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18β-甘草次酸A环开环衍生物的合成及抗肿瘤活性 被引量:12

Synthesis and Anti-tumor Activity of Opened A-Ring Modified 18β-Glycyrrhetinic Acid Derivatives
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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.
出处 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 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
关键词 18Β-甘草次酸 三萜 抗肿瘤活性 18β-Glycyrrhetinic acid Triterpenoids Anti-tumor activity
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参考文献27

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