Observations placeholder

Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis

Identifier

029113

Type of Spiritual Experience

Background

This appears to be baout other plants but is actually about PAs.

In the specific case of PA, the anti-microbial activity of usaramine, monocrotaline and azido-retronecine against some bacteria has been demonstrated. Usaramine was analyzed concerning its ability to inhibit biofilm formation in Staphylococcus epidermidis and Pseudomonas aeruginosa. Although the mechanism of action of usaramine remained unclear, it was possible to observe that it prevented the formation of biofilm by S. epidermis by about 50% at 1 mg/mL. However, no effect was detected in the formation of biofilm by P. aeruginosa. Furthermore, monocrotaline and azido-retronecine demonstrated anti-Trichomonas vaginalis activity (concentrations up to 1 mg/mL), being lethal to 70% and 85% of bacterial cells, respectively, while was devoid of toxicity towards T. vaginalis. Interestingly, no detectable damage in vaginal epithelial cells was found, a selectivity trait that may be relevant for the development of new drugs, such as topic anti-microbial agents.

A description of the experience

Biomed Pharmacother. 2016 Oct;83:323-329. doi: 10.1016/j.biopha.2016.06.033. Epub 2016 Jul 9.
Activity of pyrrolizidine alkaloids against biofilm formation and Trichomonas vaginalis.
da Silva Negreiros Neto T1, Gardner D2, Hallwass F3, Leite AJM4, de Almeida CG5, Silva LN6, de Araújo Roque A7, de Bitencourt FG8, Barbosa EG9, Tasca T10, Macedo AJ11, de Almeida MV12, Giordani RB13.
Author information
1Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Gustavo Cordeiro de Faria, SN, CEP 59010-180, Natal, RN, Brazil. Electronic address: theminegreiros@yahoo.com.br.
2USDA, ARS, Poisonous Plant Research Laboratory, 1150 East 1400 North, Logan, UT 84341, USA. Electronic address: dale.gardner@ars.usda.gov.
3Departamento de Química Fundamental, Universidade Federal de Pernambuco, Avenida Professor Moraes Rego, 1235, CEP 50670-901, Recife, PE, Brazil. Electronic address: hallwass@ufpe.br.
4Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Gustavo Cordeiro de Faria, SN, CEP 59010-180, Natal, RN, Brazil. Electronic address: ana@analeite.org.
5Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Campus Martelos, CEP 36036-330, Juiz de Fora, MG, Brazil. Electronic address: camilagdealmeida@gmail.com.
6Centro de Biotecnologia and Faculdade de Farmácia, UFRGS, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil. Electronic address: lauransilva@gmail.com.
7Herbário da UFRN, Universidade Federal do Rio Grande do Norte, Campus Universitário Lagoa Nova, CEP 59078-970, Natal, RN, Brazil. Electronic address: alan.ufrn@gmail.com.
8Laboratório de Pesquisa em Parasitologia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil. Electronic address: fe_gobbi@hotmail.com.
9Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Gustavo Cordeiro de Faria, SN, CEP 59010-180, Natal, RN, Brazil. Electronic address: euzebiobg@gmail.com.
10Laboratório de Pesquisa em Parasitologia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil. Electronic address: tiana.tasca@ufrgs.br.
11Centro de Biotecnologia and Faculdade de Farmácia, UFRGS, Av. Ipiranga, 2752, 90610-000, Porto Alegre, RS, Brazil. Electronic address: alexandre.macedo@ufrgs.br.
12Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Campus Martelos, CEP 36036-330, Juiz de Fora, MG, Brazil. Electronic address: mauro.almeida@ufjf.edu.br.
13Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Gustavo Cordeiro de Faria, SN, CEP 59010-180, Natal, RN, Brazil. Electronic address: raquebg@hotmail.com.


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 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.

Copyright © 2016 Elsevier Masson SAS. All rights reserved.
KEYWORDS:
Biological activity; Monocrotaline; Pyrrolizidine alkaloids; Usaramine
PMID:
27399809

The source of the experience

PubMed

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