1-[3-[2-[1-(5-氟-尿嘧啶基)]乙酰氨基]丙基]-2,8,9-三氧杂-5-氮杂-1-硅三环[3,3,3,0^(1,5)]十一烷的抗肿瘤活性研究  

Study on antitumor activity of 1-[3-[2-[1-(5-fluoro-uracil)]acetamide]propyl]-2,8,9-trioxa-5azal-1-silicontricyclo[3,3,3,0^(1,5)]undecane

作　　者：张庆伟[1] 叶发青[1] 郭平[1] 刘剑敏[1] 胡黎川[2] 

机构地区：[1]温州医学院药学院,浙江温州325035 [2]温州市第二人民医院药剂科,浙江温州325000

出　　处：《温州医学院学报》2009年第4期311-313,共3页Journal of Wenzhou Medical College

基　　金：浙江省自然科学基金资助项目(Y204089)

摘　　要：目的:探讨化合物1-[3-[2-[1-(5-氟-尿嘧啶基)]乙酰氨基]丙基]-2,8,9-三氧杂-5-氮杂-1-硅三环[3,3,3,01,5]十一烷(目标化合物)对人宫颈癌Hela细胞、人结肠癌SW480细胞、人肺腺癌A549细胞的抗肿瘤效应。方法:将化合物用培养液配制成浓度分别为25、50、100、200和400mg/L的溶液,采用四甲基偶氮唑盐比色分析法(MTT法)测试其对Hela细胞、SW480细胞和A549细胞的体外抗肿瘤活性。结果:化合物对人宫颈癌Hela细胞无显著性抑制作用;对SW480细胞和A549细胞具有明显抑制作用,在测定浓度范围内,随着浓度的增加,抑制率也在增加,呈现良好的剂量依赖性,其中对SW480抑制率最高,在400mg/L浓度下,抑制率达50.2%。结论:目标化合物对某些肿瘤细胞具有选择性抑制作用。Objective： To explore the antitumor activity of the compound 1-[3-[2-[1-（5-fluoro-uracil）]acetamide]propy1]-2, 8, 9-trioxa-5-azal-1-silicontricyclo[3, 3, 3,0^1,5]undecane on Hela, SW480 and A549. Methods ： The concentration of the compound was prepared as 25, 50, 100, 200, 400 mg/L using culture media. The antitumor activity on Hela, SW480 and A549 was analyzed with MTT method. Results： The compound showed no inhibitive effect in vitro on Hela and the inhibition ratio depended on the increasing concentration. The inhibitive effect on SW480 was the highest, which was up to 50.2% under the 400 mg/L concentration. Conclusion： The compound shows an elective antitumer activity.

关 键 词：5-氟尿嘧啶 杂氮硅三环 抗肿瘤 比色法 

分 类 号：O621.29[理学—有机化学]