3-氧代齐墩果酸氨基酸偶联物的合成、水溶性的测定及抗肿瘤活性研究

目的设计合成3-氧代齐墩果酸氨基酸偶联物，并测试其水溶性和体外抗肿瘤活性。方法利用HPLC法测定具有代表性结构的偶联物的水溶性，并采用MTT法测试这些偶联物对KB和KB／V两种癌细胞的抑制活性。结果共合成9个新化合物，其结构经核磁共振氢谱和质谱确证。结论被测试的6个偶联物的水溶性与3-氧代齐墩果酸相比有不同程度的改善，水溶性大小顺序是5e〉5g〉5c〉5d〉5a〉5b和3-氧代齐墩果酸。初步体外抗肿瘤活性结果表明，水溶性较高的偶联物（5e，5g，se）仍保持抗肿瘤活性。

Synthesis, water solubility and antitumor activity of amino acid conjugates of 3-oxooleanolic acid

Aim To design and synthesize a series of amino acid conjugates of 3-oxooleanolic acid,and to determine their water solubility and antitumor activities in vitro.Methods Water solubility of representative synthesized conjugates were determined with HPLC.Their antitumor activities were evaluated using KB and KB/V cells by MTT.Results Nine new compounds were obtained and characterized by 1H-NMR spectra and ESI-MS.Conclusion Water solubility of six conjugates showed various degrees improvement than 3-oxooleanolic acid.The order of water solubility is 5e>5g>5c>5d>5a>5b and 3-oxooleanolic acid.Preliminary antitumor bioassay showed that conjugates bearing higher water solubility retained antitumor activity.