Caries preventive efficacy of 2-,3-,4-aminophenylacetic acids hexafluorosilicates

Abstract

In recent years, ammonium hexafluorosilicates have been actively studied as new potential anti-caries agents, which may compete with traditional fluoride preparations in the future. The pharmacological potential of hexafluorosilicates with substituted phenylammonium cations remains unexplored. The purpose of the work is to study the caries-prophylactic effectiveness of 2-,3-,4-aminophenylacetic acids hexafluorosilicates in the experiment on a model of experimental caries.
 2-,3-,4-aminophenylacetic acids hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed method, reference drugs – NaF and (NH4)2SiF6. The studied drugs were applied to the teeth and gums of rats as part of a gel based on Na-salt of carboxymethylcellulose. The activity of alkaline and acid phosphatases was determined and the mineralization index was calculated in the pulp of incisors. The number and depth of carious lesions of the teeth were calculated and the caries prevention efficiency was calculated. The concentration of calcium ions was determined in the alveolar bone homogenate, the level of malondialdehyde, the activity of elastase, urease, and lysozyme was determined in the mucous membrane of the oral cavity homogenate.
 It was established that the caries-prophylactic efficiency of NaF, (NH4)2SiF6, I–III is 38.1%, 33.3%, 28.6%, 59.5%, 64.3%, that is, the anti-caries effect of compounds II and III exceeds the similar indicator of NaF by more than 1,6 and 1,7 times, respectively. The results of determining the phosphatases activity in the pulp of incisors showed that I–III almost completely normalize the mineralizing index. Compounds I–III provide an effective reduction of inflammatory markers, and the maximum effect is achieved when using gels with the participation of compounds II and III. The studied fluoropreparations reduce the activity of urease; the effect of all hexafluorosilicates is more effective compared to the reference drug – NaF. All hexafluorosilicates significantly return lysozyme activity to the control level compared to NaF, with compounds II and III being the most effective. Calculations using the PASS online method demonstrate an increased probability of anti-inflammatory (intestinal), anti-infectious, antiviral (influenza), antiseptic activity in the case of 3-,4-aminophenylacetic acids in the composition of salts II and III, which can lead to potentiation of their joint action and strengthening of anti-caries effect of these compounds. It is planned to continue research on the biological activity of 3-,4-aminophenylacetic acids hexafluorosilicates as potential means of caries treatment and prevention.