Effective inhibition of bacterial sialidases by phenolic acids and flavonoids

Abstract

As a pathogenicity factor in some microorganisms, sialidase is a key target for inactivation, as this would have curative and preventive effects on various diseases. Significant results are already achieved with viral sialidase inhibitors, while such studies on bacterial enzymes are scarce. Pure natural compounds representing phenols and flavonoids, were tested for their inhibitory effect on sialidases from Vibrio cholerae non-O1, Arthrobacter nicotianae and Oerskovia paurometabola. All three enzymes were isolated, purified beforehand and stored under suitable conditions. Quinic and gallic acids showed the highest inhibitory activity - 76 to 100% against the three sialidases. Fisetin had a significant inhibitory activity on two of the enzymes. The structurally related thymol and thymoquinone exerted from 80 to 100% inhibition on at least one of the enzymes. Catechin and rutin had significant inhibitory activity, varying from 49 to 100%, on some of the enzymes. Quercetin, known for its inhibitory effect on viral sialidases, had a lesser impact on the studied enzymes. The suppressive effect of quinic acid, rutin and fisetin on bacterial sialidases is observed for the first time.