Unlocking bacterial defense: Exploring the potent inhibition of NorA efflux pump by coumarin derivatives in Staphylococcus aureus.

The occurrence of bacterial resistance has been increasing, compromising the treatment of various infections. The high virulence of Staphylococcus aureus allows for the maintenance of the infectious process, causing many deaths and hospitalizations. The MepA and NorA efflux pumps are transporter proteins responsible for expelling antimicrobial agents such as fluoroquinolones from the bacterial cell.

In vitro and in silico evidences about the inhibition of MepA efflux pump by coumarin derivatives.

The discovery of antibiotics has significantly transformed the outcomes of bacterial infections in the last decades. However, the development of antibiotic resistance mechanisms has allowed an increasing number of bacterial strains to overcome the action of antibiotics, decreasing their effectiveness against infections they were developed to treat. This study aimed to evaluate the antibacterial activity of synthetic coumarins Staphylococcus aureus in vitro and analyze their interaction with the MepA efflux pump in silico.

In vitro and in silico antibacterial evaluation of coumarin derivatives against MDR strains of Staphylococcus aureus and Escherichia coli.

The increase in antibiotic resistance rates has attracted the interest of researchers for antibacterial compounds capable of potentiating the activity of conventional antibiotics. Coumarin derivatives have been reported to develop effective antibacterials with possible new mechanisms of action for treating infectious diseases caused by bacteria with a profile of drug resistance. In this context, the aim of the present study we have now prepared one variety of new synthetic coumarins evaluating the pharmacokinetic and chemical similarity in silico, their antimicrobial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922), and potential for the modulation of antibiotic resistance against Staphylococcus aureus (SA10) and Escherichia coli (EC06) clinical isolate bacteria by in vitro assay.

Inhibition of Staphylococcus aureus TetK and MsrA efflux pumps by hydroxyamines derived from lapachol and norlachol.

The present study aimed to evaluate the in vitro efflux pump inhibitory capacity of hydroxyamines derived from lapachol and norlachol, where compounds 3, 4, and 5 were tested against the S. aureus strains: RN4220 carrying the pUL5054 plasmid; and IS-58, endowed with the PT181 plasmid. The substances were synthesized from 2-hydroxy-quinones, lapachol and nor-lapachol obtaining the corresponding 2-methoxylated derivatives via dimethyl sulfate alkylation in a basic medium, which then reacted chemoselectively with 2-ethanolamine and 3-propanolamine to form the corresponding amino alcohols.

Effect of hydroxyamines derived from lapachol and norlachol against Staphylococcus aureus strains carrying the NorA efflux pump.

Isolated substances and those organically synthesized have stood out over the years for their therapeutic properties, including their antibacterial activity. These compounds may be an alternative to the production of new antibiotics or may have the ability to potentiate the action of preexisting ones. In this context, the objective of this study was to evaluate the in vitro antibacterial and efflux pump inhibitory activity of hydroxyamines derived from lapachol and norlachol, more specifically the compounds 2-(2-Hydroxyethylamino)-3-(3-methyl-2-butenyl)-1,4 dihydro-1,4-naphthalenedione, 2-(2-Hydroxyethylamino)-3-(2-methyl-propenyl)[1,4]naphthoquinone and 2-(3-Hydroxypropylamino)-3-(3-methyl-2-butenyl)-[1,4]naphthoquinone, against Staphylococcus aureus strains carrying the NorA efflux pump mechanism.

In silico evaluation of the antibacterial and modulatory activity of lapachol and nor-lapachol derivates.

The aim of this research was to investigate the pharmacological properties of 2-(2-hydroxyethylamine)-3-(3-methyl-2-butenyl)-1,4-dihydro-1,4-naphthalenedione, 2-(2-hydroxy-ethylamine)-3-(2-methyl-propenyl)-[1,4]naphthoquinone and 2-(3-hydroxy-propylamine)-3-(3-methyl-2-butenyl)-[1,4]naphthoquinone using computational prediction models, in addition to evaluating the in vitro antibacterial and modulatory activity of these compounds against bacterial ATCC strains and clinical isolates. The substances were synthesized from 2-hydroxy-quinones, lapachol and nor-lapachol obtaining the corresponding 2-methoxylated derivatives via dimethyl sulfate alkylation in a basic medium, these then reacted chemoselectively with 2-ethanolamine and 3-propanolamine to form the corresponding amino alcohols. The antibacterial activity and modulatory activity of the substances were assayed by broth microdilution method to determine the Minimum Inhibitory Concentration (MIC).

Inhibition of the essential oil from Chenopodium ambrosioides L. and α-terpinene on the NorA efflux-pump of Staphylococcus aureus.

This study was carried out to test the essential oil from C. ambrosioides leaves and its main constituent, α-Terpinene, in an antibacterial activity assay. As well, it was evaluated ability reduce resistance to norfloxacin and ethidium bromide was compared the Staphylococcus aureus 1199B whith 1199 wild type strain.

Potentiation of antibiotic activity by Mast. front of strains and .

