Ghazaleh Hatamian

University of Tehran, Iran

Systematic study of chalcone derivatives against glucosyltransferase C (GtfC) and biofilm production of Streptococcus mutans

Biography

Ghazaleh Hatamian got his bachelor in biology from Ferdowsi university of Mashhad-Iran in 2019. He started my master’s in cell and molecular biology from 2019 to 2020 and changed his field to Industrial microbiology and still working on research in the field of designing Antimicrobial drugs and biopharmaceutical analysis. He also completed an internship of design and producing vaccine and hope to continue his research on pharmaceutical field as a Ph.D. Student.

Abstract

The study of squaramidic receptors thermodynamic behavior allow for a better knowledge of their conduct in solution (7). This result promoted the idea to use them as useful receptors to functionalize Tooth decay is a bacterial infectious disease and one of the most common chronic human infections, characterized by the loss of minerals in the enamel. Treatment of this disease with traditional antibiotics is generally ineffective because the caries-causing bacteria form resistant biofilms that are resistant to these treatments.

Streptococcus mutans initiates the caries process and is known to be the main cause. The main ability of S. mutans to cause dental caries, in addition to the ability to attach to tooth surfaces and create biofilms, is to produce a micro-acidic environment in the mouth and grow in it.

S. mutans metabolizes dietary sucrose into insoluble and water-soluble glucans and Previous studies have shown that glucans produced by GtfB and GtfC are essential for the formation of S. mutans biofilms.

Chalcones are essentially isolated from natural sources, are widely found in vegetables, fruits, teas, and other plants, and act as precursors to the biosynthesis of flavonoids and isoflavones in plants. Structurally, they can be described as open-chain flavonoids in which two aromatic rings are joined by an unsaturated carbonyl system of three carbon ? and ?. Also, Chalcones are considered as a group of compounds with significant therapeutic potential.

Given the structural similarity between chalcones and effective inhibitors found to inhibit GtfC enzyme, as well as the promising antimicrobial effects reported from these compounds, chalcones appear to be effective ligands for GtfC inhibition. . Therefore, in this study, we aimed to investigate two groups of synthetic chalcones, while studying their anti-plaque properties against S. mutans, to achieve a suitable Structure-Activity Relationship (SAR) of these compounds.

The ability of the leads to inhibit the glucosyltransferase was evaluated using molecular docking method. This study has led to the discovery of several new biofilm inhibitors with enhanced potency and selectivity. One of the leads, NMe2, showed marked anti-bacterial potential and can be good candidate for in vitro and in vivo studies with the aim of introducing novel inhibitors of dental caries development.