Synthesis and anti-tumor activity of NO-donating derivatives of gambogic acid  

作　　者：WANG Jin-Xin ZHANG Bai-Hon~ XU Dan-Dan MIAO Guang-Qiang WANG Fan GUO Qing-Long YOU Qi-Dong 

机构地区：[1]Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China [2]Department of Oncology, General Hospital of People's Liberation Army, Lanzhou 730050, China [3]Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China

出　　处：《中国天然药物》2013年第1期87-96,共10页

基　　金：This project was supported by the National Natural Science Foundation of China （Nos. 30873157, 21072231）.

摘　　要：试图从 gambogic 酸和它的衍生物发现有势力 apoptosis inducer。gambogic 酸的八新不捐赠的衍生物作为潜在的反肿瘤被综合的方法在 HT-29， Bel-7402， BGC-823，和 A549 房间线上带混合物和他们的禁止的活动被 MTT 试金在 vitro 评估。在这些混合物之中的结果， 4 通过 MTT 房间试金，词法变化的观察，和 Annexin-V/PI 作为 SKOV3 房间 apoptosis inducer 与在 gambogic 酸一半的 C35 的一个氢氧根组一起被识别两倍染色的试金。在导致 apoptosis 和力量的结论化合物 4 显示出的重要效果为新 anticancer 药的发现用作潜在的铅混合物。AIM： To find a potent apoptosis inducer from gambogic acid and its derivatives. METHODS： Eight new NO-donating derivatives of gambogic acid were synthesized as potential anti-tumor lead compounds and their inhibitory activity on the HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by the MTF assay. RESULTS： Among these compounds, 4 with a hydroxyl group at C35 of the gambogic acid moiety was identified as a SKOV3 cell apoptosis inducer through the MTF cell assay, observations of morphological changes, and Annexin-V/PI double staining assay. CONCLUSION： Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for the discovery of new anticancer drugs.

关 键 词：藤黄酸及其衍生物 细胞凋亡诱导剂 NO 抗肿瘤活性 

分 类 号：R284.3[医药卫生—中药学] R965[医药卫生—中医学]