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。
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.
出处
《化学与生物工程》
CAS
2012年第5期8-11,共4页
Chemistry & Bioengineering
基金
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)
