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Strategies of porous network quinolone polymers: A comprehensive evaluation of their biological activity
Dyes and Pigments ( IF 4.5 ) Pub Date : 2020-08-29 , DOI: 10.1016/j.dyepig.2020.108809
Tingyu Shao , Fuyan Xiao , Yuling Wang , Guofan Jin

Hydrazine polymers were synthesized under the condition of hydrazine hydrate/ethanol by a clever one-pot method, and then treated with methanesulfonyl chloride and acetyl chloride, respectively, two new quinolones were easily obtained. The basic structure characterization of the prepared quinolone polymers was established based on 1H NMR spectra of aromatic rings and branched chains. In terms of cell activity, MTT assay was used to study the anti-proliferation properties of HCT-116, A549, HepG-2, and McF-7 human cancer cell lines and normal cell lines L02 compared with positive control 5-FU.The distribution and nucleation of polymeric drugs in cells were further observed by means of cell imaging. Conventional Annexin V-FITC kit was subsequently used to detect cell cycle arrest with propidium iodide (PI)and to monitor apoptosis induction with flow cytometry. The results showed that both of the novel quinolone polymers had strong cytotoxic compounds to induce cell cycle stop and trigger apoptosis in the G2/M phase in different test cancer cells. In particular, polymer 1 was more effective.



中文翻译:

多孔网络喹诺酮类聚合物的策略:对其生物学活性的综合评估

通过巧妙的一锅法在水合肼/乙醇的条件下合成肼聚合物,然后分别用甲磺酰氯和乙酰氯处理,轻松获得了两种新的喹诺酮。基于芳环和支链的1 H NMR谱图,建立了所制喹诺酮聚合物的基本结构表征。在细胞活性方面,MTT法用于研究HCT-116,A549,HepG-2和McF-7人癌细胞系和正常细胞L02与阳性对照5-FU的抗增殖特性。通过细胞成像进一步观察聚合物在细胞中的分布和成核。随后使用常规的膜联蛋白V-FITC试剂盒检测碘化丙啶(PI)引起的细胞周期停滞,并通过流式细胞术监测凋亡诱导。结果表明,两种新型喹诺酮类聚合物均具有较强的细胞毒性化合物,可以诱导细胞周期停止并触发不同测试癌细胞中G2 / M期的凋亡。特别地,聚合物1更有效。

更新日期:2020-09-03
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