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Doctoral Thesis
DOI
10.11606/T.75.2016.tde-23032016-093705
Document
Author
Full name
Lizbeth Lorena Lopez Parra
E-mail
Institute/School/College
Knowledge Area
Date of Defense
Published
São Carlos, 2016
Supervisor
Committee
Berlinck, Roberto Gomes de Souza (President)
Burtoloso, Antonio Carlos Bender
Pilli, Ronaldo Aloise
Gamboa, Ian Castro
Moraes, Luiz Alberto Beraldo de
Title in Portuguese
Uso de desreplicação por HPLC-UV-MS para a descoberta de metabólitos bioativos de invertebrados marinhos
Keywords in Portuguese
Amathia verticillata
Desreplicação
Iotrochota birotulata
Produtos naturais marinhos
Tedania brasiliensis
Trypanosoma cruzi Leishmania (L.) infantum
Zoobotryon verticillatum

Abstract in Portuguese
O presente projeto de pesquisa teve por objetivo a descoberta de metabólitos secundários potencialmente bioativos contra atividade parasitária e como agentes anti-virais e antibióticos, usando desreplicação como metodologia essencial na seleção e priorização de extratos brutos oriundos de invertebrados, para a descoberta de produtos naturais estruturalmente inéditos.

Foram preparados diversos extratos de invertebrados marinhos a partir de um fracionamento inicial. O desenvolvimento e a aplicação de uma metodologia de desreplicação permitiu a seleção de três organismos de estudo, Iotrochota birotulata, Amathia verticillata, e Tedania brasiliensis. Os extratos destes organismos foram submetidos a diferentes metodologias de fracionamento, isolamento e purificação de substâncias, dependendo dos resultados de desreplicação para cada organismo.

Como resultado do isolamento e identificação de substancias destes organismos, obteve-se dois compostos já conhecidos na literatura e dezesseis compostos inéditos, dos quais dois são derivados sintéticos. De todos os compostos isolados, a pseudoceratidina, as desbromopseudoceratidinas e as tedamidas A e B apresentaram um índice de seletividade de 243.1, 217.1 e 89.3 respectivamente para Leishmania (L.) infantum, e o composto N12-acetilpseudoceratidina de 23.2 para Trypanosoma cruzi, sendo estes resultados muito promissores para a utilização das estruturas destas moléculas como potenciais modelos para o desenvolvimento de fármacos.
Title in English
Use of dereplication by HPLC -UV -MS for the discovery of bioactive metabolites from marine invertebrates
Keywords in English
Amathia verticillata
Dereplication
Iotrochota birotulata
Marine Natural Products
Tedania brasiliensis
Trypanosoma cruzi Leishmania (L.) infantum
Zoobotryon verticillatum

Abstract in English
This research project aimed at the discovery of potentially bioactive secondary metabolites against parasitic activity and as antiviral agents and antibiotics, using dereplication as an essential methodology in the selection and prioritization of crude extracts derived from invertebrates, to the discovery of natural products structurally unpublished.

Various extracts of marine invertebrates from an initial fractionation were prepared. The development and application of a dereplication methodology allowed the selection of three study organisms, Iotrochota birotulata, Amathia verticillata, and Tedania brasiliensis. The extracts of these organisms were subjected to different methods of fractionation, isolation and purification of substances, depending on the results of dereplication for each organism.

As a result of the isolation and identification of substances of these organisms, it obtained two compounds already known in the literature and unpublished sixteen compounds, two of which are synthetic derivatives. In all isolated compounds, pseudoceratidina, the desbromopseudoceratidinas and tedamidas A and B showed an index of selectivity 243.1, 217.1 and 89.3 respectively for Leishmania (L.) infantum, and the compound N12-acetilpseudoceratidina 23.2 for Trypanosoma cruzi, which are very promising results for the use of these molecules as structures potential models for drug development.
 
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Publishing Date
2016-03-24
 
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