Kinetics for Camel (Camelus dromedarius) Retina Acetylcholinesterase Inhibrtron by Methotrexate In Vitro

The Japanese Journal of Pharmacology

Abdullah S. Alhomida¹  Fareeda Al-Khwyier¹  Abdulaziz A. Al-Jafari¹  Mohammad A. Kamal¹ 

[1]Department of Biochemistry, College of Science, King Saud University

关键词: Acetylcholinesterase;    Kinetics;    Inhibition;    Methotrexate;    Retina;   

DOI  :  10.1254/jjp.72.49

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(48)Cited-By(6)This work addresses the kinetic analysis of the interaction of methotrexate (MTX) with camel retina acetylcholinesterase (AChE, EC 3. 1. 1. 7). It was found that the MTX effect was reversible in nature. The IC50 was determined, by two methods, to be 1.362 mM. The Michaelis-Menten constant (Ks) for the hydrolysis of acetylthiocholine iodide (ASCh) by AChE was 0.123 mM in the control system, and the MTX-treated systems showed a 10-35% decrease in this value. The Vmax was 0.789 μmol/min/mg protein for the control system, while it was decreased by 23-76% in the MTX-treated systems. The Lineweaver-Burk plot, Dixon plot and their secondary replots indicated that the inhibition was a linear mixed type; i.e., uncompetitive and noncompetitive. The values of Ki and KI were estimated as 0.782 and 0.404 mM, respectively. The use of camel retina as a model for the study of human retina may open new avenues for studying various aspects of AChE.

【 授权许可】

Unknown