田丹丽,梁春坡,陈虹.鬼臼毒素衍生物的合成及细胞毒活性研究[J].中草药,2019,50(18):4281-4287
鬼臼毒素衍生物的合成及细胞毒活性研究
Synthesis and cytotoxic activities of podophyllotoxin derivatives
投稿时间:2019-03-16  
DOI:10.7501/j.issn.0253-2670.2019.18.005
中文关键词:  鬼臼毒素  抗肿瘤活性  构效关系  结构修饰  衍生物  细胞毒活性
英文关键词:podophyllotoxin  antitumor activity  structure-activity relationship  structure modification  derivatives  cytotoxic activities
基金项目:国家自然科学基金资助项目(30873363)
作者单位E-mail
田丹丽 天津市第一中心医院, 天津 300192  
梁春坡 天津医科大学总医院, 天津 300052  
陈虹 武警后勤学院 生药学教研室, 天津 300309 chenhongtian06@163.com 
摘要点击次数: 92
全文下载次数: 65
中文摘要:
      目的 基于鬼臼毒素进行结构修饰,并对得到的衍生物进行体外抗肿瘤活性评价。方法 以鬼臼毒素和醛类化合物为起始原料,经多步反应合成目标化合物,并采用MTT法测试所有的目标化合物对人宫颈癌HeLa细胞、人慢性髓性白血病急变期K562细胞及其阿霉素耐药株K562/A02的体外抗肿瘤活性。结果 合成了11个文献未报道的鬼臼毒素衍生物,其结构经1H-NMR、13C-NMR、HR-ESI-MS及熔点测定分析确证。抗肿瘤活性筛选结果表明所有目标化合物均具有不同程度的体外细胞毒活性,大部分化合物对耐药的K562细胞具有较好的细胞毒活性。结论 通过对鬼臼毒素进行结构修饰,能够增强其抗肿瘤活性。
英文摘要:
      Objective To modify the structure of podophyllotoxin derivatives and evaluate the antitumor activities of the derivatives. Methods The target compounds were synthesized by multi-step reaction with podophyllotoxin and aldehyde compound as starting material.. MTT assay was used to test antitumor activity of all the target compounds on Hela cells, K562 cells, and K562/A02 cell. Results Eleven novel derivatives were synthesized which had not been reported in any literature and the structures were characterized by 1H-NMR, 13C-NMR, HR-ESI-MS and melting point determination analysis. The antitumor activity screening results showed that all the target compounds had different degrees of cytotoxic activity in vitro. Most of the compounds had significant anti-MDR activity in vitro. Conclusion Through structural modification of podophyllotoxin derivatives, the antineoplastic activities are enhanced.
HTML  查看全文  查看/发表评论  下载PDF阅读器
关闭
您是第 21950120 位访客
版权所有: 天津中草药杂志社(天津市南开区鞍山西道308号 300193)
Address: 308# An-shan West Road, Nankai District, Tianjin, China Post Code: 300193
Tel: +86-22-27474913; 23006821 Fax: 022-23006821 E-mail:zcy@tiprpress.com
津备案:津ICP备13000267号   互联网药品信息服务资格证书编号:(津)-非经营性-2015-0031