Amelioration of Pterostilbene Antiproliferative, Proapoptotic, and Oxidant Potentials in Human Breast Cancer MCF7 Cells Using Zein Nanocomposites

Abstract

Hussam I Kutbi,1 Ahmed K Kammoun,2 Dalia Farag El-Telbany3 1Department of Pharmacy Practice, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 3Department of Pharmaceutics, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, 11571, EgyptCorrespondence: Dalia Farag El-TelbanyDepartment of Pharmaceutics, Faculty of Pharmacy, Modern University for Technology and Information (MTI) University, El-Hadaba El-Wosta, 5th District, Mokatam, Cairo, 11571, EgyptTel [phone]Fax [phone]Email [email protected]: This study aimed to explain the influence of zein nanosphere (ZN NS) formulation on the pharmacotherapeutic profile of PTS in MCF7 cells.Methods: Liquid–liquid phase separation was used to formulate PTS-ZN NSs. The formulations developed were evaluated for particle-size analysis, encapsulation efficiency, and in vitro diffusion. Also, assays of cytotoxicity, uptake, cell-cycle progression, annexin V, apoptotic gene mRNA expression and biochemical assays were carried out.Results: The PTS-ZN NS formulation selected showed 104.5± 6.2 nm, 33.4± 1.8 mV, 95.1%± 3.6%, and 89.1%± 2.65% average particle size, zeta-potential, encapsulation efficiency and in vitro diffusion, respectively. With MCF7 cells, IC50 was reduced approximately 15-fold, with increased cellular uptake, accumulation in the G2/M phase, increased percentage of cells in the pre-G1 phase, amelioration of early and late apoptosis, raised mRNA expression of CASP3 and CASP7, lower expression of cyclin-CDK1, and enhanced oxidant potential through decreased glutathione reductase (GR) activity, and enhanced reactive oxygen–species generation and lipid-peroxidation products.Conclusion: PTS-ZN NSs indicated enhanced antiproliferative, proapoptotic, and oxidant potential toward MCF7 cells compared to free PTS. Ameliorated results of nanosized carriers, cellular uptake, and sustained diffusion may contribute to these outcomes.Keywords: phototherapy, pterostilbene, MCF7 cells, nanospheres, zein

Keywords

• breast cancer
• zein
• pterostilbene
• nanoparticles
• apoptosis
• cell cycle
• oxidative stress