Synthesis, Docking Studies and Evaluation of Chalcones as Anti-Helicobacter pylori and antitumoral Agents.

Helicobacter pylori colonizes the gastric epithelium of 50 % of world population and it is the main etiological agent of human chronic gastritis, peptic ulcer, and gastric cancer. In this study, we synthesized and characterized a series of 14 chalcones and evaluated their anti-H. pylori, NO inhibition (in vitro and in silico), and AGS cells cytotoxic effects. Compounds 3b and 3h showed MIC of 8 µg/mL. We observed structure-activity relationships, mainly related to the influence of methoxy substituent at C-2 (3b) and the nitro group at C-4 (3h) in chalcone scaffold. The fourteen chalcones inhibited the NO production in LPS-stimulated macrophages and showed potential for interaction on the active site of the iNOS enzyme. Finally, 3b and 3h showed the highest selectivity to the AGS cell lines. Thus, ours results suggest 3b and 3h as potential candidates for design of new and effective agents against H. pylori and related diseases.

Melatonin promotes orofacial antinociception in adult zebrafish by modulating TRP channels.

Melatonin is an endogenous hormone, known as the sleep hormone, which has already demonstrated its antinociceptive effect. This study aimed to evaluate the participation of TRP's channels in the orofacial antinociceptive effect of melatonin (MT) in adult zebrafish. Initially, the open field test was performed to evaluate the effect of MT on the locomotor activity of adult zebrafish. Then, the animals were pre-treated with MT (0.1, 0.3 or 1 mg/mL; gavage) and acute orofacial nociception was induced by the application of capsaicin (TRPV1 agonist), cinnamaldehyde (TRPA1 agonist) or menthol (TRPM8 agonist) applied into the animal's lip. Naive groups were included. MT, per se, did not alter the locomotor activity of the animals. MT reduced the nociceptive behavior induced by the three agonists; however, the most significant effect was obtained with the lowest concentration tested (0.1 mg/mL) in the capsaicin test. The orofacial antinociceptive effect of melatonin was prevented by capsazepine (TRPV1 antagonist), but not by HC-030031 (TRPA1 antagonist). The molecular docking study indicated interaction between MT and the TRPV1, TRPA1 and TRPM8 channels and, in line with the in vivo results, there was greater affinity between MT and the TRPV1 channel. The results confirm the pharmacological relevance of melatonin as an inhibitor of orofacial nociception and this effect seems to be related to the modulation of TRP's channels.

Assessing Cotton Genotypes for Resistance to Aphis gossypii (Hemiptera: Aphididae).

Aphis gossypii Glover (Hemiptera: Aphididae) is a polyphagous species frequently associated with the presence of sooty mold and viruses lethal to plants. The purpose of this work was to characterize possible resistance categories of cotton genotypes against A. gossypii. Initially, a preliminary test was carried out with 78 genotypes, 15 of which were selected for infestation ability assays and the determination of the cumulative aphid-day rates. Posteriorly, these genotypes were also evaluated through antixenosis and antibiosis assays. The genotypes FM 910, FM 966 LL, Mocó, Gossypium hirsutum var. punctatum L. (Malvaceae), Variedade Reba = BTK-12, Deltapine, Hi-Bred, Acala 4-42, IAC PV010-1664, IAC 21, Reba B-50 PR and FMT 709 inhibited the aphid colonization. In the infestation ability assay, G. hirsutum punctatum, IAC PV010-1664 and Acala 4-42 were the least infested. In a multiple-choice assay, Deltapine Smooth Leaf and Variedade Reba = BTK-12 were significantly less infested, suggesting antixenosis. In the antibiosis assay, Gossypium arboreum L. (Malvaceae) 1 showed the lowest number of nymphs, number of nymphs per adult per day and, number of nymphs at 10 d after the birth of the first nymph in addition to reducing the reproductive period, nymphal survival, adult longevity and, developmental time. In the FM 910, the number of nymphs produced per day and, at 10 d after the birth of the first nymph decreased, which also indicated resistance. The results obtained here are unprecedented and can be explored in breeding programs to develop insect-resistant cotton cultivars.

Histopathologic evaluation of experimental murine neurocysticercosis after treatment with albendazole/nitazoxanide combination.

