Zygouri Panagiota, Tsiodoulos Grigorios, Angelidou Marina, Papanikolaou Eirini, Athinodorou Antrea-Maria, Simos Yannis V, Spyrou Konstantinos, Subrati Mohammed, Kouloumpis Antonios, Kaloudi Angela S, Asimakopoulos Georgios, Tsamis Konstantinos, Peschos Dimitrios, Vezyraki Patra, Ragos Vasileios, Gournis Dimitrios P
Department of Materials Science and Engineering, University of Ioannina 45110 Ioannina Greece
Nanomedicine and Nanobiotechnology Research Group, University of Ioannina Ioannina 45110 Greece
Nanoscale Adv. 2024 Apr 17;6(11):2860-2874. doi: 10.1039/d3na00966a. eCollection 2024 May 29.
Targeting cancer cells without affecting normal cells poses a particular challenge. Nevertheless, the utilization of innovative nanomaterials in targeted cancer therapy has witnessed significant growth in recent years. In this study, we examined two layered carbon nanomaterials, graphene and carbon nanodiscs (CNDs), both of which possess extraordinary physicochemical and structural properties alongside their nano-scale dimensions, and explored their potential as nanocarriers for quercetin, a bioactive flavonoid known for its potent anticancer properties. Within both graphitic allotropes, oxidation results in heightened hydrophilicity and the incorporation of oxygen functionalities. These factors are of great significance for drug delivery purposes. The successful oxidation and interaction of quercetin with both graphene (GO) and CNDs (oxCNDs) have been confirmed through a range of characterization techniques, including FTIR, Raman, and XPS spectroscopy, as well as XRD and AFM. anticancer tests were conducted on both normal (NIH/3T3) and glioblastoma (U87) cells. The results revealed that the bonding of quercetin with GO and oxCNDs enhances its cytotoxic effect on cancer cells. GO-Quercetin and oxCNDs-Quercetin induced G0/G1 cell cycle arrest in U87 cells, whereas oxCNDs caused G2/M arrest, indicating a distinct mode of action. In long-term survival studies, cancer cells exhibited significantly lower viability than normal cells at all corresponding doses of GO-Quercetin and oxCNDs-Quercetin. This work leads us to conclude that the conjugation of quercetin to GO and oxCNDs shows promising potential for targeted anticancer activity. However, further research at the molecular level is necessary to substantiate our preliminary findings.
在不影响正常细胞的情况下靶向癌细胞是一项特殊的挑战。然而，近年来创新纳米材料在靶向癌症治疗中的应用有了显著增长。在本研究中，我们考察了两种层状碳纳米材料——石墨烯和碳纳米盘（CNDs），它们在具有纳米尺度尺寸的同时还具备非凡的物理化学和结构特性，并探索了它们作为槲皮素纳米载体的潜力，槲皮素是一种具有强大抗癌特性的生物活性黄酮类化合物。在这两种石墨同素异形体中，氧化会导致亲水性增强以及氧官能团的引入。这些因素对于药物递送目的具有重要意义。通过一系列表征技术，包括傅里叶变换红外光谱（FTIR）、拉曼光谱、X射线光电子能谱（XPS）以及X射线衍射（XRD）和原子力显微镜（AFM），已证实槲皮素与石墨烯（GO）和碳纳米盘（氧化碳纳米盘，oxCNDs）均成功发生了氧化和相互作用。对正常细胞（NIH/3T3）和成胶质细胞瘤细胞（U87）都进行了抗癌测试。结果显示，槲皮素与GO和oxCNDs的结合增强了其对癌细胞的细胞毒性作用。GO - 槲皮素和oxCNDs - 槲皮素在U87细胞中诱导了G0/G1期细胞周期停滞，而oxCNDs导致了G2/M期停滞，表明其作用模式不同。在长期存活研究中，在所有相应剂量的GO - 槲皮素和oxCNDs - 槲皮素作用下，癌细胞的活力均显著低于正常细胞。这项工作使我们得出结论，槲皮素与GO和oxCNDs的缀合显示出靶向抗癌活性的良好潜力。然而，有必要在分子水平上进行进一步研究以证实我们的初步发现。
