Ersoz Melike, Erdemir Aysegul, Derman Serap, Arasoglu Tulin, Mansuroglu Banu
Department of Molecular Biology and Genetics, Faculty of Arts and Science, Demiroglu Bilim University, Istanbul, Turkey.
Department of Molecular Biology and Genetics, Faculty of Arts and Science, Yildiz Technical University, Istanbul, Turkey.
Pharm Dev Technol. 2020 Jul;25(6):757-766. doi: 10.1080/10837450.2020.1740933. Epub 2020 Mar 20.
Quercetin (Qu) is a natural flavonoid present in many commonly consumed food items. The dietary phytochemical quercetin prevents tumor proliferation and is a potent therapeutic cancer agent. The purpose of this study was to synthesize and characterize quercetin-loaded poly(lactic-co-glycolic acid) nanoparticles (QuNP, QuNP, and QuNP) with different size and encapsulation properties and to evaluate their activity on C6 glioma cells. Nanoparticles were synthesized by single emulsion solvent evaporation method. Then, particle size, zeta potential, polydispersity index and encapsulation efficiency of nanoparticles were determined. Particle size of QuNP, QuNP, and QuNPs were determined as 215.2 ± 6.2, 282.3 ± 7.9, and 584.5 ± 15.2 nm respectively. Treating C6 glioma cells with all nanoparticle formulations effectively inhibited the cell proliferation. QuNPs were showed the lowest IC value in 48 h with 29.9 μg/ml and achieved higher cellular uptake among other nanoparticles and Qu. Additionally, 48-h treatment with QuNPs significantly decreased MDA level (14.90 nmol/µg protein) on C6 glioma cells which is related to reduced oxidative stress in cells. Findings of this study revealed that quercetin's cellular uptake and anti-oxidant activity is improved by small-sized QuNPs in C6 glioma cells.
槲皮素（Qu）是一种存在于许多常见食品中的天然类黄酮。膳食植物化学物质槲皮素可防止肿瘤增殖，是一种有效的癌症治疗剂。本研究的目的是合成并表征具有不同尺寸和包封特性的载槲皮素聚（乳酸-乙醇酸）纳米颗粒（QuNP、QuNP和QuNP），并评估它们对C6胶质瘤细胞的活性。通过单乳液溶剂蒸发法合成纳米颗粒。然后，测定纳米颗粒的粒径、zeta电位、多分散指数和包封效率。QuNP、QuNP和QuNP的粒径分别测定为215.2±6.2、282.3±7.9和584.5±15.2nm。用所有纳米颗粒制剂处理C6胶质瘤细胞均有效抑制细胞增殖。QuNP在48小时内显示出最低的IC值，为29.9μg/ml，并且在其他纳米颗粒和槲皮素中实现了更高的细胞摄取。此外，用QuNP进行48小时处理可显著降低C6胶质瘤细胞上的MDA水平（14.90nmol/μg蛋白质），这与细胞内氧化应激降低有关。本研究结果表明，在C6胶质瘤细胞中，小尺寸的QuNP可提高槲皮素的细胞摄取和抗氧化活性。
