Transferrin-conjugated liposomes loaded with novel dihydroquinoline derivatives as potential anticancer agents.
Mengqiao WangRobert J LeeYe BiLianlian LiGuodong YanJiahui LuQingfan MengLesheng TengJing XiePublished in: PloS one (2017)
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.
Keyphrases
- cell cycle arrest
- cell death
- inflammatory response
- induced apoptosis
- drug delivery
- anti inflammatory
- pi k akt
- oxidative stress
- stem cells
- single cell
- photodynamic therapy
- endoplasmic reticulum stress
- electronic health record
- drug release
- human health
- climate change
- squamous cell
- newly diagnosed
- young adults
- data analysis
- oxide nanoparticles
- structure activity relationship