Choline and geranic acid (CAGE) ionic liquids inhibit both elastase activity and growth of oral bacteria

Abstract

Choline and geranic acid (CAGE) ionic liquids have recently been shown to have applications in the delivery of macromolecules and poorly soluble drugs across epithelial barriers and in bacterial growth inhibition. Ionic liquids are known to denature proteins by the disruption of forces that guide natural protein folding, and the inflammatory enzyme elastase was recently shown to be inhibited by a variety of ionic liquids other than CAGE. Inhibition of collagenolytic enzymes, including elastase, has been shown to improve outcomes in cases of periodontitis via amelioration of periodontal inflammation and alveolar bone resorption. In this study, we investigated whether CAGE prepared with varying stoichiometries was able to inhibit elastase at varying concentrations and whether these CAGE formulations could inhibit the growth of key pathogenic bacterial species associated with oral health conditions. We found that CAGE was capable of inhibiting both porcine elastase and human neutrophil elastase at concentrations as low as 5 mM, and that CAGE formulations were effective at inhibiting the growth of all tested pathogenic oral bacteria. The inhibition of elastase by CAGE may be a mechanism by which CAGE can improve outcomes in periodontitis independent from CAGE's known antibacterial properties.

Ionic liquids revolutionizing biomedicine: recent advances and emerging opportunities

“…165 Choline geranic acid ILs (CAGE) could inhibit human neutrophil elastase at low concentrations by disrupting the hydrophobic effect. 169 Besides, the addition of ILs can change the pH of the environment and denature proteins. [EMIM][BF 4 ] could cause conformational changes of BSA, resulting in the formation of amyloid fibers.…”