- 作者: Mohammad A. KAMAL;Abdullah S. ALHOMIDA;Ali A. AL-RAJHI;Abdulaziz A. AL-JAFARI
- 中文摘要: The present study determines the energy parameters, such as the Gibb's free energy change (.DELTA. G), enthalpy change (.DELTA. H), heat of activation (.DELTA. H*), entropy change (.DELTA. S), temperature coefficient (Q10) and activation energy (Ea), of human retinal acetylcholinesterase (AChE, EC 3.1.1.7) inhibition by tacrine. The stereo-frequency collisions factor (PZ, the number of sterically and energetically favorable collisions occurring between tacrine and AChE) was also studied in this investigation. Tacrine significantly increased the value of .DELTA. G, .DELTA. H, .DELTA. H*, Q10, Ea and PZ factor, and decreased the value of .DELTA. S for AChE. Since there is no known report on the inhibition of human retinal AChE by tacrine, these results were compared with the reported values for the energy parameters of camel retinal and chicken brain AChE inhibition by an anti-cancer drug, cyclophosphamide. The uniqueness of this approach lies in the development of the 'dual substrate and dual temperature' model, which may open up a new, more efficient avenue for the study of various enzyme catalyzed reactions.
- 英文摘要: --
- 中文關鍵字: acetylcholinesterase, Alzheimer's disease, energetic, inhibition, retina, tacrine, thermodynamics
- 英文關鍵字: --