The development of new drugs from plants is an interesting alternative approach to overcoming microbial resistance. shows resistance to diseases and pests and a higher concentration of chemical components that may be useful in the pharmaceutical industry. We investigated the potential antimicrobial and antibiotic-modifying activity of hydroalcoholic extracts of leaves, stems, bark, pulp and seeds of .

Inhibition of the TetK efflux-pump by the essential oil of Chenopodium ambrosioides L. and α-terpinene against Staphylococcus aureus IS-58.

The use of natural products is crucial to suppress the development of these micro-organisms and to reduce the concentration necessary to inhibit these microrganisms, reducing the toxicity risks also. In this study, the essential oil from Chenopodium ambrosioides Leaves and its main constituent α-Terpinene were used in the antibacterial and potentiating activity of antibiotics and ethidium bromide assays, against the bacterial strains Staphylococcus aureus IS-58, carriers of efflux pumps. The Minimum Inhibitory Concentration (MIC) was determined using a microdilution method.

Psidium guajava L., from ethnobiology to scientific evaluation: Elucidating bioactivity against pathogenic microorganisms.

Ethnopharmacological Relevance: The use of popular plants has guided pharmaceutical research aimed at combating pathogenic microorganisms. Psidium guajava L. is a plant of great versatility and it has been used both as food and as a therapeutic agent.

Cytoprotective Effect of Lygodium venustum Sw. (Lygodiaceae) against Mercurium Chloride Toxicity.

Mercury is a very dangerous metal when humans come into contact with it, whether through the air or skin or by ingestion. The aim of this work was to investigate the possible effects of the ethanol extract and fractions of Lygodium venustum Sw. against mercurium chloride toxicity towards Escherichia coli strain ATCC25922.

Potentiation of antibiotic activity of aminoglycosides by natural products from Cordia verbenacea DC.

Medicinal plants are often the only therapeutic resource for many communities and ethnic groups. Cordia verbenacea DC., "Erva-baleeira," is one of the species of plants currently used to produce a phytotherapeutic product extracted from its leaves.

HPLC-DAD phenolic profile, cytotoxic and anti-kinetoplastidae activity of Melissa officinalis.

Context Melissa officinalis subsp. inodora Bornm. (Lamiaceae) has been used since ancient times in folk medicine against various diseases, but it has not been investigated against protozoa.

Modulation of the antibiotic activity against multidrug resistant strains of 4-(phenylsulfonyl) morpholine.

The compound 4-(Phenylsulfonyl) morpholine belongs to the class of sulfonamides, which are widely used in the treatment of a large number of diseases caused by microorganisms. This compound has a morpholine group, which is also known for its antimicrobial properties. The aim of the present study was to investigate the antimicrobial and modulating activity of 4-(Phenylsulfonyl) morpholine against standard and multi-resistant strains of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and strains of the fungi Candida albicans, C.

Antibiotic-modifying activity of riachin, a non-cyanogenic cyanoglycoside extracted from Bauhinia pentandra.

Background: The search for new active compounds from the Brazilian flora has intensified in recent years, especially for new drugs with antibiotic potential. Accordingly, the aim of this study was to determine whether riachin has antibiotic activity in itself or is able to modulate the activity of conventional antibiotics.

Methods: A non-cyanogenic cyanoglycoside known as riachin was isolated from Bauhinia pentandra, and was tested alone and in combination with three antibiotics (clindamycin, amikacin, and gentamicin) against multiresistant bacterial strains (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus).

Analysis of bioactivities and chemical composition of Ziziphus joazeiro Mart. using HPLC-DAD.

The aim of this study was to evaluate the chemical profile and antioxidant, antimicrobial and antiparasitic activities of the hydroalcoholic extract of the leaves of Ziziphus joazeiro Mart. (HELZJ). The antioxidant DPPH and FRAP assays and chemical profile were determined by colorimetric methods and HPLC/DAD.

Evaluation of antibacterial, antifungal and modulatory activity of methanol and ethanol extracts of Padina sanctae-crucis.

Background: Multi-resistantmicroorganisms such as Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida tropicalis e Candida krusei are the main causes of microbial infections. Padina sanctae-crucis is a seaweed often used to check the contamination of ecosystems by materials such as heavy metals, but studies of the antimicrobial activity of the same seaweed were not found.

Methods: The tests for the minimum inhibitory concentration and modulation of microbial resistance, with the use of ethanolic and methanolic extracts of Padina Sanctae-cruces combined with drugs of the class of aminoglycosides and antifungal were used to evaluate the activity against the cited microorganisms.

Chemical composition and evaluation of modulatory of the antibiotic activity from extract and essential oil of Myracrodruon urundeuva.

Context: The combination of antibiotics with natural products has demonstrated promising synergistic effects in several therapeutic studies.

Objective: The aim of this study was to determine the effect of a combination of an ethanol extract of Myracrodruon urundeuva Fr. All.

Biological Activities and Chemical Characterization of Cordia verbenacea DC. as Tool to Validate the Ethnobiological Usage.

Knowledge of medicinal plants is often the only therapeutic resource of many communities and ethnic groups. "Erva-baleeira", Cordia verbenacea DC., is one of the species of plants currently exploited for the purpose of producing a phytotherapeutic product extracted from its leaves.