Department of Pharmaceutical Sciences, University of Calabria, Arcavacata di Rende (CS), 87036, Italy.
Anticancer Res. 2012 Jul;32(7):2843-7.
Quercetin is one of the most potent antioxidants showing anti-inflammatory, antiproliferative and antitumoral effects; however its short half-life in buffered solution (e.g. body fluids) has so far hampered its introduction into clinical practice.
To overcome this inconvenience, quercetin was covalently conjugated into a polymethacrylic acid backbone and the conjugate was tested on HeLa cancer cells.
FT-IR, UV-Vis, Gel Permeation Chromatography analyses and the Folin-Ciocalteu test were performed to characterize the conjugate. Antioxidant properties were assessed by the DPPH test and the viability experiments by trypan blue exclusion assay.
The conjugate showed a functionalization degree of 2.01 mg of Q per g, an IC(50) of 2.62 mg ml(-1) in the DPPH assay and was able to induce a 90% cell death after one day treatment, while the value for free Quercetin was 40% after three days.
Polymer conjugation significantly increases quercetin stability, leading to a sustained activity of the flavonoid.
槲皮素是一种强效抗氧化剂，具有抗炎、抗增殖和抗肿瘤作用；然而，其在缓冲溶液（如体液）中的半衰期短，迄今为止一直阻碍其引入临床实践。
为了克服这一不便，将槲皮素共价连接到聚甲基丙烯酸酯主链上，并在 HeLa 癌细胞上测试该缀合物。
通过傅里叶变换红外光谱（FT-IR）、紫外可见光谱（UV-Vis）、凝胶渗透色谱分析和 Folin-Ciocalteu 测试对缀合物进行了表征。通过 DPPH 测试评估了抗氧化性能，通过台盼蓝排斥试验评估了细胞活力实验。
该缀合物的功能化程度为每克 2.01 毫克 Q，在 DPPH 测定中的 IC（50）为 2.62 毫克 ml（-1），在一天的治疗后能够诱导 90%的细胞死亡，而游离槲皮素的 IC（50）为 40%在三天后。
聚合物缀合显著提高了槲皮素的稳定性，从而使类黄酮的活性得以持续。
