A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain.

A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain.

A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain.

A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain.

A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain.

Enriquecimiento, disponibilidad y contaminación de metales traza (Cd, Cu, Pb y Zn) en sedimentos de lagunas urbanas de Concepción-Chile

Trace metals (Cd, Cu, Pb and Zn) enrichment, availability and contamination in superficial sediments of three interconnected urban lagoons localized in Concepción-Chile, were evaluated. According to the results of geochemical fracctionation analysis, Cu and Pb are rather associated with oxi-hydroxides, Cd is associated with exchangeable and carbonates fraction, while Zn is mainly associated with organic, oxi-hydroxides and residual fraction. The estimation of the availability percentages indicate that Cu is the most mobile metal and the less mobile is the Cd. An evaluation of the geo-accumulation index and urban industrial pollution allowed to classify the studied zone as moderately to highly contaminated.

Uso da cinza da casca do arroz (CCA) obtida da geração de energia térmica como adsorvente de Zn(II) em soluções aquosas

The removal study was conducted using 1.00 g of the rice husk ash (RHA) and 20.0 mL solution with concentrations in the range of 10-1000 mg/L of Zn(II). The influence of contact time, initial metal concentration, agitation and pH of the removal process was investigated. Superior removals to 95% were obtained at the end of 24 h of contact. The agitation increased in 20% the removal of Zn(II), being needed only 5 min to reach the equilibrium. The adsorption process was studied by the models of isotherms of Langmuir, Freundlich and BET, obtaining results of R L and 1/n for a process favorable of adsorption. BET isotherm best represents the equilibrium adsorption. The results showed that the RHA has the largest capacity and affinity for the removal of Zn(II).

Utilização de pelos de animais silvestres para monitoramento ambiental de Cd, Cr, Cu, Fe, Mn, Pb e Zn

This study investigates the use of wild animal hair of C. brachyurus, C. thous and L. pardalis as biomonitors of trace metal at Parque Nacional das Emas, Brazil. Results reveal a strong correlation between Cd and Pb as well as Cu and Zn, which suggests a single source of emission. Most metals showed a lower or equal concentration than those obtained in previous studies. The research shows that monitoring may be performed only with Zn, Pb, Cd, and Cr because of statistical similarity and of a non-natural occurrence of large amounts of the material under analysis.

Determinação direta de Ca, Mg, Mn e Zn em amostras de leite de búfala da Ilha de Marajó por espectrometria de absorção atômica com chama (FAAS)

This work proposes an analytical procedure for direct determination of calcium, magnesium, manganese and zinc in buffalo milk by flame atomic absorption spectrometry (FAAS). Samples were diluted with a solution containing 10% (v/v) of water-soluble tertiary amines (CFA-C) at pH 8. For comparison, buffalo milk samples were digested with HNO3 and H2O2. According to a paired t-test, the results obtained in the determination of Ca, Mg, Mn and Zn in digested samples and in 10% (v/v) CFA-C medium were in agreement at a 95% confidence level. The developed procedure is simple, rapid, decrease the possibility of contamination and can be applied for the routine determination of Ca, Mg, Mn and Zn in buffalo milk samples without any difficulty caused by matrix constituents, such as fat content, and particle size distribution in the milk emulsion.

Desenvolvimento e aplicação de sistema passivo de coleta de poluentes atmosféricos para monitoramento de Cd, Cr, Pb, Cu, Fe, Mn, Zn e particulados totais

The objective of this study was to assess a new monitoring technique of particulate and trace metals in the atmosphere via the use of a passive sampler of air pollutants in the city of Goiânia. The average particulate weight and average concentrations of metals Fe, Cr, Zn, Pb, Cu, Mn, and Cd were 0.1104 g and 257.5; 23.4; 17.8; 6.7; 1.9; 0.8; 0.2 μg/m²/day, respectively. Higher Pb and Cr concentrations were obtained in areas with intense traffic. This study revealed that it is possible to monitor trace metals with passive sampling, developed at a low cost and operational facility.

