Transferrin-conjugated liposomes loaded with novel dihydroquinoline derivatives as potential anticancer agents

• DOI: 10.1371/journal.pone.0186821
• Publication Date: 2017-10-31T14:07:22Z
• Authors: Mengqiao Wang; Robert J. Lee; Ye Bi; Lianlian Li; Guodong Yan; Jiahui Lu; Qingfan Meng; Lesheng Teng; Jing Xie
• Keywords: HeLa

A series of 1,2-dihydroquinoline derivatives were synthesized and evaluated for cytotoxicity in HeLa, Hep G2 6HEK-293T cell lines. EEDQ2 was identified as a promising anti-cancer agent with low IC50 HeLa (18.55μg/ml) (14.53μg/ml) cells. For improving the antitumor activity tumor selectivity EEDQ2, we prepared transferrin (Tf)-modified liposomes (LPs) to deliver EEDQ2. When cells treated LP-delivered ROS level significantly enhanced, mitochondrial membrane potential reversed. Tf-LPs improved uptake by about 3.7 times compared non-targeted LPs. These data suggest that delivering is strategy treat cancer.