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Molecules 2019, 24(1), 192;

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

College of Life Sciences, Jilin University, Changchun 130012, China
College of Chemistry, Jilin University, Changchun 130012, China
School of Pharmaceutical and Food Sciences, Zhuhai College of Jilin University, Zhuhai 519041, China
Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Authors to whom correspondence should be addressed.
Received: 27 November 2018 / Revised: 27 December 2018 / Accepted: 29 December 2018 / Published: 6 January 2019
(This article belongs to the Special Issue Application of Novel Method in Pharmaceutical Study)
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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. View Full-Text
Keywords: thiophene derivatives; human serum albumin; drug delivery; nanoparticles; cytotoxicity thiophene derivatives; human serum albumin; drug delivery; nanoparticles; cytotoxicity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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.

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