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薯蓣皂苷元衍生物的合成和抗肿瘤活性研究
引用本文:董江红,何谷,吴亚克,万剑飞,范举正.薯蓣皂苷元衍生物的合成和抗肿瘤活性研究[J].中国药学杂志,2012,47(17):1407-1414.
作者姓名:董江红  何谷  吴亚克  万剑飞  范举正
作者单位:四川大学华西药学院;四川大学华西医院生物治疗国家重点实验室
摘    要:目的合成薯蓣皂苷元衍生物并研究其体外抗肿瘤活性。方法以薯蓣皂苷元为原料,选择性地合成一系列运用AutoDock4.2对接设计的薯蓣皂苷元衍生物。采用噻唑蓝(MTT)法考察了目标化合物对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2以及人慢性髓原白血病细胞K562进行体外抗肿瘤活性试验。结果合成12个新化合物,其结构经1H-NMR和13C-NMR确定,药理实验结果表明,大部分化合物有一定的抗肿瘤活性。结论大部分化合物有良好的抗肿瘤活性而对正常细胞无毒或低毒性。

关 键 词:薯蓣皂苷元衍生物  合成  噻唑蓝法  AutoDock4.2  抗肿瘤活性
收稿时间:2012-09-12;

Synthesis and Anticancer Activity Study of Diosgenin Derivatives
DONG Jiang-hong,HE Gu,WU Ya-ke,WAN Jian-fei,FAN Ju-zheng.Synthesis and Anticancer Activity Study of Diosgenin Derivatives[J].Chinese Pharmaceutical Journal,2012,47(17):1407-1414.
Authors:DONG Jiang-hong  HE Gu  WU Ya-ke  WAN Jian-fei  FAN Ju-zheng
Institution:1(1.West China School of Pharmacy,Sichuan University,Chengdu 610041,China;2.State Key Laboratory of Biotherapy and Cancer Center,West China Hospital,Sichuan University,Chengdu 610041,China)
Abstract:OBJECTIVE To synthesize diosgenin derivatives and investigate their anti-tumor activities in vitro. METHODS Designed and docked by AutoDock4.2,a series of diosgenin derivatives were selectively prepared from diosgenin. Their anti-tumor activities in vitro were evaluated for human malignant melanoma A375 cells,human lung adenocarcinoma A549 cells,human hepatoma HepG-2 cells and human myeloid leukemia K562 cells by MTT assay. RESULTS Twelve novel compounds were synthesized and the basic structures were characterized by 1H-NMR and 13C-NMR. MTT assay showed that most of the diosgenin derivatives exhibited some anti-tumor activities.CONCLUSION Most of the synthesized compounds had certain antitumor activity and showed no or little toxicity against the normal cells.
Keywords:diosgenin derivatives  synthesis  MTT assay  AutoDock4  2  antitumor activity
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