Qassim University, Saudi Arabia, and University of Technology, and Mustansiriyah University, Baghdad, Iraq. The laboratory and animal house facilities, including instrumental, and infrastructural supports of respective institutions is gratefully acknowledged.

Financial & competing interests disclosure

This research was funded by the Deputyship for Research and Innovation, Ministry of Education, Saudi Arabia [grant number (QU-IF-1-2-2)]. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

Permissions were obtained from the Medical City Hospitals, Baghdad, Iraq, and approved by the University of Technology's institutional ethics committee, Baghdad, Iraq (Ref. no. AS 2169/18/10/2018). Laboratory animals use was approved by the institutional Research Ethics Committee (Qassim University, Saudi Arabia) together with the experimental procedures, and animal care requirements, as per the Guidelines of the NIH Guide for the Care and Use of Laboratory Animals (NIH Publication no. 86–23, revised in 1996).

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