Background: Inhibition activity of 8 synthetic molecules known as anti-allergy
drugs on lipases has been investigated. The enzymatic inhibition produced by these molecules
is described here for the first time.
Objective: The used anti-allergy drugs are: Loratidine, primalan, zyrtec, histagan, periactin,
ketotifene, rifex and bilastine.
Methods: Lipase inhibition is studied using the spectrophotometric method. Molecular
docking has been achieved for the first time for these drugs using AutoDock Vina program
to discuss the nature of interactions, structure-activity relationship and the mechanism of inhibition.
Results: The biological evaluation of these molecules showed that most of these drugs are
potent lipase inhibitors with competitive type inhibition. The best drug is loratidine with
IC50=0.44mg/ml and Ki=0.86 mM and competitive type inhibition. Molecular docking
studies of the studied molecules confirmed their competitive inhibitory type with their binding
to the Catalytic Active Site (CAS) of lipases.
Conclusion: Hence, these drugs could be used for obesity or candidiasis treatment taking
advantage of the much-known details of their secondary effects as antiallergy drugs.