聚轮烷－喜树碱偶联物的制备及抗肿瘤作用.pdfVIP

920 药学学报 Acta Pharmaceutica Sinica 2010, 45 (7) : 920925 聚轮烷-喜树碱偶联物的制备及其抗肿瘤作用 赖春丽, 乐, 赵建彬, 陈建海* (南方医科大学南方医院, 广东 广州 510515) 摘要: 本文研究了聚轮烷-喜树碱偶联物的制备及其抗肿瘤作用。制备了聚轮烷-喜树碱偶联物, 并对其体外 释药行为进行研究; MTT 法及形态学考察偶联物对卵巢癌细胞株 A2780 的体外增殖抑制作用; 考察偶联物对 S180 荷瘤小鼠的生长影响, 进一步评价偶联物抗肿瘤效果。结果表明, 聚轮烷-喜树碱偶联物对卵巢癌细胞株 A2780 的增殖有明显抑制作用, 且呈量效关系; 对 S180 荷瘤小鼠的生长影响结果表明能显著减少肿瘤的生长、浸 润程度以及血管数量, 提示其抗肿瘤作用机制可能是通过影响肿瘤的血管生成, 减少供血而导致肿瘤细胞坏死。 关键词: 偶联物; 制备; 抗肿瘤作用 中图分类号: R943 文献标识码:A 文章编号: 05 13-4870 (2010) 07-0920-06 Synthesis of polyrotaxane-camptothecin conjugates and evaluation of its anti-tumor effect * LAI Chun-li, LAI Le, ZHAO Jian-bin, CHEN Jian-hai (Nanf ang Hosp ital, Southern Medical University, Guangzhou 510515, China) Abstract: To prepare polyrotaxane-camptothecin conjugates and evaluate its anti-tumor effect, polyrotaxane- camptothecin conj ugates were successfully synthesized, and the release behavior was performed; MTT assay and cell morphology were used to examine the inhibition of cells proliferation effect in vitro. The experimental study of the antitumor effect on S180 mice in vivo was also performed to further evaluate the anti-tumor effect of conjugate. The result showed polyrotaxane-camptothecin conjugates can effectively inhibit the proliferation in a dose dependent effect. In vivo study and cell morphology observation of S180 mice showed significant decrease in growth of tumor, degree of tumor infiltration and blood vessel number. Th