Kinetics of the inhibition of acetylcholinesterase from desert cobra (Walterinnesia aegyptia) venom by local anesthetics: procaine and tetracaine.
The kinetic parameters of W. aegyptia venom acetylcholinesterase (AChE) inhibition by procaine and tetracaine hydrochloride were investigated in the present study. Procaine and tetracaine reversibly inhibited the AChE activity in a concentration-dependent manner, the IC50 being about 0.28 and 0.04 mM, respectively. The Michaelis-Menten constant (K(m)) for the hydrolysis of acetylthiocholine iodide was found to be 0.051 mM with Vmax 10.2 mumole/min/mg protein. Both K(m) and Vmax were affected by procaine while only Vmax decreased with tetracaine. A Lineweaver-Burk plot and its secondary replot indicated that the nature of the inhibition is of the linear mixed type for procaine which is considered to be a mixture of competitive and noncompetitive types while the inhibition was noncompetitive for tetracaine. The values of Ki(slope) and K(intercept were estimated as 0.133 mM and 0.451 mM for procaine and 7.2 x 10(-3) mM for tetracaine, respectively, by the secondary replots of the Lineweaver-Burk plot.
al-Jafari
A A
AA
Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.
Kamal
M A
MA
Duhaiman
A S
AS
Alhomida
A S
AS
D000110:Acetylcholinesterase / Q000187:drug effects* / Q000378:metabolism*; D000777:Anesthetics / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects / Q000502:physiology; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics*; D004546:Elapid Venoms / Q000201:enzymology*; D017815:Elapidae; D004789:Enzyme Activation; D011343:Procaine / Q000494:pharmacology; D013748:Tetracaine / Q000494:pharmacology
D000777:Anesthetics; D002800:Cholinesterase Inhibitors; D004546:Elapid Venoms; D013748:Tetracaine; D011343:Procaine; D000110:Acetylcholinesterase