论文部分内容阅读
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 LH-RH-MTX and study its anti-tumor activity. METHODS: LH-RH-MTX was synthesized by covalently linking APA with [D-Lys6] LH-RH. The purified product was purified by semi-preparative reverse phase HPLC and confirmed by ESI-MS. Antitumor activity of ovarian cancer SKOV-3 cells. Results: The purity of LH-RH-MTX was 98.00%, the yield was 61.96%. The molecular weight of product was 1 268.15 by ESI-MS. MTT results show that LH-RH-MTX has obvious anti-tumor activity on human ovarian cancer SKOV-3 cells. Conclusion: LH-RH-MTX can specifically bind with LH-RH receptor-expressing tumor cells and play a role better than free MTX.