We examined the effects of two different drugs (cladribine and mitoxantrone), which are frequently used in chemotherapeutic treatment, on human serum paraoxanase1 (PON1) enzyme activity vitro. Chemotherapeutic decreased vitro PON1 activity. Cladribine mitoxantrone inhibition mechanism were not competitive inhibitors. IC50 values for cladribine calculated as 0.077 mM 0.099 mM, respectively, Ki c...

o-Carbonyl arylboronic acids such as 2-formylphenylboronic acid (2-FPBA) are employed in biocompatible conjugation reactions with the resulting iminoboronate adduct stabilized by an intramolecular N–B interaction. However, few studies have utilized these reagents active site-directed enzyme inhibitors. We show that 2-FPBA is a potent reversible, slow-onset inhibitor of mandelate racemase (MR), ...

Cyclodextrins (CDs) are cyclic oligosaccharides composed of α-d-glucose units linked by α-(1,4)-glucosidic bonds. α-CD, β-CD and γ-CD contain 6, 7 or 8 d-glucose units, respectively. CDs can bind to the active site pancreatic α-amylase competitively inhibit enzyme. Adding 0.100 mg CD/mg native wheat starch substantially reduces in vitro activity is a more potent inhibitor than α-CD γ-CD. 0.025,...

Chagas disease is caused by the protozoan parasite Trypanosoma cruzi and affects 7 million people worldwide. Considering side effects drug resistance shown current treatments, development of new anti-Chagas therapies an urgent need. T. hypoxanthine phosphoribosyltransferase (TcHPRT), key enzyme purine salvage pathway, essential for survival trypanosomatids. Previously, we assessed inhibitory ef...

polyphenol oxidase (ppo), also known as tyrosinase (ec 1.14.18.1), is a copper-containing enzyme widely distributed in microorganisms, animals, and plants. this enzyme is responsible not only for browning in plants but also for melanization in animals. thus, tyrosinase inhibitors have a huge impact on industry and the economy. in the current study, we first purified the enzyme, then evaluated i...