Novel Targeted Anti-Tumor Nanoparticles Developed from Folic Acid-Modified 2-Deoxyglucose

• Main Authors: Shaoming Jin, Zhongyao Du, Huiyuan Guo, Hao Zhang, Fazheng Ren, Pengjie Wang
• Format: Article
• Language: English
• Published: MDPI AG 2019-02-01
• Series: International Journal of Molecular Sciences
• Subjects: folic acid; 2-Deoxyglucose; nano-particles; targeted anti-tumor; self-assemble
• Online Access: https://www.mdpi.com/1422-0067/20/3/697

The glucose analog, 2-deoxyglucose (2-DG), specifically inhibits glycolysis of cancer cells and interferes with the growth of cancer cells. However, the excellent water solubility of 2-DG makes it difficult to be concentrated in tumor cells. In this study, a targeted nano-pharmacosome was developed with folic acid-modified 2-DG (FA-2-DG) by using amino ethanol as a cleavable linker. FA-2-DG was able to self-assemble, forming nano-particles with diameters of 10⁻30 nm. The biological effects were evaluated with cell viability assays and flow cytometry analysis. Compared with a physical mixture of folic acid and 2-DG, FA-2-DG clearly reduced cell viability and resulted in cell cycle arrest. A computational study involving docking simulation suggested that FA-2-DG can dock into the same receptor as folic acid, thus confirming that the structural modification did not affect the targeting performance. The results indicated that the nano-pharmacosome consisting of FA-2-DG can be used for targeting in a nano-drug delivery system.