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聚轮烷-喜树碱缀合物的合成及其抗肿瘤效果评估

[Synthesis of polyrotaxane-camptothecin conjugates and evaluation of its anti-tumor effect].

作者信息

Lai Chun-li, Lai Le, Zhao Jian-bin, Chen Jian-hai

机构信息

Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.

出版信息

Yao Xue Xue Bao. 2010 Jul;45(7):920-5.

Abstract

To prepare polyrotaxane-camptothecin conjugates and evaluate its anti-tumor effect, polyrotaxane-camptothecin conjugates 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. The result indicated anti-tumor mechanism may be through affect the angiogenesis and reduced blood supply to tumor cells and then leading to necrosis.

摘要

为制备聚轮烷-喜树碱缀合物并评估其抗肿瘤效果,成功合成了聚轮烷-喜树碱缀合物,并进行了释放行为研究;采用MTT法和细胞形态学观察体外细胞增殖抑制作用。还进行了对S180小鼠体内抗肿瘤作用的实验研究,以进一步评估缀合物的抗肿瘤效果。结果表明聚轮烷-喜树碱缀合物能以剂量依赖性方式有效抑制细胞增殖。对S180小鼠的体内研究和细胞形态学观察显示肿瘤生长、肿瘤浸润程度和血管数量显著减少。结果表明其抗肿瘤机制可能是通过影响血管生成,减少肿瘤细胞的血液供应,进而导致坏死。

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