Preparation and characterization of (−)-Epigallocatechin-3-gallate (EGCG)-loaded nanoparticles and their inhibitory effects on Human breast cancer MCF-7 cells

• Published in: Scientific reports Vol. 7; no. 1; p. 45521
• Main Authors: Zeng, Liang, Yan, Jingna, Luo, Liyong, Ma, Mengjun, Zhu, Huiqun
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 28.03.2017; Nature Publishing Group
• Subjects: 1-Phosphatidylinositol 3-kinase; 14/34; 140/131; 631/61/350/354; 631/67/1059/153; 631/67/1347; 82/1; 82/80; AKT protein; Anticarcinogenic Agents - pharmacology; Bax protein; Bcl protein; Bcl-2 protein; Breast cancer; Catechin - analogs & derivatives; Catechin - pharmacology; Cell proliferation; Cell Proliferation - drug effects; Cytotoxicity; Drug Carriers - metabolism; Encapsulation; Epigallocatechin-3-gallate; Gene Expression Regulation - drug effects; GTP-binding protein; Humanities and Social Sciences; Humans; Inhibitory Concentration 50; MCF-7 Cells; multidisciplinary; Nanoparticles; Nanoparticles - metabolism; Polyethylene glycol; PTEN protein; Regulatory proteins; Science
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/srep45521

We were employing nanotechnology to improve the targeting ability of (−)-Epigallocatechin-3-gallate (EGCG) towards MCF-7 cells, and two kinds of EGCG nanoparticles (FA-NPS-PEG and FA-PEG-NPS) were obtained, besides, their characteristics and effects on MCF-7 cells were studied. The results indicated that (i) both FA-NPS-PEG and FA-PEG-NPS have high stabilities; (ii) their particles sizes were 185.0 ± 13.5 nm and 142.7 ± 7.2 nm, respectively; (iii) their encapsulation efficiencies of EGCG were 90.36 ± 2.20% and 39.79 ± 7.54%, respectively. (iv) there was no cytotoxicity observed in EGCG, FA-NPS-PEG and FA-PEG-NPS toward MCF-7 cells over all concentrations (0~400 μg/mL) tested; (v) EGCG, FA-NPS-PEG and FA-PEG-NPS inhibited MCF-7 cells proliferation in dose-dependent manners, with the average IC 50 of 470.5 ± 33.0, 65.9 ± 0.4 and 66.6 ± 0.6 μg/mL; (vi) EGCG, FA-NPS-PEG and FA-PEG-NPS could modulated the expressions of several key regulatory proteins in PI3K-Akt pathway such as up-regulation of PTEN, p21 and Bax, and down-regulation of p -PDK1, p -AKT, CyclinD1 and Bcl-2, which gave an illustration about the mechanism by which EGCG nanoparticles inhibited MCF-7 cells proliferation. In this study, EGCG nanoparticles can significantly enhance the targeting ability and efficacy of EGCG, which is considered to an experimental foundation for further research on its activity, targeting ability and metabolism in vivo .