Targeting pathogenic fungi, bacteria and fungal-bacterial biofilms by newly synthesized quaternary ammonium derivative of pyridoxine and terbinafine with dual action profile.

Many pathogenic bacteria and microscopic fungi form rigid polymicrobial biofilms this way enhancing their resistant to treatment. A series of novel pyridoxine-based quaternary ammonium derivatives of terbinafine characterized by both antifungal and antibacterial activities was designed. The leading compound named KFU-127 exhibits promising antifungal and antibacterial activities against various bacteria and micromycetes in both planktonic and biofilm-embedded forms demonstrating MIC values comparable with those of conventional antifungals and antimicrobials. Similar to other antiseptics like benzalkonium chloride and miramistin, KFU-127 is considerably toxic for eukaryotic cells that limits is application to topical treatment options. On the other hand, KFU-127 reduces the number of viable biofilm-embedded bacteria and C. albicans by 3 orders of magnitude at concentrations 2-4 times lower than those of reference drugs and successfully eradicates S. aureus-C. albicans mixed biofilms. The mechanism of antimicrobial action of KFU-127 is bimodal including both membrane integrity damage and pyridoxal-dependent enzymes targeting. We expect that this bilateral mechanism would result in lower rates of resistance development in both fungal and bacterial pathogens. Taken together, our data suggest KFU-127 as a new promising broad spectrum topical antimicrobial capable of one-shot targeting of bacterial and fungal-bacterial biofilms.

The study of oral fluid dynamic parameters on the background of pathological and physiological dental abrasion.

OBJECTIVE: Introduction: Violation of oral fluid mineralization processes, which is determined by the mineralization potential of saliva, is associated with changes in the physicochemical parameters of the oral fluid, particularly its viscosity. The aim of our study was to study mineralization potential and types of microstallation of oral fluid as one of the factors of influence on the cariesogenic situation in the oral cavity of patients with physiological or pathological tooth abrasion. PATIENTS AND METHODS: Materials and methods: During the examination of patients' oral cavity, a comprehensive assessment of tooth hard tissues was performed in order to of study activity and prevalence of the processes occurring in them. RESULTS: Results: Assessing the physico-chemical parameters of oral fluid in patients of the first experimental group, we obtained the following results: the viscosity of saliva in subgroups was 2,17 ± 0,87 for subgroup #1, 1,78 ± 0,57 for subgroup #2, and 2,15 ± 0,86 for #3 subgroups, which did not have a significant difference between the indices within the group. During the research, the number of independent structures of oral fluid in subgroups 1-3 was 1.67 ± 0.86, 1.67 ± 0.77 and 1.57 ± 0.85. CONCLUSION: Conclusions: Thus, we have established that the mineralizing function of saliva changes when the cariesogenic situation in the oral cavity arises,. This leads to destabilization of the crystalline structure of the oral fluid and indicates the relationship between its structural and mineralizing properties.