促黄体激素释放激素-甲氨蝶呤的合成及抗肿瘤活性  

Synthesis and anti-tumor activity of luteinizing hormone-releasing hormone-methotrexate

作　　者：吴学萍[1] 谢明均[2] 孙艳[1] 潘黎军[1] 王驰[1] 

机构地区：[1]重庆医科大学药学院药物化学教研室,重庆400016 [2]宜宾市第二人民医院,宜宾644000

出　　处：《中国新药杂志》2010年第17期1609-1612,共4页Chinese Journal of New Drugs

摘　　要：目的:合成促黄体激素释放激素-甲氨蝶呤(LH-RH-MTX)并研究其抗肿瘤活性。方法:将APA与[D-Lys6]LH-RH共价连接合成LH-RH-MTX;用半制备型反相HPLC进行纯化与定量,用ESI-MS进行结构确证;应用MTT法检测其对人卵巢癌SKOV-3细胞的抗肿瘤活性。结果:LH-RH-MTX的纯度为98.00%,产率为61.96%;ESI-MS分析得产物分子量为1 268.15。MTT实验结果表明LH-RH-MTX对人卵巢癌SKOV-3细胞具有明显的抗肿瘤活性。结论:LH-RH-MTX可与表达有LH-RH受体的肿瘤细胞特异性结合并发挥作用,作用优于游离MTX。Objective： To synthesize luteinizing hormone-releasing hormone-methotrexate（LH-RH-MTX） and investigate its anti-tumor activity.Methods： LH-RH-MTX was synthesized from APA by coupling with [D-Lys6] LH-RH.The crude product was analyzed,purified and quantified by Beckman semi-preparative HPLC,and its molecular weight was determined by ESI-MS.MTT assay was applied to examine its anti-tumor activity on oophoroma SKOV-3 cells.Results： The purity of LH-RH-MTX was 98.00% with the yield of 61.69%.Its molecular weight was 1 268.15 m/z by ESI-MS analysis.The prepared LH-RH-MTX had significant anti-tumor activity on oophoroma SKOV-3 cells in vitro.Conclusion： LH-RH-MTX can incorporate specifically with the tumor cells with LH-RH receptors,whose action is better than that of free MTX.

关 键 词：促黄体激素释放激素 甲氨蝶呤 合成 抗肿瘤活性 人卵巢癌SKOV-3细胞 

分 类 号：R914.5[医药卫生—药物化学] R979.1[医药卫生—药学]