Cancer treatment represents one of the main scientific study targets today, mainly due to the pronounced side effects arising from chemotherapy. This study reports the synthesis, characterization, and anticancer activity of ten compounds from the Morita-Baylis-Hillman reaction. Ethylene glycol diacrylate was used as a double Michael acceptor in reactions with isatin derivatives to give homodimers of 3-hydroxyindolin-2-one core, recognized in the literature for its extensive pharmacological profile. The use of 1,4-diazabicyclo[2,2,2]octane (DABCO) as a catalyst and room temperature were the optimal conditions for the study reaction. The isolated yields were up to 63%, with most reaction times inferior to 24 h, some as fast as 15 min. The anticancer potential of the synthesized dimers was evaluated in vitro against three cancer strains, resulting in average inhibitory concentrations up to 0.72 µM. It was also found that the best performing homodimers are more active than their monomeric counterparts. Considering the promising selectivity indices observed, the preliminary results obtained here act as a basis for broader tests regarding the effectiveness of homodimeric adducts against cancer cells.

This investigation describes the synthesis of eugenol analogs presenting 1,2,3-triazole fragments and evaluation of their antileishmanial activity. The alkylation of guaiacol (1) with allyl bromide afforded 1-(allyloxy)-2-methoxybenzene (2) (93% yield). The Claisen rearrangement conducted with 1 gave ortho eugenol (3) (82% yield). Alkylation procedures performed with 3 produced 1-allyl-3-methoxy-2-(prop-2-yn-1-yloxy)benzene (4) (73% yield) and 1-allyl-3-methoxy-2-(pent-4-yn-1-yloxy)benzene (6) (53% yield). The copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) reactions involving alkynes 4 and 6 with different benzylic azides afforded twenty-two eugenol analogs with 1,2,3-triazole functionalities (48-93% yield). We screened the compounds at 10 μmol L 1 against Leishmania braziliensis intracellular amastigotes during macrophage infection. The action of these compounds was compared with the known leishmanicidal drug amphotericin B. None of the analogs were toxic to macrophages at 10 μmol L-1. The cytotoxic concentration at 50% (CC50), effective concentration at 50% (EC50), and selectivity index (SI) were determined to the best compounds 4-((2-allyl-6-methoxy)phenoxymethyl)-1-(4-chlorobenzyl)-1 H-1,2,3-triazole (8c) and 4-((2-allyl-6-methoxy)phenoxymethyl)-1-(4-trifluoromethoxybenzyl)-1 H-1,2,3-triazole (8h). They showed a significant leishmanicidal effect, with EC50 of 28.09 µmol L-1 (8c) and 52.03 µmol L-1 (8h). The SIs were 9.7 for 8c and > 5.7 for 8h. These compounds have the potential as new leishmanicidal agents against L. braziliensis and may represent a starting point for the development of alternative treatments for cutaneous leishmaniasis.

ABSTRACT The quantification of torques and moments of inertia for horizontal axis hydrokinetic turbine driveline is important to precisely predict the dynamic behavior of the complete system. Initially, this paper presents different models used in the literature for describing torques and moments of inertia of turbine components. A dynamic model of a small hydrokinetic turbine using belt transmission is developed. The model uses the Blade Element Momentum (BEM) for determining the power coefficient of the turbine rotor. It considers the inertial effects and dissipative torques of the whole system. The results of the turbine dynamical behavior are compared with experimental data, showing good agreement. In order to numerically analyze a more efficient drivetrain, the belt transmission is replaced by a planetary gearbox in the model, and the new results are also assessed. It was found that with planetary gears, a more compact transmission can be used, reducing the inertial effects, bringing a better performance to the machine starting, shortening the transient regime time. system Initially components developed BEM (BEM rotor data agreement drivetrain assessed gears starting time

Resumen Desde mediados de la década del 2000, el mantenimiento del régimen macroeconómico ortodoxo de los gobiernos de Lula sorprendió a varios intelectuales del sector de las ciencias sociales aplicadas. Lo que marca al gobierno de Lula, especial- mente, son dos características: i) el crecimiento económico con el boom de los commodities o el súper ciclo de las commodities, y ii) la lucha contra la pobreza. Este segundo fenómeno propició que un grupo de intelectuales formulara la tesis de que Brasil estaría en un proceso de “desarrollismo social”. Por otro lado, una fracción de economistas se reunió para formular una nueva teoría, el “nuevo desarrollismo”, criticando el proceso de desindustrialización, crisis de deuda y dependencia externa que ocurrió en Brasil. Estas dos corrientes teóricas formaron lo que algunos académicos llamaron “neo-desarrollismo”. Este artículo propone hacer una reflexión crítica y diferenciación sobre las dos corrientes.

