Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles

摘要

A series of thiophene derivatives (TPs) were synthesized and evaluated for cytotoxicity in HepG2 and SMMC-7721 cell lines by MTT assay. TP >5 was identified as a potential anticancer agent based on its ability to inhibit tumor cell growth. Drawbacks of TPs, including poor solubility and high toxicity, were overcome through delivery using self-assembling HSA nanoparticles (NPs). The optimum conditions for TP >5-NPs synthesis obtained by adjusting the temperature and concentration of TP >5. The NPs had an encapsulation efficiency of 99.59% and drug-loading capacity of 3.70%. TP >5 was slowly released from TP >5-NPs in vitro over 120 h. HepG2 and SMMC-7721 cell lines were employed to study cytotoxicity of TP >5-NPs, which exhibited high potency. ROS levels were elevated and mitochondrial membrane potentials reversed when the two cell lines were treated with TP >5-NPs for 12 h. Cellular uptake of fluorescence-labeled TP >5-NPs in vitro was analyzed by flow cytometry and laser confocal scanning microscopy. Fluorescence intensity increased over time, suggesting that TP >5-NPs were efficiently taken up by tumor cells. In conclusion, TP >5-NPs showed great promise as an anticancer therapeutic agent.