摘要
目的:通过共价结合制备肝素-藤黄酸接枝物(GA-Hep),考察GA-Hep胶束的性质及体外抗肿瘤活性。方法:通过酰胺键将藤黄酸与肝素连接制备GA-Hep,透射电镜观察胶束形貌、纳米粒度仪分析胶束的粒径及Zeta电位、荧光分光光度计检测临界聚集浓度(critical aggregation concentration,CAC)、噻唑蓝(MTT)法考察自组装胶束体外对肺癌细胞A549细胞的抑制作用。结果:GA-Hep胶束为球形,平均粒径(163±1.16)nm,Zeta电位为(-29±0.91)m V,取代度为(44.50±0.15)%,CAC值为(0.004±0.000 61)mg·m L-1,体外抗肿瘤试验结果表明GA-Hep对A549细胞的IC50为(31.22±0.14)μg·m L-1。结论:该研究表明GA-Hep具有较高的载药量,并形成稳定的胶束,同时保留了藤黄酸的抗肿瘤活性。
OBJECTIVE To prepare gambogic acid grafted heparin（ GA-Hep） and determine characters and anti-tumor activity of its self-assembly micelles. METHODS GA-Hep was prepared by conjugating heparin with gambogic acid through amido linkage.Morphologies of micelles were observed by transmission electron microscope,particle size and zeta potential determined with Nano particle instrument,CMC detected by fluorescence spectrophotometer,and inhibition of micelles on A549 proliferation determined by MTT. RESULTS Morphology of GA-Hep self-assembly micelles was spherical. Mean particle size,Zeta potential,degree of substitution and CAC values were（ 163 ± 1. 16） nm,（- 29 ± 0. 91） mV,（ 44. 5 ± 0. 15） % and（ 0. 004 ± 0. 000 61） mg·mL^- 1,respectively. IC50 of micelles on A549 proliferation was（ 26. 079 ± 0. 14） μg·mL^- 1. CONCLUSION GA-Hep micelles with good stability have high drug loading capacity and reserve antitumor activity of gambogic acid.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2016年第5期371-375,共5页
Chinese Journal of Hospital Pharmacy
基金
安徽省高等学校自然科学基金(编号:KJ2015A130)
关键词
两亲性自组装胶束
肝素
藤黄酸
临界聚集浓度
抗肿瘤
amphiphilic self-assembly micelle
heparin
gambogic acid
critical aggregation concentration
antitumor
