Convolutamydine A and synthetic analogues have antinociceptive properties in mice

AbstractConvolutamydine A, an oxindole that originated from a marine bryozoan, has several biological effects. In this study, we aimed to investigate the antinociceptive effects of convolutamydine A and two new synthetic analogues.Convolutamydine A and the two analogues were given orally to assess their ability to induce antinociceptive effects. Formalin-induced licking response, acetic acid-induced contortions, and hot plate models were used to characterize the effects of convolutamydine A and its analogues.Convolutamydine A (4,6-bromo-3-(2-oxopropyl)-3-hydroxy-2-oxindole), compound 1 (3-(2-oxopropyl)-3-hydroxy-2-oxindole), and compound 2 (5-bromo-3-(2-oxopropyl)-3-hydroxy-2-oxindole) caused peripheral antinociceptive and anti-inflammatory effects in the acetic acid-induced contortions and the formalin-induced licking models. Supraspinal effects were also observed in the hot plate model and were similar to those obtained with morphine. The peripheral effects were not mediated by the cholinergic or opioid systems. The antinociceptive effects of convolutamydine A seem to be mediated by all three systems (cholinergic, opioid, and nitric oxide systems), and the mechanism of action of compounds 1 and 2 involved cholinergic and nitric oxide-mediated mechanisms. Convolutamydine A and its analogues (compounds 1 and 2) showed good antinociceptive ability after systemic administration in acute pain models. The antinociceptive action mediated by cholinergic, opioid, and nitric oxide systems could explain why convolutamydine A, compound 1, and compound 2 retained their antinociceptive effects. The doses used were similar to the doses of morphine and were much lower than that of acetylsalicylic acid, the classical analgesic and anti-inflammatory drug.In conclusion, convolutamydine A and the two analogues demonstrated antinociceptive effects comparable to morphine's effects

Study of ph effect on AZ31 magnesium alloy corrosion for using in temporary implants

Currently, magnesium alloys are gaining great interest for medical applications due to their degrading properties in the human body ensuring a great biocompatibility. These alloys also provide profitable mechanical properties due similarities with human bone.  However, a difficulty in applying these materials in the biomaterials industries is the corrosion prior to cell healing. The effect of the chemical composition of Mg alloys on their corrosion behavior is well known. In this study, samples of AZ31 magnesium alloy were cut into chips for elemental chemical analysis by neutron activation analysis (NAA). Concentrations of the elements As, La, Mg, Mn, Na, Sb and Zn were determined in the AZ31 alloy. Visualization tests of agar corrosion development in various media, of 0.90% sodium chloride solution (mass), phosphate buffer saline (PBS) and simulated body fluid (SBF) were performed. Visualizations of the effect of agar gel corrosion revealed pH variation during the corrosion process due to the released into the cathode. The highest released of hydroxyl ions occurred in NaCl solution compared to PBS and SBF solutions indicating that NaCl solution was much more aggressive to the alloy compared to the others

A study on corrosion resistance of ISO 5832-1 austenitic stainless steel used as orthopedic implant

The ISO 5832-1 austenitic stainless steel used as biomaterial is largely applied in the area of orthopedics, especially in the manufacture of implants, such as temporary or permanent replacement of bone structures. The objective of this study was to evaluate the localized corrosion resistance of the ISO 5832-1 stainless steel used in orthopedic implants by electrochemical tests in two different solutions. The results of this study are of great interest to evaluate the corrosion of metallic implants that can result in the release of corrosion products into bodily fluids causing possible adverse biological reactions. The determination of the chemical elements in the composition of the ISO 5832-1 stainless steel was performed by neutron activation analysis (NAA). The samples for electrochemical tests were grinded with silicon carbide paper up to #4000 finishing, followed by mechanical polishing with diamond paste. The open circuit potential measurements and anodic polarization curves were obtained in solution of 0.90 wt. % of NaCl and of simulated body fluid (SBF). The results indicated that the ISO 5832-1 stainless steel presented a high resistance to crevice corrosion in simulated body fluid solution but high susceptibility to this form of corrosion in the chloride solution. &nbsp

Synthesis of ferrocenyl oxindole compounds with potential anticancer activity

A series of ferrocenyl oxindoles with potential anticancer activity were prepared from the reactions of substituted oxindoles and ferrocenylcarboxyaldehyde in the presence of KOH as catalyst. The products were characterized by spectral data including ¹H and 13C NMR, IR and mass spectrometry. The E and Z configurations were established by nOe or NOESY experiments

Glutamine and cystine-enriched diets modulate aquaporins gene expression in the small intestine of piglets

