Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis |
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| Institution: | 1. Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Gustavo Cordeiro de Faria, SN, CEP 59010-180, Natal, RN, Brazil;2. USDA, ARS, Poisonous Plant Research Laboratory, 1150 East 1400 North, Logan, UT 84341, USA;3. Departamento de Química Fundamental, Universidade Federal de Pernambuco, Avenida Professor Moraes Rego, 1235, CEP 50670-901, Recife, PE, Brazil;4. Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Campus Martelos, CEP 36036-330, Juiz de Fora, MG, Brazil;5. Centro de Biotecnologia and Faculdade de Farmácia, UFRGS, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil;6. Herbário da UFRN, Universidade Federal do Rio Grande do Norte, Campus Universitário Lagoa Nova, CEP 59078-970, Natal, RN, Brazil;7. Laboratório de Pesquisa em Parasitologia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil;1. Departamento de Engenharia Química, Universidade Federal do Rio Grande do Sul, Rua Eng. LuisEnglert s/n, 90040-040 Porto Alegre, RS, Brazil;2. Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves n° 9500, 91501-970 Porto Alegre, Brazil;1. Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, 91501-970 Porto Alegre, Brazil;2. Laboratório de Materiais Cerâmicos, Departamento de Materiais, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil;3. Instituto de Física, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil;4. Departamento de Ingeniería Química y Biotecnología, Facultad de Ciencias Físicas y Matemáticas, Universidad de Chile, Santiago, Chile;1. Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves 9500, 91501-970 Porto Alegre, Brazil;2. Laboratório de Materiais Cerâmicos, Departamento de Materiais, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil;3. Instituto de Física, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil;4. Departamento de Ingeniería Química y Biotecnología, Facultad de Ciencias Físicas y Matemáticas, Universidad de Chile, Santiago, Chile;1. Institute of Chemistry, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil;2. Institute of Physics, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil;3. School of Chemistry, University of Nottingham, University Park, Nottingham, NG7 2RD, United Kingdom;1. School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, Sichuan, PR China;2. School of Chemistry and Chemical Engineering, China West Normal University, Nanchong, 637002, Sichuan, PR China;3. Center for Molecular and Translational Medicine, Institute of Biomedical Sciences, Georgia State University, 511 Research Science Center, 157 Decatur St SE, Atlanta, GA, 30303, USA |
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| 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. |
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| Keywords: | Usaramine Monocrotaline Pyrrolizidine alkaloids Biological activity |
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