Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles
AbstractA 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. View Full-Text
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Cai, G.; Wang, S.; Zhao, L.; Sun, Y.; Yang, D.; Lee, R.J.; Zhao, M.; Zhang, H.; Zhou, Y. Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles. Molecules 2019, 24, 192.
Cai G, Wang S, Zhao L, Sun Y, Yang D, Lee RJ, Zhao M, Zhang H, Zhou Y. Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles. Molecules. 2019; 24(1):192.Chicago/Turabian Style
Cai, Guangsheng; Wang, Simiao; Zhao, Lang; Sun, Yating; Yang, Dongsheng; Lee, Robert J.; Zhao, Menghui; Zhang, Huan; Zhou, Yulin. 2019. "Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles." Molecules 24, no. 1: 192.
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