The inhibitory effect of tetramethylethylene diamine on water soluble and membrane bound acetylcholinesterase activity.
1. The inhibitory effect of N,N,N',N'-tetramethylethylene diamine (TEMED) on water soluble (WSAChE) and membrane bound (MBAChE) acetylcholinesterase was investigated. 2. TEMED (0.5-4.0 mM) reversibly inhibited WSAChE activity (18-62%) and MBAChE (20-61%) in a concentration dependent manner. 3. The IC50 being about 2.8 mM for WSAChE and 2.6 mM for MBAChE. 4. Lineweaver-Burk plots indicated that the nature of inhibition is noncompetitive for both water soluble and membrane bound acetylcholinesterase, with Km values 68 microM and 123 microM respectively. 5. An Arrhenius plot showed that the transition temperature (TT) is unaffected in the presence of TEMED. 6. The activation energy was increased below and above TT in the case of WSAChE only. 7. On the basis of this behaviour of TEMED with AChE, it can be proposed that it can be used as an eluting agent for the bounded AChE to affinity ligand and may have beneficial action on the reactivatability of irreversibly-inhibited AChE due to its structure. 8. Moreover there is a possibility that it can be used as a therapeutic agent for the treatment of Alzheimer's disease, myasthenia gravia and glaucoma like some other inhibitors of AChE.
al-Jafari
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Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000201:enzymology*; D002462:Cell Membrane / Q000201:enzymology*; D002645:Chickens; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004789:Enzyme Activation; D005029:Ethylenediamines / Q000494:pharmacology*; D005260:Female; D008297:Male; D012995:Solubility; D013816:Thermodynamics; D014867:Water
D002800:Cholinesterase Inhibitors; D005029:Ethylenediamines; D014867:Water; C005798:N,N,N',N'-tetramethylethylenediamine; D000110:Acetylcholinesterase