Investigation of Cholinesterase Inhibitor Effects of Some Chalcone Substituted Metallophthalocyanines

Year 2022, , 703 - 711, 15.12.2022

Aşkın Tekin , Tayfun Arslan

https://doi.org/10.31466/kfbd.1109715

Cited By: 1

Abstract

In this work, previously synthesized tetra-chalcone-substituted metallophthalocyanines (MPcs) containing Ni(II), Zn(II), Co(II), and Cu(II) in the inner core were investigated anticholinergic activities against Alzheimer's disease (AD). The MPcs were evaluated for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the original Ellman's colorimetric procedure. Against these two cholinesterase enzymes, all compounds showed inhibitory effects with IC50 values ranging from 1.243-2.369 μM against AChE and 2.865-3.372 μM against BChE. Among the four MPcs, CuPcs (2) showed the strongest inhibitory activity against AChE. ZnPcs (3) also showed the most effective inhibition for BChE.

Keywords

Cholinesterases, Chalcone, Phthalocyanine, Inhıbıtor

Bazı Kalkon Sübstitüe Metaloftalosiyaninlerin Kolinesteraz İnhibitör Etkilerinin İncelenmesi

Abstract

Bu çalışmada, merkezde Ni(II), Zn(II), Co(II) ve Cu(II) içeren daha önce sentezlenmiş tetra-kalkon sübstitüe metaloftalosiyaninlerin (MPcs) Alzheimer (AD) hastalığına karşı antikolinerjik aktiviteleri incelenmiştir. MPcs'ler, orijinal Ellman'ın kolorimetrik prosedürü kullanılarak asetilkolinesteraz (AChE) ve butirilkolinesteraz (BChE) inhibisyonları açısından değerlendirildi. Bu iki kolinesteraz enzimine karşı tüm bileşikler, AChE'ye karşı 1.243-2.369 μM ve BChE'ye karşı 2.865-3.372 μM arasında değişen IC50 değerleri ile inhibitör etkiler göstermiştir. Dört MPcs arasında CuPc (2), AChE'ye karşı en güçlü inhibitör aktiviteyi göstermiştir. Ayrıca, ZnPcs (3), BChE için en etkili inhibisyonu göstermiştir.

Keywords

Kolinesterazlar, Kalkon, Ftalosiyanin, İnhibitör

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