Yu Fei, Xie Ying, Wang Yan, Peng Zheng-Hong, Li Jing, Oupický David
Center for Drug Delivery and Nanomedicine, Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, Nebraska 68198, United States.
ACS Macro Lett. 2016 Mar 15;5(3):342-345. doi: 10.1021/acsmacrolett.5b00857. Epub 2016 Feb 17.
Chloroquine-containing HPMA copolymers (pCQs) were synthesized for the first time by copolymerization of methacryloylated hydroxychloroquine and HPMA. The copolymers showed lower cytotoxicity when compared with hydroxychloroquine. Treatment of cancer cells with pCQ resulted in decreased surface expression of chemokine receptor CXCR4. The pCQ copolymers showed effective inhibition of CXCR4/SDF1-mediated cancer cell migration that was fully comparable with a commercial small-molecule CXCR4 antagonist AMD3100. The reported pCQ represent unique and simple polymeric drugs with potential use as part of a combination antimetastatic therapies.
含氯喹的HPMA共聚物(pCQs)首次通过甲基丙烯酰化羟氯喹与HPMA的共聚反应合成。与羟氯喹相比,这些共聚物表现出较低的细胞毒性。用pCQ处理癌细胞导致趋化因子受体CXCR4的表面表达降低。pCQ共聚物显示出对CXCR4/SDF1介导的癌细胞迁移的有效抑制,这与市售小分子CXCR4拮抗剂AMD3100完全相当。所报道的pCQ代表了独特且简单的聚合物药物,具有作为联合抗转移疗法一部分的潜在用途。