| 孟艳秋,张良锋,张译,李凤清,朱冬青,孙伟.化学通报,2015,78(4):358-363. |
| 积雪草酸衍生物的合成及抗肿瘤活性研究 |
| Synthesis and anti-tumor activity of asiatic acid derivatives |
| 投稿时间：2014-08-31 修订日期：2014-10-14 |
| DOI： |
| 中文关键词: 积雪草酸 五环三萜类化合物 抗肿瘤活性 |
| 英文关键词:asiatic acid pentacyclic trierpenoid anti-tumor activity |
| 基金项目:国家自然科学基金资助项目(21372156)、辽宁省教育厅高等学校优秀人才支持计划项目(LR2013017)和沈阳市科技计划项目(F13-316-1-47)资助 |
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| 中文摘要: |
| 以天然产物积雪草酸为先导化合物,对C-2、C-3、C-23位羟基、C-11位氢、C-28位羧基进行结构改造,合成了13个新的积雪草酸衍生物,目标化合物结构经MS及1H NMR等确证。采用MTT法,选用高表达人癌细胞(HeLa、HepG2和BGC-823)对目标化合物进行初步的体外抗肿瘤活性研究,结果表明,所测化合物对HeLa、HepG2和BGC-823肿瘤细胞的抑制活性均明显强于积雪草酸,其中化合物I4和II4对HeLa、SKOV3和BGC-823细胞表现出很强的抑制活性,明显高于已上市药物吉非替尼,值得进一步研究。 |
| 英文摘要: |
| Structure of natural product-asiatic acid was modified for increasing its antitumor activity．Thirteen new derivatives of asiatic acid were designed and synthesized by the structure modified at C-2,C-3,C-23 hydroxyl group,C-11 hydrogen,C-28 carboxyl group．The structures of target compounds were confirmed by MS and 1H NMR analysis．The antitumor activities of target compounds were evaluated by MTT assay in HeLa,HepG2 and BGC-823 cells expressing high levels in body．The results indicated that the tested compounds were found to have a degree of inhibition on cell proliferation of HeLa,HepG2 and BGC-823 cells．Especially Compound I4 and II4showed strong inhibitory activity on these three kinds of tumor cells,significantly higher than the listed drug Gefitinib,and were worth to be intensively studied further． |
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