Jabbour, A., Institute of Dental Sciences, Faculty of Dentistry, Hebrew University-Hadassah, POB 12272, Jerusalem, 91120, Israel, Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Hebrew University, Jerusalem, 91120, Israel
Shemesh, M., Institute of Dental Sciences, Faculty of Dentistry, Hebrew University-Hadassah, POB 12272, Jerusalem, 91120, Israel
Srebnik, M., Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Hebrew University, Jerusalem, 91120, Israel
Zaks, B., Institute of Dental Sciences, Faculty of Dentistry, Hebrew University-Hadassah, POB 12272, Jerusalem, 91120, Israel
Steinberg, D., Institute of Dental Sciences, Faculty of Dentistry, Hebrew University-Hadassah, POB 12272, Jerusalem, 91120, Israel

Dental diseases are among the most prevalent afflictions of humankind. These diseases are associated with the formation of biofilms harboring pathogenic bacteria. Fructosyltransferases (FTF) are extra cellular enzymes of several oral bacteria. FTF are associated with the formation of extracellular polysaccharide matrix (fructans) which play a role in biofilm formation and oral bacteria physiology. Oxazaborolidines have been shown to inhibit biofilm formation. The purpose of this study was to examine if the anti-biofilm effect is, in part, an effect on the immobilized enzymes synthesizing the extra cellular polysaccharide participating in biofilm formation. Eight different oxazaborolidines (BNO1-BNO8) were synthesized and evaluated for their affect on the synthesis of fructans by FTF using the biomolecular interaction analysis (BIAcore) system which involves the use of real-time surface plasmon resonance (SPR) technique. The tested oxazaborolidines demonstrated a significant and immediate inhibitory effect on immobilized FTF activity. This effect was reversible. Our results show that oxazaborolidines can act as enzymatic inhibitors of FTF immobilized on the surface, also at levels lower than their MIC. Part of the anti-biofilm effect of BNOs may be accounted for this enzymatic inhibition. © 2006.