8‐hydroxyquinoline and quinazoline derivatives as potential new alternatives to combat Candida spp. biofilm

• Published in: Letters in applied microbiology Vol. 74; no. 3; pp. 395 - 404
• Main Authors: Reginatto, P., Joaquim, A.R., Rocha, D.A., Berlitz, S.J., Külkamp‐Guerreiro, I.C., De Andrade, S.F., Fuentefria, A.M.
• Format: Journal Article
• Language: English
• Published: England Oxford University Press 01-03-2022
• Subjects: 8‐hydroxyquinoline; Antifungal Agents - pharmacology; Antifungal Agents - therapeutic use; biofilm; Biofilms; Candida; catheter; Catheters; Colonization; film‐forming system; Hydroxyquinoline; Medical instruments; Microbial Sensitivity Tests; Oxyquinoline; Planktonic cells; Polystyrene; Polystyrene resins; Polyurethane; Polyurethane resins; quinazoline; Quinazolines; quinazoline; catheter; 8-hydroxyquinoline; biofilm; film-forming system
• ISSN: 0266-8254; 1472-765X
• DOI: 10.1111/lam.13607

Often associated to the colonization by Candida spp. biofilm, the catheter‐related infections are a serious health problem since the absence of a specific therapy. Hence, the main objective of this work was to evaluate the activity of 8‐hydroxyquinoline and quinazoline derivatives on Candida spp. biofilms. A quinazoline derivative (PH100) and an 8‐hydroxyquinoline derivative (PH157) were tested against nine strains of C. albicans, C. tropicalis and C. parapsilosis, and their biofilms in polystyrene microtitre plates and on polyurethane central venous catheter. The PH157 compound was incorporated into a film‐forming system‐type formulation and its capacity to inhibit biofilm formation on catheters was evaluated. The compounds were active against planktonic and sessile cells, as well as against the tested biofilms. PH157 compound performed better than the PH100 compound. The formulation containing PH157 presented results very similar to those of the compound in solution, which indicates that its activity was preserved. Both compounds showed activity against Candida spp. strains and their biofilm, with better PH157 activity. The formulation preserved the action of the PH157 compound, in addition, it facilitates its application on the catheter. The structural modifications that these compounds allow can generate compounds that are even more active, both against planktonic cells and biofilms.
Significance and Impact of the Study: Infections related to central venous catheters associated with Candida spp. colonization and biofilm formation have high rates of morbidity and mortality, mainly due to the absence of targeted and specific treatment. We believe that this work is a very important step in advancing research on the management and treatment of these infections, which are so serious. The tested compounds showed a promising character against the tested Candida spp. strains. Furthermore, the use of an innovative strategy to control the formation of Candida spp. biofilm on the surface of a polyurethane central venous catheter was tested and was successful.