Recovery of manganese and zinc from spent Zn-C and alkaline batteries in acidic medium

The anode and the internal paste of spent Zn-C and alkaline batteries were leached with 2 mol L-1 H2SO4 at 80 ºC for 2 h. Solid/liquid ratio was 1/10 (g mL-1). The leachate was treated with Na2S in order to precipitate Hg, Cd and Pb. Zn was quantitatively isolated at pH 1,5-2 by adding Na2S. Mn can be precipitated at pH close to 7. Na2S may be replaced by oxalic acid. Zn precipitated at pH around 0, whereas Mn was quantitatively recovered at pH > 4. Acidity control is a critical parameter. Na2SO4 and carbon are the end products.

Resposta antioxidante, formação de fitoquelatinas e composição de pigmentos fotoprotetores em Brachiaria decumbens Stapf submetida à contaminação com Cd e Zn

In order to evaluate the response of Brachiaria decumbens Stapf to Cd and Zn, plants were hydroponically exposed to 50 and 100 mmol L-1 of Cd and 500 and 2000 mmol L-1 of Zn. Metal content of shoots and roots was determined, as well as alterations in photosynthetic and photoprotective pigments, antioxidant metabolites and phytochelatin synthesis. Plants concentrated elevated levels of Cd and Zn, especially in roots. Zinc exposure negatively affected chlorophyll and β-carotene content, whereas the highest dose of Cd reduced VAZ cycle pigments and tocopherol levels in plant shoots. Cadmium was the maximum inducer of the phytochelatin synthesis pathway.

Síntese hidrotermal assistida por micro-ondas como metodologia sintética eficiente para obtenção da rede metalorgânica [ZN(BDC)(H2O)2]n

This work presents the optimization of the microwave-assisted hydrothermal synthesis of [Zn(BDC)(H2O)2]n . The reactions were carried out at the fixed temperature of 120 ºC for 10, 20, 30 and 40 min. Pure crystalline [Zn(BDC)(H2O)2]n was obtained in high yield (ca. 90%) with a reaction time of 10 min. The phase obtained and its purity was confirmed by Rietveld refinement, with a final value for Rwp/Rexp equal to 1.48. Increased reaction times (20, 30 and 40 min) favored the formation of unwanted by products, resulting in mixtures of several crystalline phases.

Aplicação de métodos quimiométricos na otimização da extração de Ca, Mg, K, Fe, Zn, Cu e Mn em folhas de braquiária

This work applied a 2² factorial design to the optimization of the extraction of seven elements (calcium, magnesium, potassium, iron, zinc, copper and manganese) in brachiaria leaves, determined by flame atomic absorption spectrometry. The factors sample mass and digestion type were evaluated at two levels: 200/500 mg, and dry/wet, respectively. Principal component analysis allowed simultaneous discrimination of all the significant effects in one biplot. Wet digestion and mass of 200 mg were considered the best conditions. The decrease of 60% in sample mass allowed to save costs and reagents. The method was validated through the estimation of figures of merit.

Ternary surface complex: coadsorption of Cu(II), Zn(II), Cd(II) and nitrilotris(methylenephosphonic) acid onto boehmite

This work studies the effect of NTMP (nitrilotris(methylenephosphonic acid)) on the adsorption of Cu(II), Zn(II), and Cd(II) onto boehmite in the pH range 5-9.5. The data were analyzed using the 2-pK constant capacitance model (CCM) assuming ternary surface complex formation. Under stoichiometric conditions, NTMP is more effective for removing Cu(II) than Zn(II) from solution and the contribution of ternary surface complexes are important to model the adsorption of both metals. Under nonstoichiometric conditions and high surface loading with a Me(II)/NTMP ratio of 1:5, Cu(II) and Zn(II) adsorption is significantly suppressed. In the case of Cd(II) the free metal adsorption is the most dominant species.