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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。
In this paper, the preparation of polyrotaxane-camptothecin conjugates and their antitumor effects were studied. Polyrotaxane-camptothecin conjugates were prepared and their in vitro release behavior was studied. MTT assay and morphology were used to investigate the inhibitory effect of conjugate on the proliferation of ovarian cancer cell line A2780 in vitro. The growth of tumor-bearing mice, to further evaluate the anti-tumor effect of the conjugate. The results showed that the polyrotaxane-camptothecin conjugates significantly inhibited the proliferation of ovarian cancer cell line A2780 and showed a dose-response relationship. The effect of the polyrotaxane-camptothecin conjugate on the growth of S180 tumor-bearing mice showed that the polyrotaxane- The degree of infiltration and the number of blood vessels, suggesting that its anti-tumor mechanism may be through the impact of tumor angiogenesis, reducing blood supply and lead to tumor necrosis.