TY  - JOUR
TI  - Investigation of anti-cholinesterase and anti-amyloidogenic activities of β-lactam antibiotics
AB  - Objectives: Neuroinflammation is an important factor in the pathogenesis of neurodegenerative disesases. The following study aimed to clarify the effects of β-lactam antibiotics to the cholinergic system, on acetylcholines- terase (AChE), butyrylcholinesterase (BuChE) activities, considering the structural differences of antibiotics, to evaluate the underlying mechanism of effects provided by protein-antibiotic interactions, and to clarify possible ef- fects of the antibiotics on the aggregation of Aβ-peptides. Methods: The inhibition/activation mechanisms for each antibiotic were examined kinetically by Ellman method. Destabilization effects of them on amyloid peptide fibrillation were examined and protein-ligand interactions were evaluated with most potent antibiotics by molecular docking studies. Results: Themostpowerfulinhibitionsweredetectedbythe inhibition studies of AChE with ceftazidime (CAZ) and BuChE with amoxicillin (AMX). CAZ was exhibited dose-related dual effect on AChE activity. CAZ was actually the dose-related modifier of AChE. At higher concentrations, CAZ was a nonessential activator of AChE. Molecular docking studies have been confirmed by kinetic studies. Interested β-lactam antibiotics did not prevent fibrillation rate as rifampicin. Conclusions: Inhibition/activation behaviours of studied β-lactam antibiotics on both cholinesterases may suggest that cholinergic transmission is one of the crucially important components of the β-lactam antibiotics-induced central nervous system adverse reactions.
AU  - Mirza, Hasan Cenk
AU  - Türkoğlu, Suna
AU  - Unsal Tan, Oya
AU  - özturan özer, eda
DO  - 10.1515/tjb-2021-0277
PY  - 2022
JO  - Türk Biyokimya Dergisi
VL  - 47
IS  - 3
SN  - 1303-829X
SP  - 119
EP  - 129
DB  - TRDizin
UR  - http://search/yayin/detay/1169210
ER  -