| 齐墩果酸衍生物的合成及抗肿瘤活性的研究 |
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| 作者姓名： | Meng YQ Nie HH Wang XC Li D Ge CX Zhao N Chen H Cao B |
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| 作者单位： | 沈阳化工大学制药工程教研室;中国人民解放军武警医学院生药学教研室; |
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| 基金项目： | 教育部留学回国人员基金资助项目(20080890); 辽宁省教育厅高等学校科学研究重点项目(L2010433) |
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| 摘 要： | 以天然产物齐墩果酸为先导化合物,经过氧化、酯化(酰化)、水解等反应设计合成了10个齐墩果酸衍生物,以HeLa、HepG2和BGC-823细胞为靶细胞,采用MTT法用吉非替尼和依托泊苷作阳性对照,进行初步的体外抗肿瘤活性筛选。结果表明,化合物5a对HepG2细胞、化合物7对HeLa细胞的抑制活性明显高于母体齐墩果酸。因此,化合物5a和7值得进一步研究。
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| 关 键 词： | 齐墩果酸 五环三萜化合物 抗肿瘤活性 |
Synthesis and anti-tumor activity of oleanolic acid derivatives |
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| Meng YQ,Nie HH,Wang XC,Li D,Ge CX,Zhao N,Chen H,Cao B.Synthesis and anti-tumor activity of oleanolic acid derivatives[J].Acta Pharmaceutica Sinica,2011,46(10):1215-1220. |
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| Authors: | Meng Yan-qiu Nie Hui-hui Wang Xiao-chen Li Dan Ge Chong-xun Zhao Na Chen Hong Cao Bo |
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| Institution: | MENG Yan-qiu1,NIE Hui-hui1,WANG Xiao-chen1,LI Dan1,GE Chong-xun1,ZHAO Na1,CHEN Hong2,CAO Bo2(1.Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Shenyang 110142,China,2.Department of Pharmacognosy,Medical College of Chinese People's Armed Police Forces,Tianjin 300162,China) |
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| Abstract: | Structural modifications were performed with natural product of oleanolic acid to search for novel anticancer drugs.Ten oleanolic acid derivatives were designed and obtained by the reaction of oxidation,acylation or hydrolyzation,etc.The cytotoxic activity of derivatives was evaluated against HeLa,HepG2 and BGC-823 cells in vitro by MTT assay,gefitinib and etoposide used as a positive control.The results showed that compound 5a was particularly active to inhibit HepG2 cells growth,and anti-tumor activity of... |
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| Keywords: | oleanolic acid pentacyclic triterpenoid anti-tumor activity |
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