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

PloS One
Mengqiao WangJing Xie

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.

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Citations

Jan 10, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Guangsheng CaiYulin Zhou
Oct 3, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xi WangLesheng Teng
Mar 18, 2021·Journal of Liposome Research·Hanieh AbbasiSomayeh Handali

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Methods Mentioned

BETA
dynamic light scattering
confocal microscopy

Software Mentioned

Image J

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