Neurocysticercosis (NCC) is the most common helminthic brain infection related to epilepsy. Only albendazole (ABZ) and praziquantel are used in its treatment. The development of new therapeutics has been encouraged. Taenia crassiceps cysticerci intracranial infection is the experimental model used in NCC studies. This study evaluated the histopathology of the brains of BALB/c mice experimentally infected with T. crassiceps cysticerci after the treatment with the ABZ/nitazoxanide (NTZ) combination. Thirty days after the inoculation the mice received an oral single dose of the ABZ/NTZ combination (40 mg kg-1 each). The control groups were treated with: NaCl 0.9%; ABZ or NTZ. The histopathologic evaluation of the brains was performed 24 h after treatment. The ABZ treatment induced discrete mononuclear inflammatory infiltration, meningitis, gliosis, hyperaemia and hippocampus compression; moderate ependimitis and oedema. The NTZ treatment induced accentuated inflammatory infiltration, foamy macrophages, ependimitis, choroiditis, gliosis and hyperaemia and moderate oedema. The ABZ/NTZ combination treatment induced a significant decrease in the polymorphonuclear inflammatory infiltration, ependimitis, choroiditis, gliosis, hyperaemia and ventriculomegaly in comparison with the other groups. The cysticerci showed destruction of the tegument not observed in other groups. The ABZ/NTZ combination is efficient as the parasite showed signs of destruction and lower damage to the host's tissue.

Photodynamic Therapy With Propolis: Antibacterial Effects on Staphylococcus aureus, Streptococcus mutans and Escherichia coli Analysed by Atomic Force Microscopy.

Introduction: Photodynamic therapy (PDT) is a process that uses a light source (e.g. laser), oxygen molecules and a photosensitizing agent. PDT aims to act against pathogens, including those resistant to antimicrobials. The association of PDT with natural drugs, such as Propolis, has not been widely studied. Methods: Therefore, this study aimed to evaluate the antimicrobial effect of PDT in vitro by using Propolis as a photosensitizing agent. For this purpose, the dry Propolis extract was used as a photosensitizer and a low-power laser (Photon Laser III model) was irradiated onto the microwells for 90 seconds. Gram-positive and Gram-negative bacterial strains were used in the tests at a concentration of 5 × 105 CFU/mL. Initially, the antibacterial activity of the photosensitizers without laser action was determined by using a serial microdilution method before the experiment with a laser. After the incubation of the plates in a bacteriological oven, resazurin (0.1%) was added and the minimum inhibitory concentration (MIC) was determined. Alterations in the morphology of the bacteria were analysed by using atomic force microscopy (AFM). Results: Bacteria were sensitive to Propolis with MICs ranging from 13.75 to 0.85 mg/mL, but no susceptibility was observed for methylene blue without laser application. A change was observed for MIC values of Propolis against Staphylococcus aureus after irradiation, which decreased from 1.71 mg/mL to 0.85 mg/mL. However, this behaviour was not observed in Escherichia coli, the only gram-negative strain used. In addition, AFM images revealed alterations in the size of one of the bacteria tested. Conclusion: The Propolis is more active against gram-positive bacteria and PDT improved its activity against one of the strains tested.

Um infusor autônomo para um expansor de pele subcutâneo / An autonomous infuser for a subcutaneous skin expander

Introdução: A expansão da pele é um processo fisiológico definido como a capacidade de aumentar sua área superficial em resposta a uma tensão ou a uma dada deformação. Para realizar a cirurgia reconstrutiva, os expansores de pele são implantados sob a pele e periodicamente infiltrados com uma solução salina para fornecer um retalho extra de pele. Quando o volume interno prescrito do expansor é alcançado, a cirurgia reconstrutiva é realizada. Métodos: Foi desenvolvido um dispositivo semiautomático e portátil para facilitar um procedimento de expansão da pele. O dispositivo tem como objetivo simplificar o processo de infiltração, proporcionando mobilidade e independência para o paciente, e assegurando ao médico a qualidade e a precisão das infiltrações realizadas. O dispositivo também permite expansão contínua em pacientes hospitalizados. Resultados: Usando um código, o médico tem acesso ao menu do dispositivo e define a pressão máxima e/ou o valor máximo para cada expansor do paciente. O paciente pode realizar a infiltração e ter acesso ao controle da velocidade de infiltração, reverter ou parar a operação. Todos os dados são gravados em um SIM Card e incluem data, hora, volumes inicial e final, e pressão inicial e final de cada procedimento para cada expansor. Conclusões: O dispositivo automatiza e otimiza a expansão, de modo que o que o médico possa prescrever um limite para cada expansão, seja uma pressão máxima ou voluma infiltrado. Todos os dados são gravados, fornecendo um importante banco de dados sobre o comportamento de pele relacionado a gênero, raça, idade e local da expansão.

