摘要
将18β-甘草次酸的C20位上的羧基与氨基聚乙二醇的氨基缩合形成了18β-甘草次酸的聚乙二醇轭合物,并用紫外和红外波谱分析等手段证实了该轭合物的结构。实验中发现,18β-甘草次酸的聚乙二醇轭合物的水溶性比18β-甘草次酸高280倍左右;使用B16小鼠黑色素瘤细胞测定了该轭合物的抗肿瘤活性,结果表明:其抗肿瘤活性与对照物18β-甘草次酸相当。良好的水溶性和生物活性表明18β-甘草次酸的聚乙二醇轭合物是一种具有良好应用前景的抗肿瘤药物。
To synthesize glycyrrhetinic acid polyethylene glycol derivative, 18β-GA was coupled with PEG-NH2 at its C20 earboxyl function to form an amide bond between 18β-GA and PEG-NH2. In subsequent solubility assay, we found that this 18β-GA derivative was 280 times soluble in water than GA itself, and that it had equal bioaetivity compared with GA tested with mouse B16 melnoma cell. Higher solubility and bioaetivity suggest that PEG-18β-GA might be a useful prospective anti tumor candidate.
出处
《华东理工大学学报（自然科学版）》
EI
CAS
CSCD
北大核心
2006年第4期415-417,496,共4页
Journal of East China University of Science and Technology
基金
上海市重点学科建设经费支持
关键词
甘草次酸
聚乙二醇
轭合物
合成
抗肿瘤活性
glycyrrhetinie acid
polyethylene glycol
conjugate
synthesis
anti tumor activity
