Rajamohan Rajaram, Ashokkumar Sekar, Murugavel Kuppusamy, Lee Yong Rok
Organic Materials Synthesis Laboratory, School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea.
Plasma Bioscience Research Center, Kwangwoon University, Seoul 01897, Republic of Korea.
Micromachines (Basel). 2023 Jun 30;14(7):1352. doi: 10.3390/mi14071352.
Quercetin (QRC), a flavonoid found in foods and plants such as red wine, onions, green tea, apples, and berries, possesses remarkable anti-inflammatory and antioxidant properties. These properties make it effective in combating cancer cells, reducing inflammation, protecting against heart disease, and regulating blood sugar levels. To enhance the potential of inclusion complexes (ICs) containing β-cyclodextrin (β-CD) in cancer therapy, they were transformed into nano-inclusion complexes (NICs). In this research, NICs were synthesized using ethanol as a reducing agent in the nanoprecipitation process. By employing FT-IR analysis, it was observed that hydrogen bonds were formed between QRC and β-CD. Moreover, the IC molecules formed NICs through the aggregation facilitated by intermolecular hydrogen bonds. Proton NMR results further confirmed the occurrence of proton shielding and deshielding subsequent to the formation of NICs. The introduction of β-CDs led to the development of a distinctive feather-like structure within the NICs. The particle sizes were consistently measured around 200 nm, and both SAED and XRD patterns indicated the absence of crystalline NICs, providing supporting evidence. Through cytotoxicity and fluorescence-assisted cell-sorting analysis, the synthesized NICs showed no significant damage in the cell line of MCF-7. In comparison to QRC alone, the presence of high concentrations of NICs exhibited a lesser degree of toxicity in normal human lung fibroblast MRC-5 cells. Moreover, the individual and combined administration of both low and high concentrations of NICs effectively suppressed the growth of cancer cells (MDA-MB-231). The solubility improvement resulting from the formation of QRC-NICs with β-CD enhanced the percentage of cell survival for MCF-7 cell types.
槲皮素（QRC）是一种存在于红酒、洋葱、绿茶、苹果和浆果等食物和植物中的类黄酮，具有显著的抗炎和抗氧化特性。这些特性使其在对抗癌细胞、减轻炎症、预防心脏病和调节血糖水平方面具有成效。为了增强含β-环糊精（β-CD）的包合物（ICs）在癌症治疗中的潜力，它们被转化为纳米包合物（NICs）。在本研究中，通过纳米沉淀法使用乙醇作为还原剂合成了NICs。通过傅里叶变换红外光谱（FT-IR）分析观察到，QRC与β-CD之间形成了氢键。此外，IC分子通过分子间氢键促进的聚集形成了NICs。质子核磁共振（NMR）结果进一步证实了NICs形成后质子屏蔽和去屏蔽的发生。β-环糊精的引入导致NICs内部形成了独特的羽毛状结构。粒径始终测量在200nm左右，选区电子衍射（SAED）和X射线衍射（XRD）图谱均表明不存在结晶性NICs，提供了支持证据。通过细胞毒性和荧光辅助细胞分选分析，合成的NICs在MCF-7细胞系中未显示出明显损伤。与单独的QRC相比，高浓度NICs在正常人肺成纤维细胞MRC-5中表现出较低程度的毒性。此外，低浓度和高浓度NICs的单独及联合给药均有效抑制了癌细胞（MDA-MB-231）的生长。与β-CD形成QRC-NICs导致的溶解度提高增加了MCF-7细胞类型的细胞存活百分比。
