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Transferrin-conjugated liposomes loaded with novel dihydroquinoline derivatives as potential anticancer agents.
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- المؤلفون: Wang, Mengqiao1; Lee, Robert J.1,2; Bi, Ye1; Li, Lianlian1; Yan, Guodong1; Lu, Jiahui1; Meng, Qingfan1; Teng, Lesheng1 ; Xie, Jing1
- المصدر:
PLoS ONE. 10/31/2017, Vol. 12 Issue 11, p1-13. 13p.
- الموضوع:
- معلومة اضافية
- نبذة مختصرة :
A series of 1,2-dihydroquinoline derivatives were synthesized and evaluated for cytotoxicity in HeLa, Hep G2 and 6HEK-293T cell lines. EEDQ2 was identified as a promising anti-cancer agent with low IC50 in HeLa (18.55μg/ml) and Hep G2 (14.53μg/ml) cells. For improving the antitumor activity and tumor selectivity of EEDQ2, we prepared transferrin (Tf)-modified liposomes (LPs) to deliver EEDQ2. When HeLa and Hep G2 cells were treated with LP-delivered EEDQ2, the ROS level was significantly enhanced, and mitochondrial membrane potential was reversed. Tf-LPs improved cell uptake of EEDQ2 by about 3.7 times compared with non-targeted LPs. These data suggest that Tf-LPs delivering EEDQ2 is a promising strategy to treat cancer. [ABSTRACT FROM AUTHOR]
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