| 两个海洋环肽Galaxamide类似物的合成及抗肿瘤活性研究 |
| |
| 引用本文： | 陈萌,曲桐,徐石海.两个海洋环肽Galaxamide类似物的合成及抗肿瘤活性研究[J].湖北化工,2012(5):8-11. |
| |
| 作者姓名： | 陈萌 曲桐 徐石海 |
| |
| 作者单位： | 暨南大学生命科学技术学院化学系,广东广州510632 |
| |
| 基金项目： | 国家高技术研究发展计划（863计划）资助项目（2006AA09Z408）; 国家自然科学基金资助项目（20772048） |
| |
| 摘 要： | 以亮氨酸为起始原料,改变环合位点,全合成了两个海洋环肽Galaxamide环（亮氨酰-N-甲基亮氨酰-亮氨酰-N-甲基亮氨酰-亮氨酰）]类似物。通过1 HNMR、13 CNMR、MS对其结构进行了表征,并对人肝癌细胞（HepG2）、人肺癌细胞（A549）、人宫颈癌细胞（Hela）进行了体外抗肿瘤活性的研究。结果表明,含有D构型的环肽能增强抗肿瘤活性,而环肽氮上甲基数量的增多并不能增强环肽抗肿瘤活性。
|
| 关 键 词： | Galaxamide 类似物 全合成 抗肿瘤活性 |
Study on Synthesis and Anti-Tumor Activity of Two Galaxamide Analogues |
| |
| CHEN Meng,QU Tong,XU Shi-hai.Study on Synthesis and Anti-Tumor Activity of Two Galaxamide Analogues[J].Hubei Chemical Industry,2012(5):8-11. |
| |
| Authors: | CHEN Meng QU Tong XU Shi-hai |
| |
| Affiliation: | (Department of Chemistry,College of Life Science and Technology, Jinan University,Guangzhou 510632,China) |
| |
| Abstract: | Two analogues of Galaxamide cyclo（Leu-N-Me-Leu-Leu-N-Me-Leu-Leu）,which was derived from marine and possessed anti-tumor activity with leucine（Leu） as starting material through changing the cyclization sites.The structures of the products and intermediates were characterized by 1HNMR,13CNMR and MS.And their anti-tumor activity in vitro was investigated through the MTT assay for human hepatoma carcinoma cell HepG2,human lung cancer cell A549 and human cervical carcinoma cell Hela.Cyclic peptide with D-configuration enhanced their anti-tumor activity,but increasing N-methyl amount of cyclic peptide didn′t enhance their anti-tumor activity. |
| |
| Keywords: | Galaxamide analogues total synthesis anti-tumor activity |
| 本文献已被 维普 等数据库收录！ |