Research Areas: Science & Technology ; Other TopicsABSTRACT - The regulation of glycerol permeability in the gastrointestinal tract is crucial to control fat deposition, lipolysis and gluconeogenesis. Knowing that the amino acid glutamine is a physiological regulator of gluconeogenesis, whereas cystine promotes adiposity, herein we investigated the effects of dietary supplementation with glutamine and cystine on the serum biochemical parameters of piglets fed on amino acid-enriched diets, as well as on the transcriptional profile of membrane water and glycerol channels aquaporins (AQPs) in the ileum portion of the small intestine and its impact on intestinal permeability. Twenty male piglets with an initial body weight of 8.8 ± 0.89 kg were allocated to four dietary treatments (n = 5) and received, during a four week-period, a basal diet without supplementation (control) or supplemented with 8 kg/ton of glutamine (Gln), cystine (Cys) or the combination of the two amino acids in equal proportions (Gln + Cys). Most biochemical parameters were found improved in piglets fed Gln and Cys diet. mRNA levels of AQP3 were found predominant over the others. Both amino acids, individually or combined, were responsible for a consistent downregulation of AQP1, AQP7 and AQP10, without impacting on water permeability. Conversely, Cys enriched diet upregulated AQP3 enhancing basolateral membranes glycerol permeability and downregulating glycerol kinase (GK) of intestinal cells. Altogether, our data reveal that amino acids dietary supplementation can modulate intestinal AQPs expression and unveil AQP3 as a promising target for adipogenesis regulation.info:eu-repo/semantics/publishedVersio

Evaluation of Ar, Ar-v7, and P160 Family as Biomarkers for Prostate Cancer: Insights Into the Clinical Significance and Disease Progression

PURPOSE: To assess the role of the p160 family, AR, and AR-V7 in different initial presentations of prostate cancer and their association with clinical endpoints related to tumor progression. METHODS: The study sample comprises 155 patients who underwent radical prostatectomy and 11 healthy peripheral zone biopsies as the control group. Gene expression was quantified by qPCR from the tissue specimens. The statistical analysis investigated correlations between gene expression levels, associations with disease presence, and clinicopathological features. Additionally, ROC curves were applied for distinct PCa presentations, and time-to-event analysis was used for clinical endpoints. RESULTS: The AR-V7 diagnostic performance for any PCa yielded an AUC of 0.77 (p \u3c 0.05). For locally advanced PCa, the AR-V7 AUC was 0.65 (p \u3c 0.05). Moreover, the metastasis group had a higher expression of SRC-1 than the non-metastatic group (p \u3c 0.05), showing a shorter time to metastasis in the over-expressed group (p = 0.005). Patients with disease recurrence had super-expression of AR levels (p \u3c 0.0005), with a shorter time-to-recurrence in the super-expression group (p \u3c 0.0001). CONCLUSION: Upregulation of SRC-1 indicates a higher risk of progression to metastatic disease in a shorter period, which warrants further research to be applied as a clinical tool. Additionally, AR may be used as a predictor for PCa recurrence. Furthermore, AR-V7 may be helpful as a diagnostic tool for PCa and locally advanced cancer, comparable with other investigated tools

Fatores associados à infecção pelo uso do cateter central de inserção periférica em Unidade de Terapia Intensiva Neonatal

Estudo epidemiológico, longitudinal e analítico, desenvolvido em um hospital de Minas Gerais, com o objetivo de analisar os fatores associados à infecção pelo uso do cateter central de inserção periférica em recém-nascidos internados em unidade de terapia intensiva. A coleta dos dados foi realizada por meio de uma ficha estruturada, preenchida pelos profissionais e verificada pelos pesquisadores. Foram estudados 291 cateteres inseridos em 233 recém-nascidos. Os fatores associados à retirada por suspeita de infecção foram: prematuridade, peso ao nascer até 1.500 gramas, cateter de poliuretano, localização não centralizada do cateter e tempo de uso superior a 30 dias. Após ajuste multivariado, permaneceram independentemente associados: peso inferior a 2.500 gramas na inserção, reparo e tempo de uso do cateter. Conclui-se que fatores relacionados à prática dos profissionais contribuíram para a retirada dos cateteres, sinalizando para a necessidade de intervenções que melhorem a segurança e a eficácia em seu uso

