Effects of active drug substances on enzyme activities

Enzymes are biological catalysts with a protein structure that catalyze reactions in the living metabolism. In recent years, changes in enzyme activity, particularly the reduction or complete inhibition of activity, known to as enzyme inhibition have held a significant role in research targeting the treatment of many diseases. Substances known as inhibitors perform inhibition through different mechanisms. Clarifying the inhibition characteristics exhibited by enzymes inhibited by these inhibitors provides guidance for the treatment of various diseases today. In this study, the inhibitory effects of 21 different drug active substances belonging to antibiotic, antidiabetic, antiviral, and non-steroidal anti-inflammatory (NSAI) groups on α-glucosidase, acetylcholinesterase (AChE), elastase, xanthine oxidase (XO), and lipase enzymes were individually examined, and corresponding graphs were drawn. From these graphs, IC50 values for each drug active substance were calculated, and the substance with the best inhibitory effect was identified. Additionally, the inhibition types and Ki values of the substances with the best inhibitory effect on the enzymes covered in our study were calculated. The results showed that glibornuride (IC50 = 0.35 ± 0.15 mM) for α-glucosidase, neomycin sulfate (0.65 ± 0.10 mM) for acetylcholinesterase (AChE), teicoplanin (0.44 ± 1.62 mM) for elastase, acyclovir (0.33 ± 0.04 µM) for xanthine oxidase (XO), and deksketoprofen trometamol (0.09 ± 0.005 mM) for lipase were the drug active substances with the best inhibitory effects. Among these, it was found that glibornuride for α-glucosidase, teicoplanin for elastase, and acyclovir for XO showed stronger inhibitory effects compared to the standard substances acarbose, ursolic acid, and allopurinol, respectively.