Author
SILVA NEGREIROS NETO, THEMISTOCLES - Universidade Federal Do Rio Grande Do Norte (UFRN) | |
Gardner, Dale | |
HALLWASS, FERNANDO - Federal University Of Pernambuco | |
JESSICA MATIAS LEITE, ANA - Universidade Federal Do Rio Grande Do Norte (UFRN) | |
GUIMARAES DE AMEIDA, CAMILA - Federal University - Brazil | |
NUNES SILVA, LAURA - Federal University Of Rio Grande Do Sul | |
ARAUJO ROQUE, ALAN - Universidade Federal Do Rio Grande Do Norte (UFRN) | |
GOBBI DE BIETNCOURT, FERNANDA - Federal University Of Rio Grande Do Sul | |
GUIMARAES BARBOSA, EUZEBIO - Universidade Federal Do Rio Grande Do Norte (UFRN) | |
TASCA, TIANA - Federal University Of Rio Grande Do Sul | |
JOSE MACEDO, ALEXANDRE - Federal University Of Rio Grande Do Sul | |
VEIRA DE ALMEIDA, MAURO - Federal University - Brazil | |
BRANDT GIORDANI, RAQUEL - Universidade Federal Do Rio Grande Do Norte (UFRN) |
Submitted to: Biomedicine and Pharmacotherapy
Publication Type: Peer Reviewed Journal Publication Acceptance Date: 6/20/2016 Publication Date: 6/30/2016 Publication URL: https://handle.nal.usda.gov/10113/62970 Citation: Silva Negreiros Neto, T.D., Gardner, D.R., Hallwass, F., Jessica Matias Leite, A., Guimaraes De Ameida, C., Nunes Silva, L., Araujo Roque, A.D., Gobbi De Bietncourt, F., Guimaraes Barbosa, E., Tasca, T., Jose Macedo, A., Veira De Almeida, M., Brandt Giordani, R. 2016. Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis. Biomedicine and Pharmacotherapy. 83:323-329. Interpretive Summary: This study addresses two important problems: (1) the potential activity of the pyrrolizidine alkaloid, usaramine, against two pathogens that are involved in biofilm formation. Bacterial adhesion plays a pivotal role in the surface colonization by microorganisms through structured surface-associated communities of bacteria called biofilms. Biofilm growth is believed to be a contributing factor in the delay or even prevention of the healing process. (2) The potential anti-Trichomonas activity of the pyrrolizidine alkaloid monocrotaline and the related necine base derivatives. Trichomoniasis, caused by Trichomonas vaginalis, is recognized as the most prevalent non-viral sexually transmitted disease. The selected alkaloids were tested for anti-biofilm activity and anti-Trichomonas activity. Usaramine was found to reduce more than 50% of the biofilm formation without killing the bacteria. Monocrotaline and the azido-retronecine derivative were active in killing 80 to 85 % of the T. vaginalis parasites. As such, the pyrrolizidine alkaloids are suggested as promising prototypes for topical use drugs. Technical Abstract: 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 1 mg/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 1 mg/mL. In conclusion, pyrrolizidine alkaloids are suggested as promising prototypes for new drugs especially for topical use. |