1. Transferrin-conjugated liposomes loaded with novel dihydroquinoline derivatives as potential anticancer agents.
- Author
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Wang, Mengqiao, Lee, Robert J., Bi, Ye, Li, Lianlian, Yan, Guodong, Lu, Jiahui, Meng, Qingfan, Teng, Lesheng, and Xie, Jing
- Subjects
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TRANSFERRIN , *LIPOSOMES , *QUINOLINE derivatives , *ANTINEOPLASTIC agents , *MEMBRANE potential , *MITOCHONDRIAL physiology - Abstract
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]
- Published
- 2017
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