槲皮素-3-硫酸酯钠的合成、表征及抗肿瘤活性研究

Study on Synthesis,Characterization and Anti-tumor Activity of Quercetin-3-sulphate Sodium

目的:研究槲皮素-3-硫酸酯钠的合成、表征及抗肿瘤活性,并对槲皮素和槲皮素-3-硫酸酯钠的溶解度及其抗肿瘤作用进行对照比较。方法:以芦丁为原料,合成出槲皮素-3-硫酸酯钠,通过元素分析、红外光谱、紫外光谱及核磁共振等,确定其组成结构以及测定其溶解度。同时采用噻唑蓝(MTT)比色法测定槲皮素及磺化产物对HepG2肝癌细胞株的抗肿瘤活性。结果:槲皮素-3-硫酸酯钠在水中溶解度(15℃)是3.391 mg/mL,比槲皮素增大42.6倍。由于水溶性的增强,槲皮素-3-硫酸酯钠高浓度下对HepG2细胞抑制率显著高于槲皮素。结论:槲皮素-3-硫酸酯钠的水溶性提高,抗肿瘤作用明显。

Objective： To study synthesis,characterization and anti-tumor activity of quercetin-3-sulphate sodium,compare to both solubility and antitumor activity.Methods： Using Rutin as raw material,synthetise quercetin-3-sulphate sodium and its structure were characterized by elemental analysis,IR spectra,UV spectra and 1HNMR.MTT colorimetric assay was used to detect the anti-tumor activity of quercetin and quercetin-3-sulphate sodium on human hepatocarcinoma cell line HepG2.Result： Solubility of quercetin-3-sulphate sodium in water（15℃） was 3.391 mg / mL,42.6 times more than quercetin.Because of improved solubility,quercetin-3-sulphate sodium,the proliferation rates of cell treated with quercetin-3-sulphate sodium was higher than that of quercetin.Conclusion： The solubility and the anti-tumor activity of quercetin-3-sulphate sodium are much improved.