| 积雪草酸C2、C3、C23、C28衍生物的合成及其体外抗肿瘤活性研究 |
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| 引用本文： | 孟艳秋,赵敏杰,张译,刘立伟,刘冬莹.积雪草酸C2、C3、C23、C28衍生物的合成及其体外抗肿瘤活性研究[J].现代药物与临床,2015,30(4):355-361. |
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| 作者姓名： | 孟艳秋 赵敏杰 张译 刘立伟 刘冬莹 |
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| 作者单位： | 沈阳化工大学制药工程教研室,辽宁沈阳,110142 |
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| 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资助项目(LR2013017);沈阳市科技计划资助项目(F13-316-1-47) |
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| 摘 要： | 目的设计并合成积雪草酸C2、C3、C23、C28衍生物,并对其体外抗肿瘤活性进行研究。方法以天然产物积雪草酸为先导化合物,对C2、C3、C23位羟基及C28位羧基进行结构改造,并采用SRB法对目标化合物进行初步的体外抗肿瘤活性研究。结果设计并合成了目标化合物,利用MS及1H-NMR确证了结构;体外实验中,积雪草酸衍生物的抗肿瘤活性明显高于积雪草酸,并优于对照药吉非替尼。结论积雪草酸衍生物具有良好的抗肿瘤活性,值得进一步研究。
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| 关 键 词： | 积雪草酸 结构改造 合成 抗肿瘤活性 |
| 收稿时间： | 2015/1/13 0:00:00 |
Synthesis of asiatic acid C2, C3, C23, and C28 derivatives and their antitumor activities in vitro |
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| MENG Yan-qiu,ZHAO Min-jie,ZHANG Yi,LIU Li-wei and LIU Dong-ying.Synthesis of asiatic acid C2, C3, C23, and C28 derivatives and their antitumor activities in vitro[J].Drugs & Clinic,2015,30(4):355-361. |
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| Authors: | MENG Yan-qiu ZHAO Min-jie ZHANG Yi LIU Li-wei and LIU Dong-ying |
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| Institution: | College of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China;College of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China;College of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China;College of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China;College of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China |
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| Abstract: | Objective To design and synthesize asiatic acid C2, C3, C23, and C28 derivatives, and to study their antitumor activities in vitro. Methods Asiatic acid was used as starting material to synthesize the target compounds by structural modification at C2, C3, and C23 hydroxyl groups, and C28 carboxyl group. The antitumor activities of the compounds were tested by SRB assay. Results The target compounds were synthesized and characterized by MS and 1H- NMR. The in vitro antitumor activity experiments showed that the antitumor activity of asiatic acid derivatives were higher than those of asiatic acid in vitro, and were better than control drug gefitinib. Conclusion Asiatic acid derivatives have good antitumor activities which could be a valuable candidate for further development. |
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| Keywords: | asiatic acid structure modification synthesis antitumor activity |
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