Efflux pumps are proteins present in the plasma membrane of bacteria, which transport antibiotics and other compounds into the extracellular medium, conferring resistance. The discovery of natural efflux pump inhibitors is a promising alternative. α-Bisabolol is a sesquiterpene isolated from several plants such as Matricaria chamomilla L. and has important properties such as antibacterial and anti-inflammatory activity. Currently, the formation of inclusion complexes with β-Cyclodextrin has been used for improving the physicochemical characteristics of the host molecule. This study evaluated the effect of α-Bisabolol, in isolation and in complexation with β-Cyclodextrin, as TetK and NorA efflux pump inhibitors in Staphylococcus aureus strains. The minimum inhibitory concentration (MIC) was determined. Subsequently, inhibitory activity over the pumps was observed by an MIC reduction for the antibiotics, by using subinhibitory concentrations (MIC/8) in combination with tetracycline and norfloxacin. The MIC of the compounds was ≥1024 μg/mL. α-Bisabolol potentiated the action of tetracycline and reduced the MIC of norfloxacin to a clinically relevant concentration. The complexed substance showed synergism however, the effect of the isolated α-Bisabolol was superior to the complex. These results indicate α-Bisabolol is a potential substance to be used as an efflux pump inhibitor.
The Chapada of Araripe located in the Northeast of Brazil, presents a great vegetal diversity. Associated with this, the region presents a great cultural plurality, which reflects in several popular knowledge, such as the use of medicinal plants in the region. The objective of this work was to carry out an ethnopharmacological bibliographic survey of angiosperms present in the region. The scientific name of species was associated with the keywords "traditional use", "traditional medicine" "traditional knowledge" and "Brazil" to collect information published and available on Pubmed, Science Direct, Scielo and Scopus Platform. Subsequently, the species with the greatest versatility of use were selected and their relative importance (RI) indexes were calculated. As a result, 92 species with medicinal potential were identified in the Chapada of Araripe, corresponding to 81 genera and 44 botanical families, with Fabaceae, Asteraceae, Malvaceae and Rubiaceae being the taxa that presented the highest number of species with 16, 6, 5 and 5 respectively. The 10 most versatile species were Anacardium occidentale (RI: 1.38), Astronium urundeuva (1.86), Copaifera langsdorffii (2.00), Hancornia speciosa (1.81), Himatanthus drasticus (1.62), Hymenaea stigonocarpa (1.89), Lafoensia pacari (1.83), Libidibia ferrea (1.43), Scoparia dulcis (1.71) and Ximenia americana L. (1.46). Finally, we emphasize that Chapada of Araripe is a region of great biological and cultural value, being important actions for the preservation of local flora and traditional knowledge.
Antimicrobial resistance and the consequent inefficiency of antibiotics are the main problems faced by medicine. In view of this, numerous researches have been aimed at looking for new agents with antibacterial activity, among them natural products. Thus, this study aims to evaluate the antioxidant activity of aqueous and hydroalcoholic extracts of the leaves and roots of Spondias tuberosa by Thin Layer Chromatography (TLC), as well as to verify the antibacterial action of the extracts alone and in combination with commercial antibiotics to evaluate its potential in action of change of antibiotics. The extracts showed polar and nonpolar phenolic substances with antioxidant action. The Minimum Inhibitory Concentration (MIC) of the hydroalcoholic extracts of the leaves and roots was 1,024 μg/mL compared to the Staphylococcus aureus 25923 strain, whereas with the other strains, the products showed an MIC ≥ 2,048 µg/mL. The effect of combining extracts with amikacin, ampicillin and norfloxacin against the multidrug-resistant bacteria Escherichia coli 06, Staphylococcus aureus 10 and Pseudomonas aeruginosa 24 resulted in synergistic effects with aminoglycoside alone, achieving up to 75 % reduction in the MIC of the antibiotic. In view of the results obtained, it can be concluded that the extracts of S. tuberosa presented polar and nonpolar phenolic substances, in the antibacterial activity it can positively modify the effect of the aminoglycoside antibiotic against multi-resistant bacteria, but future studies are necessary to discover the mechanism of action of such an effect.
Infections by multiresistant microorganisms have led to a continuous investigation of substances acting as modifiers of this resistance. By following this approach, the chemical composition of the essential oil from Piper caldense leaf and its antimicrobial potential were investigated. The antimicrobial activity was determined by broth microdilution method providing values for minimum inhibitory concentration (MIC), IC50, and minimum fungicidal concentration (MFC). The essential oil was tested as a modulator for several antibiotics, and its effect on the morphology of Candida albicans (CA) strains was also investigated. The chemical characterization revealed an oil composed mainly of sesquiterpenes. Among them are caryophyllene oxide (13.9%), spathulenol (9.1%), δ-cadinene (7.6%) and bicyclogermacrene (6.7%) with the highest concentrations. The essential oil showed very low activity against the strains of CA with the lowest values for IC50 and MFC of 1790 μg/mL and 8192 μg/mL, respectively. The essential oil modulated the activity of fluconazole against CA URM 4387 strain, which was demonstrated by the lower IC50 obtained, 2.7 μg/mL, whereas fluconazole itself presented an IC50 of 7.76 μg/mL. No modulating effect was observed in the MFC bioassays. The effect on fungal morphology was observed for both CA INCQS 40006 and URM 4387 strains. The hyphae projection was completely inhibited at 4096 μg/mL and 2048 μg/mL, respectively. Thus, the oil has potential as an adjuvant in antimicrobial formulations.
One of the main global problems that affect human health is the development of bacterial resistance to different drugs. As a result, the growing number of multidrug-resistant pathogens has contributed to an increase in resistant infections and represents a public health problem. The present work seeks to investigate the chemical composition and antibacterial activity of the essential oil of Syzygium cumini leaves. To identify its chemical composition, gas chromatography coupled to mass spectrometry was used. The antibacterial activity test was performed with the standard strains Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 25853 and Staphylococcus aureus ATCC 25923 and multidrug-resistant clinical isolates E. coli 06, P. aeruginosa 24 and S. aureus 10. The minimum inhibitory concentration (MIC) was determined by serial microdilution as well as the verification of the modulating effect of the antibiotic effect. In this test, the oil was used in a subinhibitory concentration. The test reading was performed after 24 h of incubation at 37 °C. The results show that the major chemical constituent is α-pinene (53.21%). The oil showed moderate activity against E. coli ATCC 25922, with the MIC of 512 µg/mL; there was no activity against the other strains. The oil potentiated the effect of antibiotics demonstrating possible synergism when associated with gentamicin, erythromycin and norfloxacin against E. coli 06 and S. aureus 10.
Alelopatia é definida pela Sociedade Internacional de Alelopatia como a ciência que estuda qualquer processo envolvendo essencialmente os metabólitos secundários produzidos pelas plantas, algas, bactérias e fungos que influenciam o crescimento e desenvolvimento de sistemas agrícolas e biológicos, incluindo efeitos positivos e negativos. Entretanto, diversas dúvidas são evidenciadas em novos pesquisadores da área, como o surgimento e evolução dessa ciência. Dessa forma, reunimos de forma didática algumas informações importantes acerca da alelopatia, as quais estão distribuídas em (1) Alelopatia: Histórico e Definições, (2) Modo de Ação dos Aleloquímicos e (3) Natureza Química dos Aleloquímicos, a fim de nortear os novos pesquisadores e possibilitar a utilização destas informações em sala de aula como recurso teórico.
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