Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside

Detalhes bibliográficos
Autor(a) principal: Martins, Nuno Miguel Martins
Data de Publicação: 2012
Tipo de documento: Dissertação
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10451/9168
Resumo: Tese de mestrado em Química (Química, Saúde e Nutrição), apresentada à Universidade de Lisboa, através da Faculdade de Ciências, 2012
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spelling Fluorescent and radionuclide labeling of a synthetic neuroactive glycosideAntimitoticCarbohydrate synthesisFluorescenseSCIRadiosynthesisTeses de mestrado - 2012Tese de mestrado em Química (Química, Saúde e Nutrição), apresentada à Universidade de Lisboa, através da Faculdade de Ciências, 2012Clinically brain and spinal cord injuries are very serious. These injuries can result in permanent, transient sensory or motor defects resulting in serious individual consequences besides social and economic ones. Currently, it is estimated that 90 million people around the world suffer from spinal cord injury (SCI). One of the main obstacles to central nervous system (CNC) trauma repair is the formation in the lesion area of a growth inhibitory cellular-molecular structure, called “glial scar”. This inhibitory environment in the injured spinal cord blocks axon growth and precludes nerve repair. We have previously reported that the new glucoside 3 is a potent inhibitor of glioma and melanoma cells growth. It inhibited human melanoma (A-375 cells) division with an ID50 below the micromolar range (0.6 +- 0.3 µM). Thereafter, 3 was found as potential useful in the treatment of SCIs. Considering the potencial application of glucoside 3 for SCI repair, there is a great interest to understand its biological behavior. Aiming to such goal, were designed new 3 derivatives containing molecular probes (fluorophore/radionuclide) suitable for conventional molecular imaging techniques. This work describes the synthesis, characterization and in vitro biological evaluation of a fluorescent label (NBD) 3 derivative. Primary cultures of astrocytes, from postnatal rats (day 0 -1), were treated with NBD-3 derivative at final concentrations of 3, 15 and 30 µM. Fluorescence microscopy images, obtained after 24 h of treatment, demonstrated the ability of NBD-3 derivative to permeate through the astrocyte cell membrane. Also, the number of astrocytes decreased as the concentration of the synthetic inhibitor increase, showing similar antimitotic activity as the original glucoside 3. The establishment of a synthetic approach to prepare fluorinated-23 derivative is also reported. This approach will be adopted for the synthesis/radiosynthesis of a fluorine label (19F/18F) 3 derivative. We also plan to perform biodistribution studies with the 18 F-3 derivative. We also plan to perform biodistribution studies with the 18F-3 derivative, in order to assess its in vivo tissue distribution/brain uptake.Santos, Isabel Rego dos, 1948-Alvarez, Alfonso Fernández-MayolarasRepositório da Universidade de LisboaMartins, Nuno Miguel Martins2013-09-16T14:51:58Z20122012-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://hdl.handle.net/10451/9168enginfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-08T15:53:23Zoai:repositorio.ul.pt:10451/9168Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:33:26.938419Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
title Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
spellingShingle Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
Martins, Nuno Miguel Martins
Antimitotic
Carbohydrate synthesis
Fluorescense
SCI
Radiosynthesis
Teses de mestrado - 2012
title_short Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
title_full Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
title_fullStr Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
title_full_unstemmed Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
title_sort Fluorescent and radionuclide labeling of a synthetic neuroactive glycoside
author Martins, Nuno Miguel Martins
author_facet Martins, Nuno Miguel Martins
author_role author
dc.contributor.none.fl_str_mv Santos, Isabel Rego dos, 1948-
Alvarez, Alfonso Fernández-Mayolaras
Repositório da Universidade de Lisboa
dc.contributor.author.fl_str_mv Martins, Nuno Miguel Martins
dc.subject.por.fl_str_mv Antimitotic
Carbohydrate synthesis
Fluorescense
SCI
Radiosynthesis
Teses de mestrado - 2012
topic Antimitotic
Carbohydrate synthesis
Fluorescense
SCI
Radiosynthesis
Teses de mestrado - 2012
description Tese de mestrado em Química (Química, Saúde e Nutrição), apresentada à Universidade de Lisboa, através da Faculdade de Ciências, 2012
publishDate 2012
dc.date.none.fl_str_mv 2012
2012-01-01T00:00:00Z
2013-09-16T14:51:58Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
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url http://hdl.handle.net/10451/9168
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language eng
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instacron:RCAAP
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