Studium kinetiky a mechanismu inhibice cholinesteráz novými inhibitory

Mgr. Katarína Vorčáková

Master's thesis

Study of kinetics and mechanism of cholinesterases inhibition by new inhibitors

Abstract:

Bola študovaná kinetika neinhibovaných a inhibovaných hydrolýz acetylcholinu a acetylthiocholinu pomocou dvoch typov enzýmov, acetylcholinesterasy a butyrylcholinesterasy. Na ich sledovanie boli použité dve nezávislé metódy, Ellmanová metóda a pH-statová metóda. Celkovo 12 nových inhibítorov (karbamáty) bolo použitých na sledovanie inhibovaných hydrolýz. Ďalej boli stanovené rozdeľovacie koeficienty log Pow študovaných inhibítorov v sústave n-oktanol:voda a bola sledovaná anticholinesterasova aktivita daných inhibítorov, vyjadrená pomocou indexu IC50.

Abstract:

Kinetics of non-inhibited and inhibited hydrolyses of acetylcholine and acetylthicholine by two types of enzyme, acetylcholinesterase and butyrylcholinesterase, were studied. There were used two methods for determination of enzymatic hydrolysis, Ellman´s and pH-stat method. There were used 12 inhibitors (carbamates) for the study of inhibited hydrolysis. Then, the partition coefficients log Pow of studied inhibitors in system n-octanol:water were determined and anticholinesterase activity of chosen inhibitors was tested. This property was characterized by the value of index IC50.

Keywords

cholinesterasy, karbamáty, Alzheimerová choroba, inhibície cholinesteras

Language used: Czech

Date on which the thesis was submitted / produced: 27. 4. 2011

Thesis defence

• Date of defence: 1. 6. 2011
• Supervisor: Mgr. Šárka Štěpánková, Ph.D.

University of Pardubice

Faculty of Chemical Technology

Master programme / field:
Special Chemical and Biological Programmes / Analysis of Biological Materials