Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis

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• 作者：Themí ; stocles da Silva Negreiros Neto^a ; ^{theminegreiros@yahoo.com.br" class="auth_mail" title="E-mail the corresponding author} ; Dale Gardner^b ; ^{dale.gardner@ars.usda.gov" class="auth_mail" title="E-mail the corresponding author} ; Fernando Hallwass^c ; ^{hallwass@ufpe.br" class="auth_mail" title="E-mail the corresponding author} ; Ana Jé ; ssica Matias Leite^a ; ^{ana@analeite.org" class="auth_mail" title="E-mail the corresponding author} ; Camila Guimarã ; es de Almeida^d ; ^{camilagdealmeida@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Laura Nunes Silva^e ; ^{lauransilva@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Alan de Araú ; jo Roque^f ; ^{alan.ufrn@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Fernanda Gobbi de Bitencourt^g ; ^{fe_gobbi@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; Euzé ; bio Guimarã ; es Barbosa^a ; ^{euzebiobg@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Tiana Tasca^g ; ^{tiana.tasca@ufrgs.br" class="auth_mail" title="E-mail the corresponding author} ; Alexandre José ; Macedo^e ; ^{alexandre.macedo@ufrgs.br" class="auth_mail" title="E-mail the corresponding author} ; Mauro Vieira de Almeida^d ; ^{mauro.almeida@ufjf.edu.br" class="auth_mail" title="E-mail the corresponding author} ; Raquel Brandt Giordani^a ; ^{raquebg@hotmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Usaramine ; Monocrotaline ; Pyrrolizidine alkaloids ; Biological activity
• 刊名：Biomedicine & Pharmacotherapy
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：83
• 期：Complete
• 页码：323-329
• 全文大小：730 K

文摘

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.