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Previous issue date: 2011-07-22 / Conselho Nacional de Desenvolvimento Cient?fico e Tecnol?gico, CNPq. / The increase in life expectancy is a worldwide occurrence that shows the relative
success of public health politics, and Brazil is among the countries where people are
living longer and in better physical health. But the increase in life expectancy has a
negative effect: the appearance of degenerative diseases typical of old age, including
several forms of dementia, like Alzheimer?s Disease (AD) that is certainly the most
important. It is an irreversible and progressive disease characterized by neuronal
deterioration that results in loss of cognitive functions such as memory, communication
skills, judgment and reasoning. Donepezil, rivastigmine and galantamine are medicines
used for the treatment of AD and act reversibly inhibiting the acetylcholinesterase
(AChE). Evidences suggest that the enzyme butyrylcholinesterase (BChE), closely
related to AChE, plays a significant role in AD because it is involved in neural
functions such as cholinergic co-regulation and non-cholinergic neurotransmission. The
aim of this research is to provide new substances with anticholinesterase action by using
?-carboline derivatives from the natural product harmane and carry out a kinetic study
to determine the inhibition profile of the enzymes AChE e BChE, which could help in
the discovery of new compounds which could be useful in the treatment of AD. Firstly,
a screening was carried out with seven ?-carboline derivatives. In a second stage, a
kinetic investigation, employing Ellman?s method, was run with these compounds and
all of them presented high anticholinesterase action for both AChE and BChE. All
seven derivatives presented a non-competitive reversible inhibition. / Torres, Juliana Mariano. ESTUDO CIN?TICO DA ATIVIDADE
ANTICOLINESTER?SICA DE DERIVADOS -CARBOL?NICOS DO
PRODUTO NATURAL HARMANA. 2011. Disserta??o (mestrado em Qu?mica
Org?nica). Instituto de Ci?ncias Exatas, Departamento de Qu?mica, Universidade
Federal Rural do Rio de Janeiro, Serop?dica, RJ, 2011.
O aumento da expectativa de vida ? um fen?meno mundial que mostra o relativo
sucesso de pol?ticas de sa?de p?blica, e o Brasil se inclui entre os pa?ses em que as
pessoas est?o vivendo por mais tempo e em condi??es melhores de sa?de. No entanto, o
aumento da expectativa de vida tem como efeito negativo o aparecimento de doen?as
degenerativas, t?picas de idades mais avan?adas, incluindo-se as v?rias formas de
dem?ncia e entre estas, a mais importante ?, sem d?vida, a Doen?a de Alzheimer (DA),
patologia irrevers?vel e progressiva caracterizada pela deteriora??o neuronal que resulta
em perda de fun??es cognitivas, tais como mem?ria, capacidade de comunica??o,
julgamento e racioc?nio. Para o tratamento da DA s?o utilizados f?rmacos como o
donepezil, galantamina e rivastigmina, os quais agem inibindo revers?velmente a
acetilcolinesterase (AChE). Evid?ncias sugerem que a enzima butirilcolinesterase
(BChE), intimamente relacionada com a AChE, tem um papel significante na DA, uma
vez que est? envolvida em fun??es neurais tais como a corregula??o da
neurotransmiss?o colin?rgica e n?o-colin?rgica. Esta pesquisa pretendeu estudar novas
subst?ncias com a??o anticolinester?sica utilizando derivados -carbol?nicos do produto
natural harmana, bem como fazer um estudo cin?tico a fim de descobrir qual o perfil de
inibi??o das enzimas AChE e BChE, a fim de buscar novos compostos que poderiam ser
?teis no tratamento dos sintomas da DA. Desta forma, foi efetuada preliminarmente
uma triagem com 7 derivados -carbol?nicos e posteriormente foi realizada uma
investiga??o cin?tica com estes compostos, uma vez que, todos apresentaram alta a??o
anticolinester?sica tanto para AChE quanto para BChE. A cin?tica enzim?tica foi
estudada segundo o m?todo de Ellman. Contudo, observou-se que todos os 7 derivados
apresentaram uma inibi??o revers?vel n?o competitiva.
| Identifer | oai:union.ndltd.org:IBICT/oai:localhost:jspui/1144 |
| Date | 22 July 2011 |
| Creators | Torres, Juliana Mariano |
| Contributors | Rumjanek, Victor marcos, Kummerle, Arthur Eugen |
| Publisher | Universidade Federal Rural do Rio de Janeiro, Programa de P?s-Gradua??o em Qu?mica, UFRRJ, Brasil, Instituto de Ci?ncias Exatas |
| Source Sets | IBICT Brazilian ETDs |
| Language | Portuguese |
| Detected Language | English |
| Type | info:eu-repo/semantics/publishedVersion, info:eu-repo/semantics/masterThesis |
| Format | application/pdf |
| Source | reponame:Biblioteca Digital de Teses e Dissertações da UFRRJ, instname:Universidade Federal Rural do Rio de Janeiro, instacron:UFRRJ |
| Rights | info:eu-repo/semantics/openAccess |
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