18β-甘草次酸A环开环衍生物的合成及抗肿瘤活性  

Synthesis and Anti-tumor Activity of Opened A-Ring Modified 18β-Glycyrrhetinic Acid Derivatives

作　　者：胡君[1] 吴洋[1] 赵长崎[2] 巨勇[1,3] 

机构地区：[1]清华大学化学系,生命有机磷化学及化学生物学教育部重点实验室,北京100084 [2]北京师范大学生命科学学院,北京100875 [3]兰州大学功能有机分子化学国家重点实验室,兰州730000

出　　处：《高等学校化学学报》2010年第9期1762-1768,共7页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金(批准号:20772071;20972086);高等学校博士学科点基金(批准号:20090002110060)资助

摘　　要：采用化学方法在18β-甘草次酸A环上进行结构修饰,合成了一系列新颖的A环具有不同官能团的开环衍生物.初步研究了它们对人体肝癌细胞HepG-2的体外细胞毒活性,结果表明,羟基的数目和位置对抑制HepG-2细胞增殖起着重要的作用.Glycyrrhetinic acid,a facile pentacyclic triterpenoid with rigid and chiral structures,is widely present in the form of aglycone or glycosides in medicinal plants,which is used as bioactive component on anti-inflammatory,anti-viral and anti-tumor-promotion effect. Owing to its relative low-toxicity,biocompatibility and bioactivity,a series of novel opened A-ring and different functional group derivatives of glycyrrhetinic acid was synthesized by chemical methods. The preliminary biological activities were tested against human liver carcinoma（ HepG-2） cell in vitro. The results show that the activity should be affected by the number and the position of hydroxyls.

关 键 词：18Β-甘草次酸 三萜 抗肿瘤活性 

分 类 号：O629.61[理学—有机化学]