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.
Highlights
Cancer is a complicated genetic disease that progresses via cell signaling, uncontrolled proliferation, metastasis, and apoptosis[1, 2]
We synthesized a serious of EEDQ derivatives
The cytotoxicity of the novel EEDQ derivatives was tested in HeLa, Hep G2 and 6HEK-293T cell lines using MTT assay
Summary
Cancer is a complicated genetic disease that progresses via cell signaling, uncontrolled proliferation, metastasis, and apoptosis[1, 2]. Traditional anti-cancer agents suffer from undesired side effects, narrow therapeutic window and drug resistance. There is a significant demand for effective and selective anti-cancer agents. EEDQ derivatives with anti-cancer activity are typically metal complexes[5, 9]. These agents have shown promising antitumor effect. Liposomes are a frequently-used delivery system to improve stability, solubility, therapeutic value and reducing side effects of agents[11]. When LPs were used to enhance solubility of EEDQ derivatives, the cell penetration capacity of drugs was adversely affected. The receptor for transferrin (TfR) is ubiquitous expressed in all cells. Expression levels of TfR in most normal cell is 100-fold lower
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