A In${}^{III}$-MOF with imidazole decorated pores as 5-Fu delivery system to inhibit colon cancer cells proliferation and induce cell apoptosis in vitro and in vivo

A new nontoxic porous In${}^{III}$-based metal‐organic framework [In(Hpbic)(pbic)](DMF)${}_2$ (1) (DMF = N,N‐dimethylacetamide) was successfully prepared with 2‐(pyridin‐4‐yl)‐1H‐benzo[d]imidazole‐5‐carboxylic acid (H${}_2$pbic) as organic linker via a solvothermal process. Further, the nanostructure 1 could be obtained via a green grinding method. Nitrogen adsorption measurements revealed the presence of micropores as well as moderate high BET surface areas in the activated nanostructure 1 (1a). The drug loading experiment shows that 5‐fluorouracil (5‐Fu) is preferentially captured into the pore of the nanostructure 1a with a loading capacity of 32.6 %. Meanwhile, the controlled release of 5‐Fu in a simulated human body with liquid phosphate‐buffered saline solution was realized. In addition, the Cell Counting Kit‐8 (CCK‐8) assay was conducted to determine the inhibitory effect of 5‐Fu@1a on human colon cancer cell SW60 viability and proliferation, the results indicated the excellent anti‐cancer activity of 5‐Fu@1a in vitro. To reveal the related mechanism, the Annexin V‐FITC/PI assay and reactive oxygen species (ROS) level detection was carried out after 5‐Fu@1a treatment. Finally, the in vivo xenograft model was constructed in mice, the tumor volume, and mice body weight were recording at indicated time. The in vivo results suggested the significant inhibitory activity of 5‐Fu@1a in mice. (© 2019 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)