Artigo Produção Nacional Revisado por pares

Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis

2016; Elsevier BV; Volume: 83; Linguagem: Inglês

10.1016/j.biopha.2016.06.033

ISSN

1950-6007

Autores

Themístocles da Silva Negreiros Neto, Dale R. Gardner, Fernando Hallwass, Ana Jéssica Matias Leite, Camila Guimarães de Almeida, Laura Nunes Silva, Alan de Araújo Roque, Fernanda Gobbi de Bitencourt, Euzébio Guimarães Barbosa, Tiana Tasca, Alexandre José Macêdo, Mauro V. de Almeida, Raquel Brandt Giordani,

Tópico(s)

Pediatric health and respiratory diseases

Resumo

Crotalaria genus belongs to the subfamily Papilionoideae comprising about 600 species spread throughout tropical, neotropical and subtropical regions. In this study, seeds of Crolatalaria pallida were used to the isolation of usaramine, a pyrrolizidine alkaloid. Thus, Pseudomonas aeruginosa and Staphylococcus epidermidis were utilized as strains to test some activities of this alkaloid, such as antibiofilm and antibacterial. Meanwhile, monocrotaline obtained from Crotalaria retusa seeds, was used as the starting material for synthesis of necine base derivatives with anti-Trichomonas vaginalis potential. Alkaloids were characterized by 1D and 2D NMR techniques and GC-MS analysis. Usaramine demonstrated a highlighted antibiofilm activity against S. epidermidis by reducing more than 50% of biofilm formation without killing the bacteria, thus it could be assumed as a prototype for the development of new antibiofilm molecules for pharmaceutical and industrial purposes. Monocrotaline activity against T. vaginalis was evaluated and results indicated inhibition of 80% on parasite growth at 1mg/mL, in addition, neither cytotoxicity against vaginal epithelial cells nor hemolytic activity were observed. On the other hand, retronecine showed no anti-T. vaginalis activity while azido-retronecine was more active than monocrotaline killing 85% of the parasites at 1mg/mL. In conclusion, pyrrolizidine alkaloids are suggested as promising prototypes for new drugs especially for topical use.

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