Introduction: Skin expansion is a physiological process defined as the ability of human skin to increase its superficial area in response to a stress or given deformation. In reconstructive surgery, skin expanders are implanted beneath the skin and periodically infiltrated with a saline solution to provide an extra flap of skin. When the prescribed internal volume of the expander is reached, reconstructive surgery is performed. Methods: A semiautomatic and portable device was developed and built to facilitate a skin expansion procedure. The device aims to simplify the infiltration process, providing mobility and independence to the patient and assuring the physician of the infiltration quality and precision. The device also enables continuous expansion in hospitalized patients. Results: Using a code, the doctor accesses the menu of the device and sets the maximum pressure and/or value for each expander of the patient. The patient can control the infiltration velocity and reverse or stop the operation. All data are recorded on a simcard and include date, time, initial and final volumes, and initial and final pressures of each procedure for each expander. Conclusions: The device motorizes and optimizes the expansion, allowing the doctor to prescribe a maximum infiltration pressure or volume. All data are recorded to provide an important database of skin behavior related to sex, race, age, and expansion site.

Effects of polyethylene film wrap on cooler shrink and the microbial status of beef carcasses.

The present study evaluated the use of polyethylene film wrapping of beef half carcasses and its effects on cooler shrink, cooling characteristics and microbial status of the half carcasses. Film wrapping reduced cooler shrink by 55.2%, 43.1%, 36.0% and 30% after 24, 48, 72 and 96 h of cooling, respectively, compared to the unwrapped half carcasses, whereas the surface water activity showed no significant differences among the time periods. The wrapped half carcasses had a lower cooling rate and higher surface and internal temperatures. The highest values of the aerobic mesophiles, Staphylococcus aureus and Enterobacteriaceae were found in the half carcasses wrapped in film. No significant differences were found in the values of Escherichia coli. The polyethylene film was effective in reducing cooler shrink; however, it caused a delay in cooling, thereby enabling greater microbial occurrences and counts and impairing the hygienic and sanitary conditions of the carcasses, which may be an impediment to the practical application of this technology.

Larval development of Physocephala (Diptera, Conopidae) in the bumble bee Bombus morio (Hymenoptera, Apidae)

Larval development of Physocephala (Diptera, Conopidae) in the bumble bee Bombus morio (Hymenoptera, Apidae). In the summer of 2012, a high incidence of conopid larvae was observed in a sample of female B. morio collected in remaining fragments of semidecidual forest and Cerrado, in the municipality of Sorocaba, state of São Paulo, Brazil. The larval development of conopid flies was studied, beginning at the larval instars (LO to L3) and PUP, until the emergence of the imago under laboratory conditions and inside the host. At the first instar, or LO, the microtype larvae measured less than 1 mm in length. During the transition from L1 to L3, the larvae grew in length. At L3, the larvae doubled their length (4 mm) and then started to develop both in length and width, reaching the PUP stage with 10 mm in length and 7 mm in width. The main characteristic that differentiates L3 from the early instars is the larger body size and the beginning of posterior spiracle development. The development from PUP to puparium took less than 24h. The bees died ten days after the fly oviposition, or just before full PUP development. The early development stages (egg-LO to L1) were critical for larva survival. The pupa was visible between the intersegmental sternites and, 32 days after pupation, a female imago of Physocephala sp. emerged from one bee. The puparium and the fly measured approximately 10 mm in length. In a single day of collection, up to 45% of the bumble bees collected were parasitized by conopid flies.

Incidencia das lesoes traumaticas agudas na escolinha de Futebol do Gremio Futebol Portoalegrense / Incidence of acute traumatic injuries at Gremio Football PortoAlegrense Soccer School

O comprometimento traumatico agudo do sistema locomotor causa tanto dor, como limitacao de movimentos e, muitas vezes, incapacidade parcial ou total do atleta. Neste cenario as complicacoes como: deformidades, rigidez articular e atrofias musculares sao muito frequentes. O diagnostico precoce e a abordagem terapeutica adequadas sao fundamentais para recuperacao total da funcao do segmento lesado. Foram acompanhados 150 atletas infantis da Escolinha de Futebol do Gremio Football Portoalegrense (EFGFP), com idade entre 10 e 15 anos, do sexo masculino, no periodo de marco a dezembro de 1992, e registradas as lesoes traumaticas agudas apresentadas por estes atletas, periodo de afastamento ate recuperacao total e evento onde sofreram estas lesoes