Abstract Since the mid-2000s, the maintenance of the orthodox macroeconomic regime of the Lula’s governments surprised several intellectuals in the applied social sciences sector. What marks Lula’s government, especially, are two characteristics: i) the economic growth with the commodities boom or the commodities super cycle, and ii) the fight against poverty. This second phenomenon propitiated for a group of intellectuals to formulate the thesis that Brazil would be in a process of “social developmentalism”. On the other hand, a fraction of economists met to formulate a new theory, the “new developmentalism”, criticizing the process of de-industrialization, debt crisis and external dependence that occurred in Brazil. These two theoretical currents formed what some academics called “neo-developmentalism”. This article proposes to make a critical reflection and differentiation on the two currents.

ABSTRACT Scarabeoidea (Insecta: Coleoptera) present more than 2000 species recorded from all over Brazil. They have been scarcely recorded from caves, and truly troglobitic species are yet to be found in the country. In this study, we carried out a review of all existing scarab beetles deposited until 2017 in the Coleção de Invertebrados Subterrâneos de Lavras (ISLA), at the Universidade Federal de Lavras (UFLA) (Minas Gerais, Brazil), one of the most important collections of subterranean invertebrates in South America. Ninety-two individuals belonging to 52 species were recorded, distributed in six families (Cetoniidae, Hybosoridae, Melolonthidae, Passalidae, Scarabaeidae and Trogidae). Scarabaeidae was the most diverse of them, representing more than 50% of the total of species recorded. We found Scarabeoidea beetles in 51 of the ~ 1600 caves examined, distributed in nine Brazilian states: Alagoas, Bahia, Distrito Federal, Espírito Santo, Goiás, Minas Gerais, Pará, Piauí, and Tocantins. Our results provide evidence that Scarabaeoidea beetles are not frequent in Brazilian caves, and their records in this kind of environment are mostly accidental. Exceptions include Trogidae and Aphodiinae species, which may be associated with bat guano. Our study presents the first list of Scarabaeoidea species sampled in Brazilian caves.

Morita-Baylis-Hillman adducts (MBHA) is a class of polyfunctional molecules that has been standing out due to their versatility and expressive biological activities. Therefore, this paper describes the synthesis and antiproliferative activity of some new MBHA/7-choroquinoline hybrids. The Michael acceptors were obtained starting from 4,7-dichloroquinoline which were submitted to the Morita-Baylis-Hillman reaction with ortho, meta and para-nitrobenzaldehyde. The in vitro screening of the synthetized MBHA against NCI-H292, HCT-116 and MCF-7 cancer cells suggests the influence of the spacer chain in its inhibition potential. The 50% inhibitory concentration (IC50) obtained in the antiproliferative assay using MCF-7, HCT-116, HL-60 and NCI-H292 cancer cells indicate expressive cytotoxic potential of the adducts containing nitro group in the ortho position, with IC50 of 4.60 µmol L-1. MBHA/7-choroquinoline hybrids were more active than MBHA described in literature, indicating the improvement of the cytotoxic effect due to 7-chloroquinoline moiety in the molecular structure, with maximum selectivity index values of 11.89.

BACKGROUND: The burden of HIV is especially concerning for Eastern and Southern Africa (ESA), as despite expansion of test-and-treat programmes, this region continues to experience significant challenges resulting from high rates of morbidity, mortality and new infections. Hard-won lessons from programmes on the ground in ESA should be sharedOBJECTIVES: This report summarises relevant evidence and regional experts' recommendations regarding challenges specific to ESAMETHOD: This commentary includes an in-depth review of relevant literature, progress against global goals and consensus opinion from expertsRESULTS: Recommendations include priorities for essential research (surveillance data collection, key and vulnerable population education and testing, in-country testing trials and evidence-based support services to improve retention in care) as well as research that can accelerate progress towards the prevention of new infections and achieving ambitious global goals in ESACONCLUSION: The elimination of HIV in ESA will require continued investment, commitment to evidence-based programmes and persistence. Local research is critical to ensuring that responses in ESA are targeted, efficient and evaluated

A exposição excessiva à radiação solar (RS) é o principal causador do câncer de pele. O objetivo desse trabalho foi investigar a percepção de estudantes do ensino médio sobre RS e suas implicações à saúde humana. Os dados foram coletados através de questionários e as respostas foram avaliadas por tabelas de frequências relativa, absoluta e percentual. Devido ao tamanho da amostra, utilizamos o teste de Fisher a 5% de significância (e hipótese alternativa bilateral) para correlacionar as respostas. Os alunos, independente de terem estudado ou não sobre RS não sabem definir RS e não têm percepção sobre os efeitos da RS à saúde humana. Este diagnóstico mostra, por um lado, a carência conceitual dos estudantes. Por outro, ele sugere também a ineficácia dos recursos didáticos convencionais e meios de informação acessíveis. Portanto, a inserção deste conceito na educação básica é primordial dada sua relevância social e por se tratar de um problema de saúde pública.

The excessive exposure to solar radiation (SR) is the main cause of skin cancer. The main aim of this paper was to investigate the perception of high school students about the SR and its implications for human health. The data have been collected through questions and the answers were evaluated by tables of relative, absolute and percentual frequency. Due to the size of our sample, we have used the Fischer test at 5% of significance (and bilateral alternative hypothesis) to correlate the answers. The students, whether they studied or not SR, don’t know to define SR and don’t have perception about its effects on the human health. This diagnosis shows, on the one hand, the conceptual lack of students. On the other, it also suggests the ineffectiveness of conventional didactic resources and accessible information media. Thus, the insertion of this concept in basic education is essential due to its social relevance and because it’s a public health problem.

Resumo Pouco se sabe se a morte celular induzida pela terapia fotodinâmica (PDT) compromete os macrófagos (MΦ), envolvidos nas respostas imunes induzidas pela PDT. Neste estudo, foram avaliados parâmetros de citotoxicidade dos MΦ mediada pela PDT e a produção de citocinas, frente à protoporfirina IX (PpIX). MΦ peritoneais de camundongos BALB/c foram estimulados in vitro com PDT, luz, PpIX ou lipopolissacarídeo (LPS). Após isto, a viabilidade celular (VC), a lipoperoxidação, os níveis de óxido nítrico (NO), de DNA degradado, de TNF-α, IL-6 e IL-10 foram avaliados. A exposição curta à PDT reduziu a VC em 10-30%. Os níveis de NO e de DNA degradado duplicaram, sem aumento da lipoperoxidação. Houve aumento de TNF-α e IL-10, sendo maior na presença de LPS. Já a produção de IL-6 reduziu em dez vezes. A PDT induz estresse celular, gera radicais NO e causa dano ao DNA, tornando o microambiente citotóxico. Ainda, modula citocinas pró e anti-inflamatórias em MΦ.

Abstract Little is known regarding whether photodynamic therapy (PDT)-induced cell death can substantially compromise macrophages (MΦ), which are important cells in PDT-induced immune responses. Here, parameters of PDT-mediated MΦ cytotoxicity and cytokine production in response to protoporphyrin IX (PpIX) were evaluated. Peritoneal MΦ from BALB/c mice were stimulated in vitro with PDT, light, PpIX, or lipopolysaccharide (LPS). After that, cell viability, lipid peroxidation, Nitric Oxide (NO), DNA damage, TNF-α, IL-6 and IL-10 were evaluated. Short PDT exposure reduced cell viability by 10–30%. There was a two-fold increase in NO and DNA degradation, despite the non-increase in lipoperoxidation. PDT increased TNF-α and IL-10, particularly in the presence of LPS, and decreased the production of IL-6 to 10-fold. PDT causes cellular stress, induces NO radicals and leads to DNA degradation, generating a cytotoxic microenvironment. Furthermore, PDT modulates pro- and anti-inflammatory cytokines in MΦ.

Wax deposit is of a great concern in the petroleum industry and causes partial or total blockage of the pipelines. In this work, four Brazilian crude oils (P1-P4) and five inhibitors solutions (I1-I5) were used associating rheology results to understand, at a molecular level, the characteristics of the saturated fractions by high-resolution mass spectrometry (Orbitrap coupled to atmospheric pressure chemical ionization (APCI) source) and two-dimensional gas chromatography coupled to mass spectrometry (GC × GC-MS). The effectiveness of wax inhibitors can be demonstrated by the viscosity decrement. The characterization of the saturated fractions by GC × GC-MS and high resolution mass spectrometry showed that is possible to conclude that inhibitor I1 favored the inhibition process of paraffins when oils have a smaller and monocyclic saturated chain hydrocarbon (HC) profiles, whereas for oils with larger amounts of polycyclic chain HCs, the inhibitor I4 appeared to be the alternative.

Paper spray ionization (PSI) is a promising analytical tool for direct analysis in mass spectrometry (MS). However, this technique usually uses chromatographic paper, which rarely accomplishes a stable MS signal and could vary with the sample matrix effect. In the present study, the application of graphene oxides (GO) was scrutinized as modifier paper substrate for PSI-MS methods. The developed substrate efficiency was evaluated towards creatinine determination in urine samples. The GO-PSI-MS developed method for creatinine in urine samples showed linearity in the range of 0.1 to 3.4 ppm with R2 = 0.9991. The precision was evaluated and the values were between 1.1 to 6.8% and the accuracy above 96.8%. The limit of quantification (LOQ) and limit of detection (LOD) were 0.05 and 0.17 ppm, respectively. The GO-PSI developed was compared to conventional chromatographic paper for PSI-MS methods, and the results showed that the modified paper with GO bolsters method linearity, precision, and LOQ values.

The Cannabis sativa L. plant has a complex chemical composition, containing various chemical compounds such as terpenes, sugars, hydrocarbons, steroids, flavonoids, and amino acids. Few works have attempted to identify the constitutional isomers of cannabinoids that are found in the plant. The present study reported the analysis of seven cannabinoid standards: five neutral and two acidic, as well as Cannabis products (hashish and marijuana) and parts of the Cannabis plant (flower and leaf) using mono-dimensional gas chromatography coupled with mass spectrometry (GC-MS) and two-dimensional gas chromatography coupled with quadrupole MS (GC × GC-QMS), ultra performance liquid chromatography coupled with electrospray ionization-quadrupole-time of flight (UPLC-ESI-QTOF)-MS and UPLC-ESI-travelling wave ion mobility (TWIM)-MS. The results of GC-MS demonstrated close retention times (∆tR = 1.303 min) in separation of the five cannabinoid standards, whereas GC × GC-QMS provided a substantially better identification and distinction of constitutional isomers of cannabinoids, where a total of 11 cannabinoids were identified in the hashish sample. UPLC-QTOF-MS and UPLC-TWIM-MS data obtained complete chemical information, in which ESI(+) revealed the presence of seven constitutional isomers of ∆9-tetrahydrocannabinol (∆9-THC), whereas ESI(-) proved the presence of four isomers of ∆9-tetrahydrocannabinolic acid A (∆9-THCA A).

Resumo Neste trabalho, avaliamos a descoloração de efluentes têxteis durante seu tratamento em um sistema de fermentação em estado sólido (SSF). Os ensaios foram conduzidos com resíduo de pupunha (Bactris gasipaes) utilizando o fungo de podridão branca Ganoderma lucidum EF 31. A influência da concentração de corante, as quantidades de resíduo e da fase líquida foram estudadas tanto na eficiência de descoloração como na produção de enzima. De acordo com os resultados, independentemente das condições experimentais utilizadas, a lacase foi a principal enzima ligninolítica produzida por G. lucidum. A atividade de lacase mais elevada foi obtida em baixas concentrações de efluentes, sugerindo um efeito inibitório no metabolismo fúngico. A maior remoção de cor foi obtida com 10 gramas de resíduo da pupunha e 60 mL do efluente final. Nos ensaios de controle realizados com o corante sintético RBBR, foram atingidos cerca de 20% mais descoloração do que os obtidos com o efluente industrial. A adsorção de RBBR no resíduo de pupunha também foi investigada. Os testes de equilíbrio mostraram que a adsorção deste corante seguiu as isotermas de Langmuir e Freundlich. Assim, os resultados experimentais indicam que o resíduo de pupunha é um substrato adequado tanto para a produção de lacase quanto para a remoção de cor em efluentes industriais.

Abstract In this work we have assessed the decolorization of textile effluents throughout their treatment in a solid-state fermentation (SSF) system. SSF assays were conducted with peach-palm (Bactris gasipaes) residue using the white rot fungus Ganoderma lucidum EF 31. The influence of the dye concentration and of the amounts of peach-palm residue and liquid phase on both the discoloration efficiency and enzyme production was studied. According to our results, independently of experimental conditions employed, laccase was the main ligninolytic enzyme produced by G. lucidum. The highest laccase activity was obtained at very low effluent concentrations, suggesting the existence of an inhibitory effect of higher concentrations on fungal metabolism. The highest percentage of color removal was reached when 10 grams of peach palm residue was moistened with 60 mL of the final effluent. In control tests carried out with the synthetic dye Remazol Brilliant Blue R (RBBR) decolorization efficiencies about 20% higher than that achieved with the industrial effluent were achieved. The adsorption of RBBR on peach-palm residue was also investigated. Equilibrium tests showed that the adsorption of this dye followed both Langmuir and Freundlich isotherms. Hence, our experimental results indicate that peach-palm residue is suitable substrate for both laccase production and color removal in industrial effluents.

ABSTRACT The red-tailed Amazon parrot (Amazona brasiliensis) is a threatened species of psittacine bird that inhabit coastal regions of Brazil. In view of the threat of this species, the aim of this study was to perform a health evaluation in wild nestlings in Rasa Island, determining the prevalence of enterobacteria and infectious agents according to type of nest. Blood samples were collected from 64 birds and evaluated for antibodies of Chlamydia psittaci by commercial dot-blot ELISA. Cloacal and oropharyngeal swabs samples were collected from 23 birds from artificial wooden nests, 15 birds from PVC nests and 2 birds from natural nests for microbiological analysis. Swab samples were collected from 58 parrots for C. psittaci detection by PCR and from 50 nestlings for Avian Influenza, Newcastle Disease and West Nile viruses’ detection analysis by real-time RT-PCR. Ten bacterial genera and 17 species were identified, and the most prevalent were Escherichia coli and Klebsiella oxytoca. There was no influence of the type of nest in the nestlings’ microbiota. All samples tested by ELISA and PCR were negative. There is currently insufficient information available about the health of A. brasiliensis and data of this study provide a reference point for future evaluations and aid in conservation plans.

Resumo Este trabalho apresenta estudo sobre o comportamento de vigas de concreto armado reforçadas à flexão, pela adição de concreto e barras de aço na região tracionada e chumbadores de expansão na ligação viga-reforço, submetidas a carregamento cíclico. O programa experimental incluiu ensaios em seis vigas de concreto armado em escala real, simplesmente apoiadas, inicialmente com seção transversal retangular com 150 mm de largura e 400 mm de altura, comprimento entre os apoios de 4000 mm e comprimento total de 4500 mm. Todas as vigas, depois de receber dois ciclos de carga estática, de modo a criar uma condição de pré-fissuração, foram reforçadas à flexão por encamisamento parcial e, em seguida, submetidas a uma carga cíclica até ao final de 2x106 ciclos ou da ocorrência de ruptura por fadiga. Após a aplicação das cargas cíclicas, as vigas que não romperam por fadiga foram submetidas a uma carga estática até a ruptura. As principais variáveis foram a condição de interface de ligação entre viga e reforço (lisa ou rugosa), a taxa de armadura de flexão na viga e no reforço, e amplitude do carregamento cíclico. Com base nos resultados obtidos nos ensaios e em estudos anteriores de vigas semelhantes testadas apenas com carga estática, é feita uma discussão do comportamento dessas vigas reforçadas e apresentada uma proposta para dimensionamento da ligação viga-reforço, para os casos de carregamento predominantemente estático e cíclico.

Abstract This work presents a study on the behavior of reinforced concrete beams strengthened in bending by the addition of concrete and steel on their tension side and having expansion bolts as shear connectors at the junction between the beam and the jacket, subjected to a cyclic loading. The experimental program included tests on six full scale reinforced concrete beams, simply supported, initially with rectangular cross section 150 mm wide and 400 mm high, span of 4000 mm and total length of 4500 mm. All the beams, after receiving two cycles of static loading in order to create a pre-cracking condition, were strengthened in bending by partial jacketing and then subjected to cyclic loading until the completion of 2x106 cycles or the occurrence of fatigue failure. Following the cyclic loading, the beams that did not fail by fatigue were subjected to a static load up to failure. The main variables were the beam-jacket interface condition (smooth or rough), the flexural reinforcement ratio in the beam and in the jacket, and cyclic load amplitude. On the basis of the obtained test results and the results of previous studies of similar beams tested only under static loading, the behavior of the strengthened beams is discussed and a proposal for the beam-jacket connection design is presented, for the cases of predominantly static and cyclic loading.