| 2β-羟基熊果酸的合成及其抗肿瘤活性 |
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| 引用本文： | 黄丽荣,陈磊,杨小生,马琳,张建新,王道平.2β-羟基熊果酸的合成及其抗肿瘤活性[J].应用化学,2013,30(10):1133-1138. |
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| 作者姓名： | 黄丽荣 陈磊 杨小生 马琳 张建新 王道平 |
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| 作者单位： | (1.贵州大学精细化工研究开发中心教育部绿色农药与农业生物工程重点实验室 贵阳 550025；
2.中国科学院天然产物化学重点实验室 贵阳 550002) |
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| 基金项目： | 国家自然科学基金，贵州省科技厅基金 |
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| 摘 要： | 以熊果酸为原料，经C-3羟基氧化、C-28羧基苄酯化保护、C-2乙酰化及水解、还原、脱保护得到2β-羟基熊果酸，6步反应的总收率为60.1%。 中间体及目标化合物结构经IR、1H NMR、13C NMR和MS测试技术确证。 以噻唑蓝(MTT)比色法检测2β-羟基熊果酸对人白血病细胞K562及人肺癌细胞A549肿瘤细胞的体外抑制活性，结果表明，对2种肿瘤细胞的生长均表现出一定的抑制作用。
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| 关 键 词： | 熊果酸 2&beta -羟基熊果酸 合成 体外肿瘤细胞抑制活性 |
| 收稿时间： | 2012-12-03 |
| 修稿时间： | 2013-01-11 |
Synthesis and Antitumor Activity of 2β-Hydroxyursolic Acid |
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| HUANG Lirong
,
CHEN Lei
,
YANG Xiaosheng
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MA Lin
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ZHANG Jianxin
,
WANG Daoping.Synthesis and Antitumor Activity of 2β-Hydroxyursolic Acid[J].Chinese Journal of Applied Chemistry,2013,30(10):1133-1138. |
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| Authors: | HUANG Lirong CHEN Lei YANG Xiaosheng MA Lin ZHANG Jianxin WANG Daoping |
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| Institution: | (1.Ministry of Education Key Laboratory of Green Pesticide and Ago-Bioengineering,Center for ;
Research and Development of Fine Chemicals of Guizhou University,Guiyang 550025,China;
2.The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550002,China) |
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| Abstract: | Using ursolic acid as the precursor, 2β-hydroxyursolic acid was synthesized by 6-step successive reactions including oxidation, benzylation, acetylation, hydrolysis, reduction, and group deprotection reactions. The overall yield is 60.1%. Its structure was determined by IR, 1H NMR, 13C NMR and MS. The antitumor activity of the target compound was evaluated against the proliferation of human leukemia cell K562 and human lung carcinoma cell A549 by the MTT assay. The results indicate that the target compound has inhibitive activity toward cell growth for the two tumor cells. |
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| Keywords: | ursolic acid 2β-hydroxyursolic acid synthesis inhibition activity to tumor cell |
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