Antimicrobial activity of carvacrol and its derivatives on spp.: systematic review of preclinical studies.

The scope of the study was to analyze original preclinical studies on the antimicrobial effects of carvacrol and derivatives on the genus. According to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses statement, four databases (PubMed, Web of Science, SCOPUS and EMBASE) were searched. The search retrieved 392 records, of which 11 papers were selected.

Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity.

Paracoccidioidomycosis (PCM) is a systemic infection caused by spp. (). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, caused by ().

Essential oil of is active against mycobacteria.

There is critical need for new therapeutic options for treatment of diseases caused by mycobacteria. essential oils (EOs) and crude extracts (CEs) were tested for their anti- and anti-nontuberculous mycobacteria activity. Minimum inhibitory concentration (MIC) of EOs ranged from 15.

Polymyxin B Activity Rescue by (-)-Camphene-Based Thiosemicarbazide Against Carbapenem-Resistant .

Due to the significant shortage of therapeutic options for carbapenem-resistant (CRE) infections, new drugs or therapeutic combinations are urgently required. We show in this study that (-)-camphene-based thiosemicarbazide (TSC) may act synergistically with polymyxin B (PMB) against CRE, rescuing the activity of this antimicrobial. With the specific aim of a better molecular understanding of this effect caused by the presence of TSC, theoretical calculations were also performed in this study.

Binding of piperine to mycobacterial RNA polymerase improves the efficacy of rifampicin activity against and nontuberculous mycobacteria.

Piperine (PPN) is a known inhibitor of efflux pumps in and synergism with rifampicin (RIF) has been proven. The current study evaluates the activity of PPN and synergism with RIF in rapidly and slowly growing nontuberculous mycobacteria (NTM). Also, to propose a possible mechanism of interaction of PPN with (Mlp) RNA polymerase (RNAp).

Rescue of susceptibility to second-line drugs in resistant clinical isolates of .

Antibiotic resistance is one of the biggest threats to global health, and this study aimed better understand how the efflux pumps are related to this process in tuberculosis clinical isolates. The combination of antibiotics plus efflux pumps (EP) inhibitors was able to restore the susceptibility of clinical isolates in 100% of aminoglycosides resistance and 33.3% of the fluoroquinolones resistance.

3,5-dinitrobenzoylhydrazone derivatives as a scaffold for antituberculosis drug development.

The development of drugs is essential to eradicate tuberculosis. Sixteen 3,5-dinitrobenzoylhydrazone () derivatives and their synthetic precursors 3,5-dinitrobenzoylhydrazide () and methyl ester () were screened for their anti- () potential. Twelve compounds had minimum inhibitory concentration (MIC) ranging from 0.

Proteomic profiling of carbapenemase (KPC)-producer after induced polymyxin resistance.

To elucidate the changes in protein expression associated with polymyxin resistance in , we profiled a comparative proteomic analysis of polymyxin B-resistant mutants KPC-2-producing , and of its susceptible counterparts. Two-dimensional reversed phase nano ultra-performance liquid chromatography mass spectrometry was used for proteomic analysis. Our results showed that the proteomic profile involved several biological processes, and we highlight the downregulation of outer membrane protein A (OmpA) and the upregulation of SlyB outer membrane lipoprotein (conserved protein member of the PhoPQ regulon) and AcrA multidrug efflux pump in polymyxin B-resistant strains.

Rescue of streptomycin activity by piperine in .

To evaluate the modulatory effect of piperine (PIP) on streptomycin (SM) activity in (). SM and PIP minimum inhibitory concentration (MIC) and combinatory activity were determined in HRv and in susceptible and resistant clinical isolates. Ethidium bromide accumulation assay and relative quantification of efflux pumps genes ( and ), after SM and SM+PIP combination exposure, were also performed.

Antituberculosis Activities of Lapachol and β-Lapachone in Combination with Other Drugs in Acidic pH.

The treatment of multidrug-resistant tuberculosis (MDR-TB) is a challenge to be overcome. The increase of resistant isolates associated with serious side effects during therapy leads to the search for substances that have anti-TB activity, which make treatment less toxic, and also act in the macrophage acidic environment promoted by the infection. The aim of this study was to investigate lapachol and β-lapachone activities in combination with other drugs against at neutral and acidic pH and its cytotoxicity.

(-)-Camphene-based derivatives as potential antibacterial agents against and spp.

To evaluate the activity of (-)-camphene-based thiosemicarbazide (TSC) and 4-hydroxy-thiosemicarbazone (4-OH-TSZ), alone and in combination against Gram-positive. MIC were determined for , spp. reference strains and clinical isolates.

Structure-activity relationship of natural and synthetic coumarin derivatives against .

Eight coumarin derivatives () obtained from natural (-)-mammea A/BB () and 13 synthetic coumarins () had their cytotoxicity and biological activity evaluated against HRv reference strain and multidrug-resistant clinical isolates. Anti- activity was evaluated by resazurin microtiter assay plate, and the cytotoxicity of natural and synthetic products using J774A.1 macrophages by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.

Synthesis and biological evaluation of 12 novel (-)-camphene-based 1,3,4-thiadiazoles against .

To evaluate the activity, cytotoxicity and efflux pumps inhibition of a series of 12 novels (-)-camphene-based 1,3,4-thiadiazoles (TDZs) against (). The minimum inhibitory concentration (MIC), cytotoxicity for three cell lines, ethidium bromide accumulation and checkerboard methods were carried out. Compounds (, , , , and ) showed significant anti- activity (MIC 3.

Insight about cell wall remodulation triggered by rifampicin in Mycobacterium tuberculosis.

Rifampicin plays an important role during the treatment of tuberculosis, which makes it to be recommended throughout the regimen. The molecular target for rifampicin activity and resistance is the bacterial RNA polymerase coded by rpoB. However, it has been observed that Mycobacterium tuberculosis could use different metabolic pathways contributing to drug activity/resistance.

Determination of minimum bactericidal concentration, in single or combination drugs, against .

To evaluate an assay to detect minimum bactericidal concentration (MBC) in , using as single model rifampicin, isoniazid, levofloxacin (LVX) and linezolid (LNZ) and in combination. MBCs were carried out directly from resazurin microtiter assay plate and 3D checkerboard in HRv and five resistant clinical isolates. The proposed MBC assay showed similar values to those determined by MGIT™, used as control.

Minimum Bactericidal Concentration Techniques in : A Systematic Review.

Minimum bactericidal concentration (MBC) assay is an accepted parameter for evaluating new antimicrobial agents, and it is frequently used as a research tool to provide a prediction of bacterial eradication. To the best of our knowledge, there is no standardization among researchers regarding the technique used to detect a drug's MBC in . Thus, the aim of this systematic review is to discuss the available literature in determining a drug's MBC in , to find the most commonly used technique and standardize the process.

Synthesis and anti-Mycobacterium tuberculosis activity of imide-β-carboline and carbomethoxy-β-carboline derivatives.

A series of methyl β-carboline carboxylates (2a-g) and of imide-β-carboline derivatives containing the phthalimide (4a-g), maleimide (5b, g) and succinimide (6b, e, g) moiety were synthesized, and evaluated for their activity against Mycobacterium tuberculosis HRv. The most active β-carboline derivatives against the reference strain were assayed for their cytotoxicity and the activity against resistant M. tuberculosis clinical isolates.

Activity of (-)-Camphene Derivatives Against Mycobacterium tuberculosis in Acidic pH.

Background: For more than 60 years, the lack of new anti-tuberculosis drugs and the increase of resistant Mycobacterium tuberculosis lineages exhibit a therapeutic challenge, demanding new options for the treatment of resistant tuberculosis.

Objective: Herein, we determined the (i) activities of (-)-camphene and its derivatives and (ii) combinatory effect with pyrazinamide (PZA) against Mycobacterium tuberculosis in acidic pH and (iii) cytotoxicity on VERO cells.

Methods: The activity of (-)-camphene and its 15 derivatives was determined in M.

Possible Binding of Piperine in Mycobacterium tuberculosis RNA Polymerase and Rifampin Synergism.

The activity of rifampin (RIF) and piperine was evaluated at the relative transcript levels of 12 efflux pumps (EPs), and an additional mechanism was proposed to be behind the synergic interactions of piperine plus RIF in AutoDock v4.2.3 and Molegro v6 programs were used to evaluate PIP binding in RNA polymerase (RNAP).

Hydrazone, benzohydrazones and isoniazid-acylhydrazones as potential antituberculosis agents.

To evaluate the potential of three benzohydrazones (-), four acylhydrazones derived from isoniazid (INH-acylhydrazones) (-) and one hydrazone () as antituberculosis agents. Inhibitory and bactericidal activities were determined for the reference () strain and clinical isolates. Cytotoxicity, drug combinations and ethidium bromide accumulation assays were also performed.