Journal ArticleDOI
In silico and in vitro evaluation of efflux pumps inhibition of α,β-amyrin
Raissa C Oliveira,Paulo Nogueira Bandeira,Telma L. G. Lemos,Hélcio Silva dos Santos,Jackelyne Roberta Scherf,Janaína Esmeraldo Rocha,Raimundo Luiz Silva Pereira,Thiago Sampaio de Freitas,Priscila R. Freitas,Francisco N. Pereira-Junior,Márcia Machado Marinho,Emanuelle Machado Marinho,Emmanuel Silva Marinho,Carlos Emídio Sampaio Nogueira,Henrique Douglas Melo Coutinho,Alexandre Magno Rodrigues Teixeira +15 more
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TLDR
Sarma et al. as mentioned in this paper evaluated the antibacterial activity of α, β-amyrin mixture isolated from Protium heptaphyllum against the multidrug-resistant strains of Escherichia coli 06 and Staphylococcus aureus 10.Abstract:
The use of the bacterial efflux pump mechanism to reduce the concentrations of antibiotics in the intracellular to the extracellular region is one of the main mechanisms by which bacteria acquire resistance to antibiotics. The present study aims to evaluate the antibacterial activity of the α,β-amyrin mixture isolated from Protium heptaphyllum against the multidrug-resistant strains of Escherichia coli 06 and Staphylococcus aureus 10, and to verify the inhibition of the efflux resistance mechanisms against the strains of S. aureus 1199B and K2068, carrying the NorA and MepA efflux pumps, respectively. The α,β-amyrin did not show clinically relevant direct bacterial activity. However, the α,β-amyrin when associated with the gentamicin antibiotic presented synergistic effect against the multidrug-resistant bacterial strain of S. aureus 10. In strains with efflux pumps, α,β-amyrin was able to inhibit the action of the efflux protein NorA against Ethidium Bromide. However, this inhibitory effect was not observed in the MepA efflux pump. In addition, when evaluating the effect of standard efflux pump inhibitors, clorptomazine and CCCP, α,β-amyrin showed a decrease in MIC, demonstrating the presence of the efflux mechanism through synergism. Docking studies indicate that α, β-amyrin have a higher affinity energy to MepA, and NorA than ciprofloxacin and norfloxacin. Also, α, β-amyrin bind to the same region of the binding site as these antibiotics. It was concluded that the α, β-amyrin has the potential to increase antibacterial activity with the association of antibiotics, together with the ability to be a strong candidate for an efflux pump inhibitor.Communicated by Ramaswamy H. Sarma.read more
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Ethnobotanical Uses, Phytochemistry, Toxicology, and Pharmacological Properties of Euphorbia neriifolia Linn. against Infectious Diseases: A Comprehensive Review
Arifa Sultana,Md. Jamal Hossain,Md. Ruhul Kuddus,Mohammad A. Rashid,Miss Sharmin Zahan,Saikat Mitra,Arpita Roy,Safaet Alam,Md. Moklesur Rahman Sarker,Isa Naina Mohamed +9 more
TL;DR: In this article , the authors summarize the classification, morphology, and ethnobotanical uses of E. neriifolia L. and its derived phytochemicals with the recent updates on the pharmacological properties against emerging infectious diseases, mainly focusing on bacterial, viral, fungal, and parasitic infections.
Journal ArticleDOI
Terpenes as bacterial efflux pump inhibitors: A systematic review
Kaio Jefté Santos De Oliveira Dias,Gustavo Marinho Miranda,Jonatas Reis Bessa,Ana Carolina Justino de Araújo,Priscilla Ramos Freitas,Ray S. Almeida,Cicera Laura R. Paulo,José Bezerra de Araújo Neto,Henrique Douglas Melo Coutinho,Jaime Ribeiro-Filho +9 more
TL;DR: The results of the present review suggest that terpenes are significant efflux pump inhibitors and, as such, can be used in drug development targeting the combat of antibacterial resistance.
Journal ArticleDOI
Tackling multidrug-resistant Staphylococcus aureus by natural products and their analogues acting as NorA efflux pump inhibitors.
TL;DR: In this paper , the authors discuss natural products and their derived compounds as NorA efflux pump inhibitors (EPIs), which are considered promising alternative therapeutic options with the potential to revive the effects of antibiotics and reduce bacterial virulence.
Journal ArticleDOI
Antibacterial and antibiotic modifying activity of chalcone (2E)-1-(4'-aminophenyl)-3-(4-methoxyphenyl)-prop-2-en-1-one in strains of Staphylococcus aureus carrying NorA and MepA efflux pumps: In vitro and in silico approaches.
Jacilene Barbosa da Silva,Janaína Esmeraldo Rocha,Jayze da Cunha Xavier,Thiago Sampaio de Freitas,Henrique Douglas Melo Coutinho,Paulo Nogueira Bandeira,Mateus Rodrigues de Oliveira,Matheus Nunes da Rocha,Emanuelle Machado Marinho,Norberto de Kassio Vieira Monteiro,L. R. Ribeiro,Ramon Róseo Paula Pessoa Bezerra de Menezes,Márcia Machado Marinho,Alexandre Magno Rodrigues Teixeira,Hélcio Silva dos Santos,Emmanuel Silva Marinho +15 more
TL;DR: In this paper , the antibacterial and antibiotic modifying activity of chalcone (2E)-1-(4'-aminophenyl)-3-(4-methoxyphenyl)-prop-2-en-1-one against the bacteria Staphylococcus aureus carrying a NorA and MepA efflux pump was evaluated.
Journal ArticleDOI
Anti-inflammatory effect, antibiotic potentiating activity against multidrug-resistant strains of Escherichia coli and Staphylococcus aureus, and evaluation of antibiotic resistance mechanisms by the ibuprofen derivative methyl 2-(-4-isobutylphenyl)propanoate.
Maria Regivânia Xavier,Thiago Santiago Freitas,Raimundo Luiz Silva Pereira,Emanuelle Machado Marinho,Paulo Nogueira Bandeira,Amanda P. de Sousa,Larissa Santos Oliveira,Lucas L. Bezerra,José Bezerra de Araújo Neto,M. M. Silva,B.G. Cruz,Janaína Esmeraldo Rocha,Cristina Rodrigues dos Santos Barbosa,Antonio Wlisses da Silva,Jane Eire Silva Alencar de Menezes,Henrique Douglas Melo Coutinho,Márcia Machado Marinho,Emmanuel Silva Marinho,Hélcio Silva dos Santos,A.M.R. Teixeira +19 more
TL;DR: In this paper , the anti-inflammatory effect and antibacterial potential of the ibuprofen derivative Methyl 2-(-4-isobutylphenyl)propanoate (MET-IBU) was evaluated using a zebrafish model.
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