| 18β-甘草次酸A环官能团化衍生物的合成及抗肿瘤活性 |
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| 引用本文： | 高振北,胡君,康潇,许传莲,巨勇. 18β-甘草次酸A环官能团化衍生物的合成及抗肿瘤活性[J]. 高等学校化学学报, 2012, 33(4): 750-754. DOI: 10.3969/j.issn.0251-0790.2012.04.019 |
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| 作者姓名： | 高振北 胡君 康潇 许传莲 巨勇 |
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| 作者单位： | 1. 浙江理工大学生命科学学院, 杭州 310018;2. 清华大学化学系, 生命有机磷化学及化学生物学教育部重点实验室, 北京 100084 |
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| 基金项目： | 浙江省自然科学基金，浙江省生物医学工程“重中之重”学科开放基金，国家自然科学基金 |
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| 摘 要： | 采用化学方法对18β-甘草次酸A环进行改造, 合成了一系列新型18β-甘草次酸A环官能团化衍生物. 对人白血病细胞株HL-60、K562、肝癌细胞BEL-7404及乳腺癌细胞MDA-MB-231的体外抗肿瘤活性筛选结果表明, 化合物5对4种肿瘤细胞系的抑制活性均强于18β-甘草次酸; 构效关系分析表明, A环内烯键的形成对抑制肿瘤细胞增殖有重要影响; 同时利用Hoechst33258和AO/EB染色, 在荧光显微镜下观察到了细胞凋亡小体的形成.
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| 关 键 词： | 18β-甘草次酸 结构改造 A环官能团化衍生物 抗肿瘤细胞增殖活性 |
| 收稿时间： | 2011-05-06 |
Synthesis of A-Ring Functional Derivatives of 18β-Glycyrrhetinic Acid and Their Antiproliferative Effect in Tumor Cells |
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| GAO Zhen-Bei , HU Jun , KANG Xiao , XU Chuan-Lian , JU Yong. Synthesis of A-Ring Functional Derivatives of 18β-Glycyrrhetinic Acid and Their Antiproliferative Effect in Tumor Cells[J]. Chemical Research In Chinese Universities, 2012, 33(4): 750-754. DOI: 10.3969/j.issn.0251-0790.2012.04.019 |
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| Authors: | GAO Zhen-Bei HU Jun KANG Xiao XU Chuan-Lian JU Yong |
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| Affiliation: | 1. College of Life Science, Zhejiang Sci-Tech University, Hangzhou 310018, China;2. Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China |
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| Abstract: | Thirteen analogues of 18β-glycyrrhetinic acid were synthesized using various chemical methods and one of them exhibited certain cytotoxicity against cell-lines of HL60 cells,K562 cells,BEL-7404 cells and MDA-MB-231,respectively,via MTT method.The results show that compound 5 with C-C bond in the A-ring of 18β-glycyrrhetinic acid has markedly antiproliferative effect on these four tumor cells compared with 18β-glycyrrhetinic acid.K562 cells with nuclear apoptotic bodies were observed after staining with Hoechst 33258 and AO/EB with flourescence microscope. |
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| Keywords: | 18β-Glycyrrhetinic acid Chemical modification A-Ring functional derivative Antiproliferative effect |
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