A Novel Polyhedral Oligomeric Silsesquioxane-Cefotaxime Conjugate: Synthesis, Characterization, In Vitro Antibacterial Activity And Cellular Cytotoxicity

Abstract

In recent years, polyhedral oligomeric silsesquioxanes (POSS) have become the subject of great interest. The main aim of this study is the development of a chloro-functionalized polyhedral oligomeric silsesquioxane (POSS-Cl) based novel polyhedral oligomeric silsesquioxane-cefotaxime (POSS-CTX) conjugate that exhibits potent antibacterial activity and biocompatibility. The chloro-functionalized POSS, cefotaxime (CTX) and polyhedral oligomeric silsesquioxane-cefotaxime (POSS-CTX) structures were characterized for their chemical structure, morphology and thermal behavior by employing fourier transform infrared spectroscopy (FTIR), 1H nuclear magnetic resonance spectroscopy (NMR), scanning electron microscope/energy dispersive X-ray spectroscopy (SEM/EDX), and the thermal analysis differential thermal analyzer (DTA), thermo gravimetric analyzer (TGA), differential scanning calorimetric analyzer (DSC) techniques. In addition, the antibacterial activities were tested with broth microdilution methods on E.coli and S.aureus bacteries. The cellular cytotoxicity was performed on the L929 mouse skin fibroblast cell with MTT test. The IC50 values of cefotaxime for E.coli and S.aureus were 62.71±14.30 and 144.17±20.90 μg/mL, respectively. However, in the POSS-cefotaxime (POSS-CTX) conjugate, the IC50 values for E.coli and S.aureus were 11.51±3.02 and 26.20±11.14 μg/mL. These results suggest that the POSS-CTX conjugate was more antibacterial active than the cefotaxime. These POSS based antibacterial POSS-CTX conjugate can provide benefits many areas such as medical materials, antibacterial coating, antibacterial packaging.

Keywords: Polyhedral oligomeric silsesquioxane, Cefotaxime, Antibacterial Activities, Cellular Cytotoxicity.