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| 藤黄酸构效关系的研究 | |
| 引用本文： | 李念光,尤启冬,黄雪峰,王进欣,郭青龙,陈晓光,李燕,李洪燕.藤黄酸构效关系的研究[J].中国天然药物,2008,6(1):37-42. |
| 作者姓名： | 李念光 尤启冬 黄雪峰 王进欣 郭青龙 陈晓光 李燕 李洪燕 |
| 作者单位： | 1. 江苏省肿瘤发生与干预重点实验室,南京,210009;中国药科大学药物化学教研室,南京,210009;南京中医药大学药物化学教研室,南京,210046 2. 江苏省肿瘤发生与干预重点实验室,南京,210009;中国药科大学药物化学教研室,南京,210009 3. 江苏省肿瘤发生与干预重点实验室,南京,210009;中国药科大学生理学教研室,南京210009 4. 中国医学科学院中国协和医科大学药物研究所,北京,100050 |
| 基金项目： | 国家高技术研究发展计划(863计划) , 国家教育委员会重大科技攻关项目 , 江苏省自然科学基金 |
| 摘 要： | 目的：研究藤黄酸的构效关系。方法：通过对天然产物藤黄酸的结构剖析，在去除复杂桥环结构的基础上．合成了色酮和讪酮2个系列的化合物。并通过MTT法对其进行了初步的药理实验活性筛选。结果：这些具有平面环结构的小分子化合物的活性虽然比藤黄酸的活性要低，但是引入异戊烯基能显著提高其抗肿瘤活性。结论：藤黄酸结构中的异戊烯基和桥环结构对其抗肿瘤活性有着很重要的作用。 |
| 关 键 词： | 藤黄酸 小分子化合物 抗肿瘤活性 |
| 文章编号： | 1672-3651（2008）01-0037-06 |
| 收稿时间： | 2007-04-13 |
| 修稿时间： | 2007年4月13日 |
Structure-activity Relationship of Gambogic Acid |
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| LI Nian-Guang,YOU Qi-Dong,HUANG Xue-Feng,WANG Jin-Xin,GUO Qing-Long,CHEN Xiao-Guang,LI Yan,LI Hong-Yan.Structure-activity Relationship of Gambogic Acid[J].Chinese JOurnal of Natural Medicines,2008,6(1):37-42. | |
| Authors: | LI Nian-Guang YOU Qi-Dong HUANG Xue-Feng WANG Jin-Xin GUO Qing-Long CHEN Xiao-Guang LI Yan LI Hong-Yan |
| Institution: | LI Nian-Guang, YOU Qi-Dong , HUANG Xue-Feng, WANG Jin-Xin, GUO Qing-Long, CHEN Xiao-Guang , LI Yan , LI Hong-Yan(1Key Laboratory of Carcinogesis and Intervention of Jiangsu Province, Nanfing 210009; 2 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009; 3 Department of Physiology, China Pharmaceutical University, Nanjing 210009 ; 4 Department of Medicinal Chemistry, Nanfing University of Traditional Chinese Medicine, Nanfing 210046; 5 Institute of Materia Medica, Chinese Academy of Medical Sciences ＆ Peking Union Medical College, Beijing 100050, China) |
| Abstract: | AIM: To investigate the basic structure-activity relationship of gambogic acid. METHODS: Through simplifying the complex skeleton of the natural gambogic acid, two series of derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. RESULTS: The cytotoxic activities of all these small compounds with planar ring were much less potent than those of the natural gambogic acid, and the introduction of prenyl to these small molecular compounds could increase their antitumor activities. CONCLUSION: The structure-activity relationship of synthesized compounds indicated that the prenyl groups and the bridgecore in gambogic acid were very important for keeping its antitumor activities. |
| Keywords: | Gambogic acid Small molecular compounds Antitumor activity |
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