Next Article in Journal
Anti-Cancer Effects of Green Tea Polyphenols Against Prostate Cancer
Next Article in Special Issue
MicroRNAs as a Novel Tool in the Diagnosis of Liver Lipid Dysregulation and Fatty Liver Disease
Previous Article in Journal
Synthesis and Antifungal Potential of Some Novel Benzimidazole-1,3,4-Oxadiazole Compounds
Previous Article in Special Issue
Impact of Gelatin Supplemented with Gum Arabic, Tween 20, and β-Cyclodextrin on the Microencapsulation of Turkish Oregano Extract
Article

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

1
College of Life Sciences, Jilin University, Changchun 130012, China
2
College of Chemistry, Jilin University, Changchun 130012, China
3
School of Pharmaceutical and Food Sciences, Zhuhai College of Jilin University, Zhuhai 519041, China
4
Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(1), 192; https://doi.org/10.3390/molecules24010192
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)
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
Show Figures

Graphical abstract

MDPI and ACS Style

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. https://doi.org/10.3390/molecules24010192

AMA Style

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. https://doi.org/10.3390/molecules24010192

Chicago/Turabian Style

Cai, Guangsheng, Simiao Wang, Lang Zhao, Yating Sun, Dongsheng Yang, Robert J. Lee, Menghui Zhao, Huan Zhang, and Yulin Zhou. 2019. "Thiophene Derivatives as Anticancer Agents and Their Delivery to Tumor Cells Using Albumin Nanoparticles" Molecules 24, no. 1: 192. https://doi.org/10.3390/molecules24010192

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop