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This work provides the coordination chemistry of the resulting compound of 2-(2-furyl)-3-hydroxychromone and nicotinoyl chloride with first row transition metal ions. Good performance in H2 evolution was shown by the copper-containing photocatalyst.

Microbial infections caused by sessile microorganisms are known to be a more challenging issue than infections caused by the same microorganisms in the planktonic state. Pseudomonas aeruginosa is an opportunistic pathogen and biofilm-forming agent. This species presents intense cellular communication mediated by signaling molecules. This process is known as quorum sensing (QS) and induces the transcription of specific genes that favors cell density growth and three-dimensional bacterial grouping. In this context, the discovery of compounds capable of inhibiting the action of the QS signaling molecules seems to be a promising strategy against biofilms. This work aimed to evaluate the anti-biofilm action and the in vitro safety profile of a sulfamethoxazole-Ag complex. The results obtained indicate potential anti-biofilm activity through QS inhibition. In silico tests showed that the compound acts on the las and pqs systems, which are the main regulators of biofilm formation in P. aeruginosa. Additionally, the molecule proved to be safe for human peripheral blood mononuclear cells.

Rapidly growing mycobacteria (RGM) are pathogens that belong to the mycobacteriaceae family and responsible for causing mycobacterioses, which are infections of opportunistic nature and with increasing incidence rates in the world population. This work evaluated the use of six water-soluble cationic porphyrins as photosensitizers for the antimicrobial photodynamic therapy (aPDT) of four RGM strains: Mycolicibacterium fortuitum, Mycolicibacterium smeagmatis, Mycobacteroides abscessus subs. Abscessus, and Mycobacteroides abscessus subsp. massiliense. Experiments were conducted with an adequate concentration of photosensitizer under white-light irradiation conditions over 90 min and the results showed that porphyrins 1 and 2 (M = 2H or ZnII ion) were the most effective and significantly reduced the concentration of viable mycobacteria. The present work shows the result is dependent on the metal-center ion coordinated in the cationic porphyrin core. Moreover, we showed by atomic force microscopy (AFM) the possible membrane photodamage caused by reactive oxygen species and analyzed the morphology and adhesive force properties. Tetra-positively charged and water-soluble metalloporphyrins may be promising antimycobacterial aPDT agents with potential applications in medical clinical cases and bioremediation.

In order to obtain a better knowledge about the endangered species Colletia paradoxa (Rhamnaceae), which appears in fragmented populations, a study was carried out with six populations from differe...

Antibiotic resistance associated with pulmonary infection agents has become a public health problem, being considered one of the main priorities for immediate resolution. Thus, to increase the therapeutic options in the fight against resistant microorganisms, the synthesis of molecules from pre-existing drugs has shown to be a promising alternative. In this sense, the present work reports the synthesis, characterization, and biological evaluation (against fungal and bacterial agents that cause lung infections) of potential metallodrugs based on sulfamethoxazole complexed with Au

Antimicrobial photodynamic therapy (aPDT) has gained prominence in microbiology, especially in treating non-invasive infections. Diseases such as mycobacteriosis, which causes localized infections and has a slow treatment, tend to be future targets for this type of technology. Therefore, this study aimed to explore the action of two isomeric Pd(II)-porphyrins on fast-growing mycobacterial strains (RGM). Tetra-cationic porphyrins (4-PdTPyP and 3-PdTPyP) were synthesized and applied against standard strains of Mycobacteroides abscessus subsp. abscessus (ATCC 19977), Mycolicibacterium fortuitum (ATCC 6841), Mycolicibacterium smegmatis (ATCC 700084), and Mycobacteroides abscessus subsp. massiliense (ATCC 48898). Reactive oxygen species (ROS) scavengers were used in an attempt to determine possible ROS produced by the photosensitizers (PS) under study. Moreover, the impact of porphyrin on the mycobacterial surface was further evaluated by atomic force microscopy (AFM), and we observed significant damage on cells walls and altered nanomechanical and electrostatic adhesion properties. The results presented herein show that the positively charged porphyrin at the meta position (3-PdTPyP) was the most efficient PS against the RGM strains, and its bactericidal activity was proven in two irradiation sessions, with singlet oxygen species being the main ROS involved in this process. This study demonstrated the therapeutic potential of porphyrins, especially the 3-PdTPyP derivative

Microbial infections caused by sessile microorganisms are known to be a more challenging issue than infections caused by the same microorganisms in the planktonic state.

The production of reactive species over physiological levels associated to pathogenic bacteria could represent a high risk for many diseases. The Rosmarinus officinalis L. is used around the world due its pharmacological proprieties. So, in this study our aim is to test for the first time if R. officinalis L. extract (eeRo) and its fractions (DCM, EA, ButOH) could have better or similar antioxidant action to standars and among themselves in vitro or ex vivo, in brain, stomach and liver of rats. Moreover, we intend to clarify their possible effects on pathogenic bacteria. The eeRo was obtained from the dried leaves subjected to an alcoholic extraction and fractioned. The quantification of the constituents of eeRo and fractions were done by HPLC. The antioxidant proprieties of R. officinalis was analyzed by DPPH•- radical scavenging, total antioxidant, dichlorofluorescein, lipid peroxidation and sodium nitroprusside -induced lipid peroxidation assays. The Minimum inhibitory concentrations of R. officinalis L. were tested with standard strains of danger bacteria. The eeRo, DCM, EA had significant total antioxidant and DPPH•- radical scavenging activities. The DCM and eeRo got significant effects against basal levels of reactive species in liver, stomach and brain. The eeRo and DCM protected the liver and brain against lipid peroxidation. The eeRo, DCM, EA and ButOH had inhibitory effect in the Gram-positive and Gram-negative bacteria. In general way, the DCM and eeRo had the best antioxidant and antibacterial effects among all tested fractions. Keywords: Microorganisms, Medicine, Food, Plant, Free radicals

Colletia paradoxa (Spreng.) Esc. (Rhamnaceae, Colletieae) is a medicinal plant, threatened with extinction in Brazil, presenting great morphological variability. Our objective is to investigate the phytochemical components, antioxidant capacity and antimycobacterial activity of different morphotypes of C. paradoxa in different environments. For this, the crude extract of the leaves and branches of the individuals sampled was used. The elimination capacity of the free radicals was determined by the DPPH method, the antimycobacterial activity by the broth microdilution method and the phenolic content by the spectrophotometric method using the Folin-Ciocalteu reagent and by HPLC. The extracts of C. paradoxa and its morphotypes showed significant amounts of phenolic compounds, including quercetin, quercitrin and rutin, besides considerable antioxidant and antimycobacterial activity No connection was detected between the phytochemical composition and different morphotypes of C. paradoxa.

Using molecular hybridization, specific sulfonamide derivatives of eugenol were synthesized with subtle modifications in the allylic chain of the eugenol subunit (and also in the nature of the substituent group in the sulfonamide aromatic ring) which allowed us to study the influence of structural changes on the antimicrobial potential of the hybrids. Antimicrobial test results showed that most of the synthesized hybrid compounds showed good activity with better results than the parent compounds. Molecular docking studies of the hybrids with the essential bacterial enzyme DHPS showed complexes with low binding energies, suggesting that DHPS could be a possible target for the antibacterial sulfonamide-eugenol hybrids. Furthermore, most of the final compounds presented similar docking poses to that of the crystallographic ligand sulfamethoxazole. The results obtained allow us to conclude that these are promising compounds for use as new leads in the search for new antibacterial sulfonamides.

Achyrocline flaccida aqueous extract was obtained by macerating wildflowers. The phytochemical profile present in the A. flaccida aqueous extract was elucidated by HPLC-ESI-MS/MS. Toxicity was evaluated in vitro by comet assay in peripheral blood mononuclear cells (PBMCs) and in vivo using Caenorhabditis elegans as a model. The antioxidant activity was also evaluated, and antimycobacterial activity was assessed by the broth microdilution method. The compounds present in the aqueous extract mainly belonged to the flavonoid class (89%). The concentrations that showed protective effects in C. elegans against oxidative stress and antimycobacterial activity had no toxic effects. The antimycobacterial activity test demonstrated that the concentration of 1,560 µg mL−1 inhibited the growth and eradication of the mycobacterial tested strains. Based on our findings, the A. flaccida aqueous extract presents a viable potential in developing new phytotherapeutic drugs against mycobacteria of clinical relevance.

We report the photoinactivation evaluation of Ag(II) porphyrins (cationic AgTMeP and anionic AgTPPS) in the antimicrobial photodynamic therapy (aPDT) of rapidly growing mycobacterial strains. The aPDT assays in the Mycolicibacterium fortuitum, Mycobacteroides abscessus subs. abscessus, Mycobacteroides abscessus subsp. massiliense, and Mycolicibacterium smegmatis strains conducted without aggregating photosensitizers (PS) under irradiation for 90 min (270 J/cm

In this manuscript, we report, for the first time, the photoinactivation evaluation of tetra-cationic porphyrins with peripheral Pt (II)-bpy complexes in the photodynamic inactivation (PDI) of rapidly growing mycobacterial strains (RGM). Two different isomeric Pt (II)-porphyrins were synthetized and applied. PDI experiments in the strains of Mycobacteroides abscessus subsp. Abscessus (ATCC 19977), Mycolicibacterium fortuitum (ATCC 6841), Mycobacteroides abscessus subsp. Massiliense (ATCC 48898), and Mycolicibacterium smegmatis (ATCC 700084) conducted with adequate concentration (without aggregation) of photosensitizers (PS) under white-light illumination for 90 min showed that the most effective PS significantly reduced the concentration of viable mycobacteria. The present results show that positively charged porphyrins at the meta position (3-PtTPyP) are more efficient PS against M. abscessus, M. fortuitum, M. massiliense, and M. smegmatis. The effectiveness of the molecule as PS for PDI studies is also clear with mycobacteria, which is strongly related with the porphyrin peripheral charge and coordination platinum (II) compounds and consequently their solubility in physiological media. Tetra-cationic PS may be promising anti-mycobacterial PDI agents with potential applications in medical clinical cases and bioremediation.

This study investigated the chemical constituents of Gaultheria procumbens essential oil and is the first to relate cytogenotoxicity with oxidative metabolism and antimicrobial activity. Chromatographic analysis of the essential oil showed methyl salicylate (99.96%) and linalool (0.04%) as the major compounds. The essential oil showed no signs of cytogenotoxicity at different concentrations (1.82 to 58.34 mg mL−1). Furthermore, G. procumbens essential oil and methyl salicylate were used to evaluate the minimal inhibitory concentrations (MIC) and minimal microbicidal concentrations (MMC). The results showed efficacy against several microorganisms, including Aeromonas caviae, Candida albicans, and Mycobacterium fortuitum with MIC values ranging from 1.82 to 3.64 mg mL−1 and MMC values ranging from 3.64 to 12.67 mg mL−1, which were confirmed by time-kill kinetics. Based on our results, the essential oil is a promising alternative to developing future formulations to treat infections caused by microorganisms.

The antibacterial activity of sulfadiazine Au-PPh3, sulfadiazine Ph2P-Au-Au-PPh2, sulfamethoxazole Au-PPh3, sulfamethoxazole Ph2P-Au-Au-PPh2, sulfamethoxazole Au-PPh3 were tested against Pseudomonas aeruginosa. The antibacterial activity of sulfonamide was tested against P. aeruginosa through the MIC assay, quantitative analysis of biofilm inhibition and observation of biofilm formation with fluorescence microscopy. Besides, the compounds presented remarkable inhibition of P. aeruginosa biofilm formation. Furthermore, molecular docking was performed to identify the key structural features of these compounds with the binding site of the LasR receptor.

The drug-resistant strains of Staphylococcus aureus have been considered as one of the serious health threats, which are related to high patient hospitalization rates. Besides, Staphylococcus aureus biofilm formation exhibits a drug-tolerant nature and shows nonspecific resistance against a broad-spectrum of antibiotics. The emergence of drug-resistant bacteria stimulated the development of novel medicines as a strategy to control infections. In this study, we evaluated the antibacterial and anti-biofilm activity of gold-complexed sulfonamides against Staphylococcus aureus strains such as methicillin-resistant S. aureus and clinical isolates. Our data showed that the exposure of gold-complexed sulfonamides promoted a remarkable reduction in the bacterial adhesion. Also, confocal microscopy displayed the effects of the compounds on in the bacterial cell biofilm, revealed that the compounds decreased the biofilm formation. Our results also demonstrated that gold-complexed sulfonamides exhibited potent antibacterial activity against Staphylococcus aureus strains. Besides, all compounds presented a synergic antibacterial activity when were associated with classical antibiotics. Gold-complexed sulfonamide compounds did not promote toxic effects on Caenorhabditis elegans. Thus, our results showed that the coordination of sulfonamide with gold is a promising alternative in the development of safe and active compounds against methicillin-resistant and clinical isolates S. aureus.

Three diterpenes (1, 4, 5), four lignans (2, 6, 7a, 7b), one sequiterpene (3) and one alkaloid (8) were isolated from an acidic ether fraction of Aristolochia triangularis Cham. native from Brazil. The compounds were identified as: ent-Kaur-16-en-19-al (1), zuonin B (2), nerolidol (3), (−)-Kaur-16-en-19-oic acid (4), ent-Kauran-16β,17-diol (5), dihydrocubebin (6), a mixture of α and β-cubebin (7a + 7b) and aristolactam BII (8). The methanol extract, fractions and the isolated substances were evaluated to check their antimicrobial/antimycobacterial activity against bacteria (14 strains), fungi (9 strains) and mycobacteria (3 strains). Shigella sonnei was highly susceptible to (−)-Kaur-16-en-19-oic acid (4), which showed a potency similar to the antibacterial substance chloramphenicol (MICs at

Biofilms are considered important sources of infections on biomedical surfaces, and most infections involving biofilm formation are associated with medical device implants. Therefore, there is an urgent need for new antimicrobial compounds that can combat microbial resistance associated with biofilm formation. In this context, this work aimed to evaluate the antibiofilm action of sulfamethoxazole complexed with Au, Cd, Cu, Ni and Hg on rapidly growing mycobacteria (RGM), as well as to evaluate their safety through cytotoxic assays. The results demonstrate potentiation of the novel compounds in antibiofilm activity, mainly in the complex with Au, which was able to completely inhibit biofilm formation and had the capacity to destroy the biofilm at all the concentrations tested. All cytotoxic data suggest that the majority of sulfamethoxazole metallic derivatives are antimicrobial alternatives, as well as safe molecules, which could be used as potential therapeutic agents for bacterial and biofilm elimination.

Background: Irvingia gabonensis stem bark is a medicinal plant used in most parts of Africa to manage a number of ailments including neurodegenerative diseases that occur without scientific basis. This work characterized the phenolic composition, evaluated the cholinergic enzymes (acetylcholinesterase, AChE and butyrylcholinesterase, BChE) inhibition, and assessed the antioxidant activity of phenolic extracts from I. gabonensis (Aubry-Lecomte ex O‘Rorke) Baill bark. Methods: Total phenol and flavonoids content was evaluated in addition to antioxidant activity as shown by Fe2+ chelation, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability, and 2,2-azino-bis-(3-ethylbenthiazoline-6-sulfonic acid) (ABTS) radical scavenging ability. Inhibitory activities on AChE and BChE were evaluated. Results: The extract was found to be rich in phenolic acid (ellagic acid) and flavonoids (quercetrin, kaempferol, and apigenin). The phenolic extracts displayed DPPH radical scavenging ability (IC50=19.98 μg/mL), ABTS radical scavenging ability (IC50=18.25 μg/mL), iron chelation (IC50=113.10 μg/mL), and reducing power (Fe3+ to Fe2+) (5.94 mg ascorbic acid equivalent/100 g). Extracts of I. gabonensis inhibited AChE (IC50=32.90 μg/mL) and BChE (IC50=41.50 μg/mL) activities in concentration-dependent manner. Conclusions: Hence, possible mechanism through which the stem bark executes their anti-Alzheimer’s disease activity might be by inhibiting cholinesterase activities in addition to suppressing oxidative-stress-induced neurodegeneration.

Tithonia diversifolia (Hemsl.) A. Gray leaves have long been used to manage neurodegenerative diseases without scientific basis. This study characterized the phenolic constituents, evaluated the antioxidant properties of phenolic extracts from T. diversifolia leaves used as traditional medicine in Africa and its inhibition of key enzymes linked to Alzheimer’s disease. The extract was rich in phenolic acids (gallic acid, chlorogenic acid, caffeic acid and p-coumaric acid) and flavonoids (apigenin) and had 1,1-diphenyl-2-picryl-hydrazil radical scavenging abilities (IC50 = 41.05 μg. mL−1), 2,2-Azino-bis3-ethylbenthiazoline-6sulphonic acid radical scavenging ability (IC50 = 33.51 μg. mL−1), iron chelation (IC50 = 38.50 μg. mL−1), reducing power (Fe3+- Fe2+) (7.34 AAEmg/100 g), inhibited acetylcholinesterase (IC50 = 39.27 μg mL−1) and butyrylcholinesterase (IC50 = 35.01 μg mL−1) activities. These results reveal the leaf as a rich source of phenolic compounds with antioxidant and cholinesterase inhibitory activity. Keywords: Tithonia diversifolia leaves, Antioxidant activity, Cholinergic enzymes, Alzheimer’s disease

Tiger nut has been reportedly used in traditional medicine as sex enhancer. Hence, this study sought to investigate its effect in supplemented diet on some key biochemical indices relevant to erectile function in male rats. The rats were divided into five groups (n = 8): rats fed basal diet; rats fed diet supplemented with 10% processed tiger nut; rats fed diet supplemented with 10% raw tiger nut; rats fed diet supplemented with 20% processed tiger nut and rats fed diet supplemented with 20% raw tiger nut. After 14 days, the corpus cavernosum was isolated for the investigation of adenosine deaminase (ADA), acetylcholinesterase (AChE) and arginase activities as well as nitric oxide (NOx) and malondialdehyde (MDA) contents. A marked reduction in ADA, AChE and arginase activities with a concomitant increase in NOx content when compared to the control was observed. These activities could further buttress aphrodisiac properties of tiger nut as obtained in folklore.

Scutia buxifolia Reissek (Rhamnaceae), popularly known in Brazil as “coronilha”, is a plant species used in folk medicine for several disorders, including inflammation. However, no studies have been done with this species to confirm its topical anti-inflammatory action. In this study we evaluate the topical antiedematogenic and anti-inflammatory effects of the gel containing crude extract (CE) and the gel containing ethyl acetate (EtOAc) fraction of S . buxifolia on croton oil or UVB radiation-induced ear edema in mice, and perform gel stability study. Antiedematogenic and anti-inflammatory effects were evaluated through ear edema induced by irritant agent croton oil, UVB irradiation-induced skin injury model and neutrophil infiltration. The gel stability study was performed by analyzing organoleptical aspects, pH, viscosity, and quantification of quercetin and rutin by HPLC. The topical treatment with S . buxifolia gel reduced the ear edema and myeloperoxidase activity. Antiedematogenic and anti-inflammatory effects of S . buxifolia were obtained with concentrations of 0.3, 1 and 3%, with maximal inhibition in the concentration of 1% for gel containing CE (inhibitions of 100, 73 ± 0.05 and 97 ± 0.08% for croton oil- or UVB irradiation-induced ear edema and myeloperoxidase activity, respectively) and EtOAc fraction (inhibitions of 79 ± 0.05, 73 ± 0.05 and 89 ± 0.04% for croton oil- or UVB irradiation-induced ear edema and myeloperoxidase activity, respectively). Such effects may be attributed, at least in part, to rutin and quercetin, as well as other compounds found in this species. No important changes were detected in the stability study, in all aspects analyzed in temperature below 25 °C. Our results demonstrate that topically applied S . buxifolia gel presented anti-inflammatory effects, provided that it was maintained at a temperature below 25 °C.

The exploitation of forest resources, especially non-timber forest products, has effects on different biological levels, from the biochemical level of an organism to the ecosystem level. The present study addresses the effects of different management strategies (protected area, managed area, and an area where the species is cultivated in agroforestry systems) in reproductive phenology, fruit features, and phytochemical profiles of Dimorphandra gardneriana (Leguminosae), a tree species, pioneer, and socioeconomically important plant of the Brazilian Savanna. Its fruits are exploited by extractivist communities to obtain rutin and quercetin, which are internationally traded bioflavonoids (two of the ten most exported phytochemicals in Brazil). The results showed that the effects on these parameters were characterized as positive, increasing according to the level of exploitation. The agroforestry system had higher yields of flavonoids of economic interest, viable fruits and seeds, followed by the management area and the protected area. Finally, knowledge about the planting effects on fava d'anta fruit production can be a great ally for effectively managing forest resources. A varied system of exploitation implies greater and more stable economic returns for extractive communities, favoring the conservation of the species in protected areas.

Organic selenium compounds are widely associated with numerous pharmacological properties. However, selenium compounds, such as Ebselen (Ebs) and Diphenyl Diselenide (DPDS), could interact with mitochondrial respiratory complexes, especially with thiol groups. The present study evaluated whether the insertion of functional groups, o-methoxy, and p-methyl on organic selenium compounds promotes changes in mitochondrial functioning parameters and whether this is related to antibacterial activity. Here we tested some in vitro parameters after the exposure of mitochondria to different concentrations of β-selenoamines 1-phenyl-3-(p-tolylselanyl)propan-2-amine (C1) and 1-(2-methoxyphenylselanyl)-3-phenylpropan-2-amine (C2) and analogs of DPDS 1,2-bis(2-methoxyphenyl)diselenide (C3) and 1,2-bisp-tolyldiselenide (C4). We also evaluated the antibacterial activity of β-selenoamines and diselenides against Methicillin-resistant Staphylococcus aureus and Escherichia coli. Our results showed that o-methoxy insertion increased the antioxidant properties, without affecting the mitochondrial membrane potential. The compounds with a p-methyl insertion affected the mitochondrial membrane potential and significantly decreased the State III respiration and RCR. Besides, the p-methyl compounds presented antibacterial activity at lower concentrations than those shown in o-methoxy, precisely by the same mechanism that promotes damage to thiol groups and better absorption in gram-positive bacteria due to their relationship with cell wall constituents. Finally, our study confirms that structural modifications in organic selenium compounds provide changes in mitochondrial functioning but also raise their antibacterial effect. This strategy can be used as a target for the development of new enough potent antibacterial to restrict the advance of resistant bacterial infections.

This manuscript reports, at the first time, the photoinactivation evaluation of tetra-cationic and anionic porphyrins as photosensitizers (PS) for the photodynamic inactivation (PDI) of rapidly growing mycobacteria strains. Two different charged porphyrin groups were obtained commercially. PDI experiments in the strains Mycobacterium massiliense e Mycobacterium fortuitum conducted with adequate concentration (without aggregation) of photosensitizer under white light at a fluence rate of 50 mW/cm2 over 90 min showed that the most effective PS caused a 100 times reduction in the concentration of viable mycobacteria. The present results show that porphyrin with positively charge are more efficient PS than anionic porphyrin (negatively charged) against M. massiliense e M. fortuitum. It is also clear that the effectiveness of the molecule as PS for PDI studies with mycobacteria is strongly related with the porphyrin peripheral charge, and consequently their solubility in physiological media. Cationic PSs might be promising anti-mycobacteria PDI agents with potential applications in medical clinical cases and bioremediation.

Eugenol has diverse biological properties including antimycobacterial activity, and the triazole ring is an important heterocycle in antimycobacterial compounds. Therefore, this research aimed to synthesize novel eugenol-derived 1,2,3-triazole as antimycobacterial agents with interesting cytotoxic profile and pharmacological assets. Sixteen compounds were obtained and characterized by nuclear magnetic resonance (NMR), infrared (IR), and high-resolution mass spectrometry (HRMS). Among them, the best growth inhibition properties from a microdilution assay were observed for three derivatives: a benzylic ether (minimum inhibitory concentration (MIC) = 48.89 µM) against Mycobacterium abscessus (ATCC 19977), an O-galactosyde (MIC = 31.76 µM) against Mycobacterium massiliense (ATCC 48898) and a sulfonate (MIC = 88.64 µM) against Mycobacterium fortuitum (ATCC 6841). They can form biofilms, and the infection progression is challenging to control due to multi-drug resistance profiles against diverse antibiotics. In conclusion, the above-mentioned compounds represent starting points in the search of bioactive molecules against mycobacteria with low cytotoxicity and better pharmacological profiles.

Highlights • Rapidly growing mycobacteria (RGM) causing infections by biofilm formation. • Semi-quantitative method of biofilm formation was adapted for macrotechnics. • Sulphonamides complexed with metals is a promising anti-adhesion agent. • Sulphonamides complexed with metal is a possible inhibitor of signaling of biofilm formation., Rapidly growing mycobacteria (RGM) are found in non-sterile water and often associated with severe post-surgical infections and affect immunocompromised patients. In addition, RGM can prevent the host's immune response and have the ability to adhere to and form biofilms on biological and synthetic substrates, making pharmacological treatment difficult because conventional antimicrobials are ineffective against biofilms. Thus, there is an urgent need for new antimicrobial compounds that can overcome these problems. In this context, sulfonamides complexed with Au, Cd, Ag, Cu, and Hg have shown excellent activity against various microorganisms. Considering the importance of combating RGM-associated infections, this study aimed to evaluate the activity of sulfonamide metal complexes against RGM biofilm. The sulfonamides were tested individually for their ability to inhibit mycobacterial formation and destroy the preformed biofilm of standard RGM strains, such as Mycobacterium abscessus, M. fortuitum, and M. massiliense. All sulfonamides complexed with metals could reduce, at subinhibitory concentrations, the adhesion and biofilm formation of three RGM species in polystyrene tubes. It is plausible that the anti-biofilm capacity of the compounds is due to the inhibition of c-di-GMP synthesis, which is an important signal for RGM biofilm formation. Hence, the impacts and scientific contribution of this study are based on the discovery of a potential new therapeutic option against RGM-associated biofilm infections. Sulfonamides complexed with metals have proven to be a useful and promising tool to reduce microbial adhesion on inert surfaces, stimulating the improvement of methodologies to insert compounds as new antibacterial and coating agents for medical and hospital materials.

The A22 is a chemical compound that acts as a reversible inhibitor of a bacterial cell wall protein MreB leading the rods to the coccoid form. Thus, by changing the bacterial form, many properties can be affected, as the acquisition of nutrients, cell division, the clamping surfaces, motility and pathogenesis. Infections caused by strains of Pseudomonas aeruginosa have great clinical importance because these microorganisms can include more than one resistance mechanism acting together, limiting treatment options. Thus, it is important to investigate the action of A22 against P. aeruginosa, once there are urgent needs for new antimicrobial compounds for increase the arsenal therapeutic to treat diseases caused by this microrganism. Therefore, this study investigated for the first time the antimicrobial activity of A22 against seve standards strains of Gram negative microorganisms and twenty-eight clinical isolates of P. aeruginosa. This study performed an additional investigation to analyze the cyto and genotoxic potential effects from A22 on human peripheral blood mononuclear cells (PBMCs). The antibacterial activity of A22 was studied by broth microdilution method and time-kill assay. The cytotoxicity was evaluated by MTT assay at 24, 48 and 72 h of exposure to A22 and the genotoxicity was evaluated by the Comet assay. The susceptibility tests showed A22 has a relevant antibacterial activity against P. aeruginosa, including multidrug-resistant (MDR) clinical isolates. The A22 treatment not showed genotoxic effects against PBMCs in almost all concentrations tested at 24 and 48 h of exposure. Only for concentration of 32 μg/mL (highest tested) the damage index was significantly higher in all moments. The MTT assay demonstrated that A22 was able to maintain cell viability in all exposure times. In summary, the A22 demonstrated important anti-Pseudomonas activity and showed no cyto and genotoxic significant effect. These results need to be considered in future in vitro and in vivo studies in order to introduce the A22 as a possible therapeutic option.

denosine deaminase (ADA) is a critical control point in the regulation of adenosine levels. This study aimed to investigate the effects of a polyphenolic flavonoid, rutin, on the activity of ADA in serum, the cerebral cortex, liver, kidney, and biochemical parameters in diabetic rats. The animals were divided into four groups (n=6) for the following treatments: control; diabetic (streptozotocin 55 mg/kg); diabetic with rutin (100 mg/kg/day); diabetic with glibenclamide (10 mg/kg/day). After 30 days, ADA activity and biochemical parameters were analyzed. The ADA activity in the serum was significantly elevated in the diabetic group compared to the control group (p

Several species of rapidly growing mycobacteria (RGM) have been associated with biofilms in areas such as biomedical devices, water distribution systems, cosmetic surgery, and catheter-related blood infections. Biofilms which exhibit antimicrobial resistance such as those formed by the genus Mycobacterium pose a significant risk to health and are of particular interest to researchers. Licarin A (a neolignan found in numerous plant species e.g. nutmeg) has been reported to show a wide range of biological actions including anti-inflammatory, antioxidant, and antibacterial properties. The aim of this study was to prepare a set of Licarin A derivatives and investigate the impact of specific structural changes on its antimycobacterial ability, and its effect on the biofilm formation of RGM species. Initially, the phenolic sub-unit and alkenyl side chain of Licarin A were modified to create derivatives with a higher partition coefficient; as the activity of a compound against mycobacteria seems to be strongly influenced by its hydrophobicity. Further, polar groups were inserted into the side chain to change the hydrophilic-lipophilic profile of the molecules. Results showed variability in the susceptibility profile of mycobacteria against the Licarin A derivatives under analysis. A number of the derivatives showed significant inhibitory activity of planktonic growth of the three strains of mycobacteria used, with even lower MIC values than those observed with reference drugs and Licarin A itself. Cytotoxicity assays showed they also have low toxicity, confirming that structural modifications to the Licarin A have made improvements to its antimycobacterial properties.

The main objective of this study was to demonstrate the antimicrobial potential of the crude extract and fractions of Chenopodium ambrosioides L., popularly known as Santa-Maria herb, against microorganisms of clinical interest by the microdilution technique, and also to show the chromatographic profile of the phenolic compounds in the species. The Phytochemical screening revealed the presence of cardiotonic, anthraquinone, alkaloids, tannins and flavonoids. The analysis by HPLC-DAD revealed the presence of rutin in the crude extract (12.5 ± 0.20 mg/g), ethyl acetate (16.5 ± 0.37 mg/g) and n-butanol (8.85 ± 0.11 mg/g), whereas quercetin and chrysin were quantified in chloroform fraction (1.95 ± 0.04 and 1.04 ± 0.01 mg/g), respectively. The most promising results were obtained with the ethyl acetate fraction, which inhibited a greater number of microorganisms and presented the lowest values of MIC against Staphylococcus aureus and Enterococcus faecalis (MIC = 0.42 mg/mL), Pseudomonas aeruginosa (MIC = 34.37 mg/mL), Paenibacillus apiarus (MIC = 4.29 mg/mL) and Paenibacillus thiaminolyticus (MIC = 4.29 mg/mL). Considering mycobacterial inhibition, the best results were obtained by chloroform fraction against M. tuberculosis, M. smegmatis, and M. avium (MIC ranging from 156.25 to 625 µg/mL). This study proves, in part, that the popular use of C. ambrosioides L. can be an effective and sustainable alternative for the prevention and treatment of diseases caused by various infectious agents.

The phenolic extract of Senecio biafrae leaves was investigated to determine the in vitro antioxidant, phenolic profiles, and inhibition of key enzymes relevant to type II diabetes mellitus (α‐amylase and α‐glucosidase) and Alzheimer's disease (acetylcholinesterase and butrylcholinesterase). The phenolic extract demonstrated significant scavenging abilities against all in vitro antioxidant parameters assessed. Reversed‐phase HPLC of the extract revealed the presence of gallic acid, chlorogenic, caffeic acid, rutin, quercetin, and kaempferol. The extract also inhibited activities of α‐amylase (IC 50 = 126.90 μg/ml), α‐glucosidase (IC 50 = 139.66 μg/ml), acetylcholinesterase (IC 50 = 347.22 μg/ml), and butrylcholinesterase (IC 50 = 378.79 μg/ml), which may be attributed to the antioxidant potential of the extract and its phenolic composition. Therefore, this study suggests that the leaves of S. biafrae may be useful in the management of diabetes mellitus and Alzheimer's disease.

Schinus molle L. is used to treat various diseases; however, the literature lacks information regarding its possible immunotoxic effects. The aim of the study was to investigate the immunotoxic effects of essential oil from leaves of Schinus molle L. in cultures of human lymphocytes and macrophages. The cultures were treated with essential oil (EO) of Schinus molle L. and subsequently subjected to genotoxic analysis (comet assay), mutagenic analysis (micronucleus frequency and chromosomal aberration), and cytotoxic (cell viability) and functional parameters (interleukins secretions). Our analyses have determined that the essential oil from leaves of Schinus molle L. presents several compounds with α-pinene being the major compound; in addition, the compound verbenene was firstly identified; genotoxic effects were detected only in macrophages and only at the two highest concentrations tested. An important finding is that Schinus molle L. oil causes an activation of the immune system. This action has its mechanism centered by the cascade nitric oxide-interleukin-10-tumor necrosis factor alpha.

The present study aimed to genotypically and phenotypically characterize clinical isolates of carbapenem-resistant Enterobacteriaceae collected from inpatients at the University Hospital of Santa Maria, during seven months. Among the clinical isolates subjected to the modified Hodge test (MHT), 62.5% were positive, indicating possible production of carbapenemase. Polymerase chain reaction (PCR) demonstrated that blaKPC was the most frequently found gene (31%), followed by blaIMP (12.5%). Combined use of the methods is needed to identify carbapenem resistance in enterobacteria to prevent their spread and control the infections caused by these organisms. RESUMO Objetivou-se caracterizar fenotípica e genotipicamente isolados clínicos de enterobactérias resistentes aos carbapenêmicos (CRE) provenientes do Hospital Universitário de Santa Maria (RS). Entre os isolados clínicos submetidos ao teste modificado de Hodge (MHT), 62,5% apresentaram positividade, indicando possível produção de carbapenemase. A reação em cadeia da polimerase (PCR) demonstrou que o blaKPC foi o gene mais encontrado (31%), seguido de blaIMP (12,5%). O uso conjunto de distintas metodologias faz-se necessário para identificar a resistência aos carbapenêmicos produzida pelas enterobactérias, de modo a auxiliar o controle de infecção prevenindo a disseminação desses microrganismos.