Serological and molecular evidence of hepadnavirus infection in swine

Introduction and objective Recently, investigations in a swine herd identified evidence of the existence of a novel member of the Hepadnavirus family endemic in swine. The aim of this study was to investigate the serological and molecular markers of Hepadnavirus circulation in Brazilian domestic swine and wild boar herds, and to evaluate the identity with HBV and other Hepadnaviruses reported previously. Material and Methods For the study, 376 swine were screened for hepatitis B virus serological markers. Analyses were performed in serum samples using commercial enzyme-linked immunosorbent assay (ELISA) kits (DiaSorin®) for anti-HBc, HBsAg and anti-HBs. Reactive and undetermined swine serum samples were selected to perform DNA viral extraction (QIAamp DNA Mini Kit, Qiagen®), partial genome amplification and genome sequencing. Results From 376 swine samples analysed, 28 (7.45%) were reactive to anti-HBc, 3 (0.80%) to HBsAg and 6 (1.6%) to anti-HBs. Besides, more 17 (4.52%) swine samples analyzed were classified in the grey zone of the EIA test to anti-HBc and 2 (0.53%) to HBsAg. From 49 samples molecularly analyzed after serological trial, 4 samples showed a positive result for the qualitative PCR for Hepadnavirus. Phylogenetic reconstruction using partial genome sequencing (360 bp) of 3 samples showed similarity with HBV with 90.8–96.3% of identity. Conclusions Serological and molecular data showed evidence of the circulation of a virus similar to hepatitis B virus in swine

High anti-SARS-CoV-2 antibody seroconversion rates before the second wave in Manaus, Brazil, and the protective effect of social behaviour measures: results from the prospective DETECTCoV-19 cohort

Background: The city of Manaus, Brazil, has seen two collapses of the health system due to the COVID-19 pandemic. We report anti-SARS-CoV-2 nucleocapsid IgG antibody seroconversion rates and associated risk factors in Manaus residents before the second wave of the epidemic in Brazil. Methods: A convenience sample of adult (aged ≥18 years) residents of Manaus was recruited through online and university website advertising into the DETECTCoV-19 study cohort. The current analysis of seroconversion included a subgroup of DETECTCoV-19 participants who had at least two serum sample collections separated by at least 4 weeks between Aug 19 and Oct 2, 2020 (visit 1), and Oct 19 and Nov 27, 2020 (visit 2). Those who reported (or had no data on) having a COVID-19 diagnosis before visit 1, and who were positive for anti-SARS-CoV-2 nucleocapsid IgG antibodies at visit 1 were excluded. Using an in-house ELISA, the reactivity index (RI; calculated as the optical density ratio of the sample to the negative control) for serum anti-SARS-CoV-2 nucleocapsid IgG antibodies was measured at both visits. We calculated the incidence of seroconversion (defined as RI values ≤1·5 at visit 1 and ≥1·5 at visit 2, and a ratio >2 between the visit 2 and visit 1 RI values) during the study period, as well as incidence rate ratios (IRRs) through cluster-corrected and adjusted Poisson regression models to analyse associations between seroconversion and variables related to sociodemographic characteristics, health access, comorbidities, COVID-19 exposure, protective behaviours, and symptoms. Findings: 2496 DETECTCoV-19 cohort participants returned for a follow-up visit between Oct 19 and Nov 27, 2020, of whom 204 reported having COVID-19 before the first visit and 24 had no data regarding previous disease status. 559 participants were seropositive for anti-SARS-CoV-2 nucleocapsid IgG antibodies at baseline. Of the remaining 1709 participants who were seronegative at baseline, 71 did not meet the criteria for seroconversion and were excluded from the analyses. Among the remaining 1638 participants who were seronegative at baseline, 214 showed seroconversion at visit 2. The seroconversion incidence was 13·06% (95% CI 11·52–14·79) overall and 6·78% (5·61–8·10) for symptomatic seroconversion, over a median follow-up period of 57 days (IQR 54–61). 48·1% of seroconversion events were estimated to be asymptomatic. The sample had higher proportions of affluent and higher-educated people than those reported for the Manaus city population. In the fully adjusted and corrected model, risk factors for seroconversion before visit 2 were having a COVID-19 case in the household (IRR 1·49 [95% CI 1·21–1·83]), not wearing a mask during contact with a person with COVID-19 (1·25 [1·09–1·45]), relaxation of physical distancing (1·31 [1·05–1·64]), and having flu-like symptoms (1·79 [1·23–2·59]) or a COVID-19 diagnosis (3·57 [2·27–5·63]) between the first and second visits, whereas working remotely was associated with lower incidence (0·74 [0·56–0·97]). Interpretation: An intense infection transmission period preceded the second wave of COVID-19 in Manaus. Several modifiable behaviours increased the risk of seroconversion, including non-compliance with non-pharmaceutical interventions measures such as not wearing a mask during contact, relaxation of protective measures, and non-remote working. Increased testing in high-transmission areas is needed to provide timely information about ongoing transmission and aid appropriate implementation of transmission mitigation measures. Funding: Ministry of Education, Brazil; Fundação de Amparo à Pesquisa do Estado do Amazonas; Pan American Health Organization (PAHO)/WHO.World Health OrganizationRevisión por pare