Kinetička analiza heterocikličkih α-D-manopiranozida kao potencijalnih inhibitora butirilkolinesteraze

master's thesis

• Title (english): Kinetic analysis of heterocyclic α-D-mannopiranosides as potential inhibitors of butyrylcholinesterase
• Author: Matej Poletar
• Mentor: Srđanka Tomić-Pisarović (mentor)
• Committee member: Srđanka Tomić-Pisarović (predsjednik povjerenstva)
• Committee member: Marko Močibob (član povjerenstva)
• Committee member: Snežana Miljanić (član povjerenstva)
• Committee member: Vesna Petrović Peroković (član povjerenstva)
• Granter: University of Zagreb; Faculty of Science; (Department of Chemistry); Zagreb
• Defense date and country: 2017-09-28, Croatia
• Scientific / art field, discipline and subdiscipline: NATURAL SCIENCES; Chemistry

Abstract

U okviru ovog diplomskog rada ispitana su inhibitorna svojstva 11 novih heterocikličkih α-D-manopiranozida.
Aktivnost liofilizirane butirilkolinesteraze izolirane iz konjskog seruma
(EqBChE, akt. 0,08 U/mL) određena je spektrofotometrijskom metodom po Ellmanu. Mjerenja
aktivnosti su vršena uz acetiltiokolin-jodid kao supstrat (u konc. rasponu 0,04 – 1 mM), tiolni
reagens DTNB (0,3 mM) i spojeve 1 – 11 (10 – 300 μM). Povećanje apsorbancije TNB aniona
praćeno je u kvarcnim kivetama (ukupni volumen reakcijske smjese 2 mL) u
0,1 M fosfatnom puferu (pH 7,4) pri 25 oC i valnoj duljini 412 nm kroz 90 sekundi na
spektrofotometru AnalytikJena Specord 200. Od jedanaest ispitanih spojeva, šest je pokazalo
inhibitornu aktivnost prema EqBChE, od kojih su dva relativno dobri inhibitori s konstantama
inhibicije 12,40±1,226 μM (za spoj 7) i 37,28±3,982 μM (za spoj 4).

Abstract (english)

The aim of this thesis is to investigate inhibitory properties of 11 newly synthesized heterocyclic
α-D-mannopiranosides towards BChE. Ellman's spectrophotometric method was used to
determine activities of lyophilized butyrylcholinesterase from equine serum (EqBChE, act. 0,08
U/mL). Measurments were conducted with acetylthiocholine iodide as a supstrate (conc. range
0,04 – 1 mM), thiol reagent DTNB (0,3 mM) and compounds 1 -11 (10 – 300 μM). Increase in
TNB anion absorbance was monitored in quartz cuvettes (total volume 2 mL) in 0,1 M
phosphate buffer medium (pH 7,4) at 25 oC and wavelength 412 nm during 90 seconds on
AnalytikJena Specord 200 spectrophotometer. Six out of eleven tested compounds have shown
inhibitory effect on BChE and two of them are relatively good BChE inhibitors with constants
of inhibition 12,40±1,226 μM (compound 7) i 37,28±3,982 μM (compound 4).

• Keywords: butirilkolinesteraza; inhibitori; α-D-manopiranozidi; Ellmanova metoda
• Keywords (english): Butyrylcholinesterase; inhibitors; α-D-mannopiranosides; Ellman's procedure
• Language: croatian
• URN:NBN: urn:nbn:hr:217:235664
• Study programme: Title: Graduate university studies in chemistry; specializations in: Research programme; Course: Research programme; Study programme type: university; Study level: graduate; Academic / professional title: magistar/magistra kemije (magistar/magistra kemije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access; Embargo expiration date: 2019-09-28
• Created on: 2017-10-25 10:06:43