EVALUATION OF THE POTENCY OF A NEW SERIES OF PYRIDOXAL OXIME DERIVATIVES IN THE REACTIVATION OF TABUN, PARAOXON AND VX-PHOSPHYLATED (CROSBI ID 614664)
Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija
Podaci o odgovornosti
Bušić, Valentina ; Gašo-Sokač, Dajana ; Katalinić, Maja
engleski
EVALUATION OF THE POTENCY OF A NEW SERIES OF PYRIDOXAL OXIME DERIVATIVES IN THE REACTIVATION OF TABUN, PARAOXON AND VX-PHOSPHYLATED
Quaternary salts of pyridoxal oxime were synthesized by the quaternization of the pyridoxal oxime with substituted phenacyl bromides using microwave heating. Microwave-assisted rapid synthesis was done in solvent (acetone) and under solvent-free condition. In this study we investigated these new oxime interactions with human recombinant acetylcholinesterase (AChE, EC 3.1.1.7) and human butyrylcholinesterase (BChE, EC 3.1.1.8). We tested the oxime’s reversible inhibition of enzymes and oxime-assisted reactivation of phosphylated enzymes. All of the tested oximes reversibly inhibited AChE and BChE with inhibition constants (Ki) in micromolar to milimolar range but showing week enzyme selectivity. Furthermore, the oximes were tested in 1 mM concentration as reactivators of AChE and BChE inhibited by organophosphorus compounds tabun, paraoxon and VX. Unfortunately, the tested oximes were not efficient in reactivation of either tabun, paraoxon or VX inhibited enzymes, especially compared to the oximes currently used in medical treatment practice. However two of tested oximes showed a potency to reactivate BChE inhibited by VX, and therefore could be considered in the area of organophosphorus compounds bioscavenger development and pre-treatment drugs.
acetylcholinesterase; butyrylcholinesterase; pyridoxal oxime; reactivation of phosphylated enzymes; reversible inhibition
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
Podaci o prilogu
82-82.
2014.
objavljeno
Podaci o matičnoj publikaciji
The Interply of Biomolecules HDBMB2014, Congress of the Croatian Society of Biochemistry and Molecular Biology, 24-27 September, 2014, Zadar, Croatia
Katalinić, Maja ; Kovarik, Zrinka
Zadar: Hrvatsko Društvo za Biotehnologiju
978-953-95551-5-1
Podaci o skupu
Congress of the Croatian Society of Biochemistry and Molecular Biology
poster
24.09.2014-27.09.2014
Zadar, Hrvatska