p-Nitroanilinin antikolinerjik etkilerinin belirlenmesi

Yıl 2023, Cilt: 3 Sayı: 1, 9 - 15, 15.06.2023

Adem Ertürk

Öz

Kolinesterazlar, doğal olarak oluşan bir nörotransmitter olan, nörotransmitter asetilkolinin (ACh) kolin ve asetik aside parçalanmasını katalize ederek sinir sisteminin düzgün çalışmasına izin verir. İnsan vücudundaki kolinesterazlar iki tiptir: asetilkolinesteraz (AChE; E.C.3.1.1.7) ve butirilkolinesteraz (BChE; E.C.3.1.1.8). Bu çalışmada, p-Nitroanilinin antikolinerjik etkisi deneysel ve teorik olarak araştırılmış ve bir AChE inhibitörü olarak bilinen takrin ile karşılaştırılmıştır. p-Nitroanilin için IC50 değerleri hesaplandı; AChE'ye karşı 17,77 nM, BChE'ye karşı 18,73 nM. Ayrıca Ki değerleri AChE'ye karşı 1,80 ± 0,16 nM, BChE'ye karşı 6,49 ± 1,63 nM olarak bulundu. Docking Score değerleri AChE için -4,631, BChE için -3,779 olarak hesaplandı.

Anahtar Kelimeler

Alzheimer hastalığı, Enzim inhibisyonu, Asetilkolinesteraz, Butirilkolinesteraz

Determination of anticholinergic effects of p-nitroaniline

Öz

Abstract

Cholinesterases allow the nervous system to function properly by catalyzing the breakdown of the neurotransmitter acetylcholine (ACh), a naturally occurring neurotransmitter, into choline and acetic acid. Cholinesterases in the human body are of two types: acetylcholinesterase (AChE; E.C.3.1.1.7) and butyrylcholinesterase (BChE; E.C.3.1.1.8). In this study, the anticholinergic effect of p-Nitroaniline was investigated experimentally and theoretically and compared with tacrine, which is known as an AChE inhibitor. IC50 values were calculated for p-Nitroaniline; 17.77 nM against AChE, 18.73 nM towards BChE. Also, Ki values was found to be 1.80 ± 0.16 nM against AChE and 6.49 ± 1.63 nM on BChE. Docking Score values were calculated as -4.631 for AChE and -3.779 for BChE.

Anahtar Kelimeler

Alzheimer’s disease, Enzyme inhibition, Acetylcholinesterase

Kaynakça

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