Antimalarial activity of piperidine alkaloids from Senna spectabilis and semisynthetic derivatives
In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids ( - )-cassine and ( - )-spectaline were isolated from the flowers of Senna spectabilis (syn. Cassia spectabilis). Their structures were elucidated using a combination of spe...
| Autores: | , , , , , , , |
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| Tipo de documento: | artigo |
| Estado: | Versão publicada |
| Data de publicação: | 2014 |
| País: | Brasil |
| Recursos: | Universidade Estadual Paulista (UNESP) |
| Repositório: | Repositório Institucional da UNESP |
| Idioma: | inglês |
| OAI Identifier: | oai:repositorio.unesp.br:11449/114545 |
| Acesso em linha: | http://dx.doi.org/10.5935/0103-5053.20140195 http://hdl.handle.net/11449/114545 |
| Access Level: | Acceso aberto |
| Palavra-chave: | piperidine alkaloids Senna spectabilis semisynthetic derivatives antimalarial activity Plasmodium falciparum |
| Resumo: | In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids ( - )-cassine and ( - )-spectaline were isolated from the flowers of Senna spectabilis (syn. Cassia spectabilis). Their structures were elucidated using a combination of spectroscopic and spectrometric data analysis. Further, these compounds were acetylated yielding the derivatives ( - )-3-O-acetylcassine and ( - )-3-O-acetylspectaline. All compounds were screened against P. falciparum-infected red blood cells (RBC) in culture, aiming to identify antimalarial prototypes. Among all compounds screened, the first two alkaloids (IC50 1.82 µM and IC50 2.76 µM) were more effective than the derivatives (IC50 24.47 µM and IC50 25.14 µM) in comparison to the standard compound chloroquine (IC50 0.30 µM). These data show that piperidine alkaloids constitute a class of natural products that feature a broad spectrum of biological activities, and are, therefore, important templates for drug design, including antimalarial. |
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