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目的:制备甲基丙烯酸化淫羊藿苷,考察甲基丙烯酸化淫羊藿苷对肝癌HepG2细胞增殖的影响。方法:通过淫羊藿苷和甲基丙烯酸酐的亲核加成反应,获得甲基丙烯酸化淫羊藿苷;采用核磁共振氢谱、扫描电镜以及纳米粒度分布仪对其进行表征。以不同浓度(0、10、20、30、40 mol/l)的甲基丙烯酸化淫羊藿苷作用于HepG29肝癌细胞,不同时间(24,48 h)后用共聚焦显微镜和MTT法检测甲基丙烯酸化淫羊藿苷对HepG2细胞增殖的影响。结果:淫羊藿苷可通过亲核加成反应获得甲基丙烯酸化淫羊藿苷,其甲基丙烯酸酐基团的个数可以通过改变反应条件来改变,甲基丙烯酸化淫羊藿苷在水中能发生分子的自组装形成带负电荷的球形纳米粒子,且随溶液p H的不同,纳米粒子的zeta电位不同。各浓度的甲基丙烯酸化淫羊藿苷均明显抑制HepG2细胞的增殖,并呈明显的时间与浓度依赖性;20 mol/l的甲基丙烯酸化淫羊藿苷与40 mol/l的淫羊藿苷抑制HepG2细胞增殖的作用相当;作用48 h后,20、30和40 mol/l甲基丙烯酸化淫羊藿苷对HepG2细胞增殖的抑制率分别达42.40%、77.06%和95.31%,而40 mol/l淫羊藿苷的抑制率则为39.25%。结论:淫羊藿苷结构修饰产物甲基丙烯酸化淫羊藿苷可显著抑制HepG2细胞增殖,且作用强度高于淫羊藿苷,是一种潜在的抗肿瘤候选药物。
Objective: To prepare methacrylated icariin and investigate the effect of methacrylic Icariin on the proliferation of HepG2 cells. Methods: Icariin was obtained by nucleophilic addition reaction of icariin and methacrylic anhydride. Its structure was characterized by 1H-NMR, SEM and nano-particle size distribution. HepG29 hepatocarcinoma cells were treated with different concentrations of icariin at different concentrations (0, 10, 20, 30 and 40 mol / l), and the cells were treated with different time (24 and 48 h) Effect of Basic Acrylation of Icariin on HepG2 Cell Proliferation. Results: Icariin can be obtained by nucleophilic addition reaction of icariin, the number of methacrylic anhydride groups can be changed by changing the reaction conditions, methacryl Icariin in Self-assembly of molecules in water can take place to form negatively charged spherical nanoparticles, and the zeta potential of the nanoparticles varies with the pH of the solution. Methacrylated icariin at various concentrations significantly inhibited the proliferation of HepG2 cells in a time and concentration dependent manner; 20 mol / l of methacryloylated icariin and 40 mol / l of epimedium The inhibitory rates of icariin on proliferation of HepG2 cells were the same at 48 h, but the inhibitory rates of 20, 30 and 40 mol / l methacryloylated icariin on HepG2 cells reached 42.40%, 77.06% and 95.31%, respectively The inhibition rate of 40 mol / l icariin was 39.25%. CONCLUSION: Icariin structurally modified product Icariin can significantly inhibit the proliferation of HepG2 cells and its action intensity is higher than Icariin, which is a potential anti-tumor candidate drug.