Naslov
Isothiocyanates: Cholinesterase Inhibiting, Antioxidant, and Anti-Inflammatory Activity

Autori
Burčul, Franko ; Generalić Mekinić, Ivana ; Radan, Mila ; Rollin, Patrick ; Blažević, Ivica

Izvornik
Journal of enzyme inhibition and medicinal chemistry (1475-6366) 33 (2018), 1; 577-582

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
isothiocyanates, antioxidation, cholinesterase inhibition, anti-inflammatory activity

Sažetak
Finding a new type of cholinesterase inhibitor that would overcome the brain availability and pharmacokinetic parameters or hepatotoxic liability has been a focus of investigations dealing with the treatment of Alzheimer’s disease. Isothiocyanates have not been previously investigated as potential cholinesterase inhibitors. These compounds can be naturally produced from their glucosinolate precursors, secondary metabolites widely distributed in our daily <i>Brassica</i> vegetables. Among eleven tested compounds, phenyl isothiocyanate and its derivatives showed the most promising inhibitory activity. 2-Methoxyphenyl ITC showed best inhibition on acetylcholinesterase with IC₅₀ of 0.57 mM, while 3-methoxyphenyl ITC showed the best inhibition on butyrylcholinesterase having 49.2% at 1.14 mM. Assessment of the antioxidant efficacy using different methods led to a similar conclusion. The anti-inflammatory activity was also tested using human COX-2 enzyme, ranking phenyl isothiocyanate and 3-methoxyphenyl isothiocyanate as most active, with ~99% inhibition at 50 μM.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA