In Vitro and In Silico Evaluation of Cholinesterase Inhibition by Alkaloids Obtained from Branches of Abuta panurensis Eichler

Alkaloids are natural products known as ethnobotanicals that have attracted increasing attention due to a wide range of their pharmacological properties. In this study, cholinesterase inhibitors were obtained from branches of Abuta panurensis Eichler (Menispermaceae), an endemic species from the Amazonian rainforest. Five alkaloids were isolated, and their structure was elucidated by a combination of 1D and 2D 1H and 13C NMR spectroscopy, HPLC-MS, and high-resolution MS: Lindoldhamine isomer m/z 569.2674 (1), stepharine m/z 298.1461 (2), palmatine m/z 352.1616 (3), 5-N-methylmaytenine m/z 420.2669 (4) and the N-trans-feruloyltyramine m/z 314.1404 (5). The compounds 1, 3, and 5 were isolated from A. panurensis for the first time. Interaction of the above-mentioned alkaloids with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes was investigated in silico by molecular docking and molecular dynamics. The molecules under investigation were able to bind effectively with the active sites of the AChE and BChE enzymes. The compounds 1–4 demonstrated in vitro an inhibitory effect on acetylcholinesterase with IC50 values in the range of 19.55 µM to 61.24 µM. The data obtained in silico corroborate the results of AChE enzyme inhibition

Alkaloids of Abuta panurensis Eichler : In silico and in vitro study of acetylcholinesterase inhibition, cytotoxic and immunomodulatory activities

Natural products obtained from species of the genusAbuta(Menispermaceae) are known as ethnobotanicals that are attracting increasing attention due to a wide range of their pharmacological properties. In this study, the alkaloids stepharine and 5-N-methylmaytenine were first isolated from branches ofAbuta panurensisEichler, an endemic species from the Amazonian rainforest. Structure of the compounds was elucidated by a combination of 1D and 2D NMR spectroscopic and MS and HRMS spectrometric techniques. Interaction of the above-mentioned alkaloids with acetylcholinesterase enzyme and interleukins IL-6 and IL-8 was investigatedin silicoby molecular docking. The molecules under investigation were able to bind effectively with the active sites of the AChE enzyme, IL-6, and IL-8 showing affinity towards the proteins. Along with the theoretical study, acetylcholinesterase enzyme inhibition, cytotoxic, and immunomodulatory activity of the compounds were assessed byin vitroassays. The data obtainedin silicocorroborate the results of AChE enzyme inhibition, the IC(50)values of 61.24 mu M for stepharine and 19.55 mu M for 5-N-methylmaytenine were found. The compounds showed cytotoxic activity against two tumor cell lines (K562 and U937) with IC(50)values ranging from 11.77 mu M to 28.48 mu M. Thein vitroassays revealed that both alkaloids were non-toxic to Vero and human PBMC cells. As for the immunomodulatory activity, both compounds inhibited the production of IL-6 at similar levels. Stepharine inhibited considerably the production of IL-8 in comparison to 5-N-methylmaytenine, which showed a dose dependent action (inhibitory at the IC(50)dose, and stimulatory at the twofold IC(50)one). Such a behavior may possibly be explained by different binding modes of the alkaloids to the interleukin structural fragments. Occurrence of the polyamine alkaloid 5-N-methylmaytenine was reported for the first time for the Menispermaceae family, as well as the presence of stepharine inA.panurensis.Peer reviewe

ANÁLISE POSTURAL EM ESCOLARES NA CIDADE DE QUIXADÁ/CE

De acordo com a Organização Mundial da Saúde (OMS), 80% da população sofrerá, ao menos duas vezes na vida, alguma crise de dor nas costas. Um dos principais motivos é a chamada “escoliose” – que, segundo a instituição afeta de 2% a 4% da população mundial. No Brasil, a prevalência varia entre 1,03 e 15,8%. A escoliose é definida como uma deformação morfológica da coluna vertebral nos três planos do espaço. Assim, a coluna realmente se torce, não somente para os lados, mas para frente e para trás e em volta do seu próprio eixo

Utilização de tóros mandibular para reconstrução de seio maxilar: revisão de literatura

O tóros mandibular é uma exostose óssea benigna, de crescimento lento que se desenvolve geralmente ao longo da superfície lingual da mandíbula, de ocorrência não rara porém assintomática, que na maioria das vezes se passa despercebida. O objetivo deste trabalho foi foi realizar uma revisão de literatura sobre o uso de tóros mandibular como fonte doadora de enxerto autógeno em procedimento de reconstrução do seio maxilar para reabilitação implantossuportada. Os resultados mostraram que os enxertos autógenos para as reconstruções ósseas na implantodontia têm um papel fundamental, pois é o material com as melhores propriedades biológicas para estes procedimentos de enxertia. Entretanto, a necessidade de um acesso cirúrgico à área doadora para a coleta do material acarreta maior morbidade para o procedimento. Por outro lado, pacientes que apresentam exostoses ósseas com indicação de remoção são ótimos candidatos para utilização do osso removido como enxerto em reconstruções ósseas para fins de reabilitação implantossuportada

Određivanje fizikalno-kemijskih svojstava, stabilnosti i citotoksičnosti plavog bojila dobivenog iz ploda jague (Genipa americana L.)

Research background. The current commercial scenario indicates an increase in the demand for natural dyes. Compared to synthetic dyes, natural ones have the advantage of being sustainable, making them of great interest for the food and cosmetic industries. The development of new natural dyes is necessary, as well as the carrying out of complementary research regarding the existing ones. Experimental approach. The present study aims to characterize the physicochemical and biological characteristics of the dye obtained from dehydrated endocarp of the genipap (Genipa americana) fruit, as well as perform the relevant stability and cytotoxicity tests. The chemical characterization was performed by HPLC-MS/MS analyses. The stability studies were carried out by spectrophotometry and cytotoxicity assays using cell culture and fluorometric methods. Results and conclusions. After dehydration and milling of the fruit endocarp, water was added to the obtained powder (in the ratio 4:1) to extract the dye. Five compounds were elucidated using HPLC-MS/MS and confirmed the presence of the geniposide as its main compound. With the X-ray diffraction and electron microscopy analysis, we characterised the obtained powder as being amorphous and of porous structure with a variable size. The thermogravimetric analysis indicated a maximum loss of 61% mass after exposure to a temperature range from 240 to 760 °C. The obtained blue dye was stable in the absence of light, at room temperature and had neutral pH. In the cytotoxicity assay, (95.0±1.3) % of viable human fibroblasts were observed after exposure to this dye. The genipap fruit can be a viable alternative to produce a natural blue dye, since it is easy to obtain and has very low toxicity in food, pharmaceutical or cosmetic products. Novelty and scientific contribution. This study demonstrates for the first time the physicochemical and biological properties of a natural blue dye from G. americana fruit.Pozadina istraživanja. Na tržištu se povećala potražnja za prirodnim bojilima. Njihova je prednost nad sintetičkima ta da potječu iz održivih izvora, pa su od velikog interesa za prehrambenu i kozmetičku industriju. Stoga je bitno razvijati nova prirodna bojila, te dodatno ispitati postojeća. Eksperimentalni pristup. Svrha je ovoga rada bila ispitati fizikalno-kemijska i biološka svojstva bojila dobivenog ektrakcijom dehidriranog endokarpa ploda biljke jagua (Genipa americana), te testirati njegovu stabilnosti i citotoksičnost. Kemijska svojstva određena su spregnutim sustavom visokodjelotvorne tekućinske kromatografije i tandemne spektrometrije masa (HPLC-MS/MS). Stabilnost je ispitana spektrofotometrijom, a citotoksičnost pomoću staničnih kultura i fluorometrijom. Rezultati i zaključci. Nakon dehidriranja i meljave endokarpa jague, za ekstrakciju bojila dobiveni je prah pomiješan s 20 % vode. Metodom HPLC-MS/MS detektirano je pet spojeva, te je potvrđena prisutnost genipozida kao glavnog sastojka. Rendgenskom difrakcijom i elektronskom mikroskopijom struktura dobivenog praha okarakterizirana je kao amorfna i porozna, s česticama različitih veličina. Termogravimetrijskom je analizom utvrđen gubitak od 61 % mase praha nakon izlaganja temperaturama između 240 i 760 °C. Dobiveno je bojilo bilo stabilno u mraku, pri sobnoj temperaturi i neutralnoj pH-vrijednosti. U testu citotoksičnosti utvrđena je stopa preživljavanja fibroblasta od (95,0±1,3) % nakon njihovog izlaganja bojilu. Stoga je zaključeno da plod voćke jagua može poslužiti kao izvor prirodnog bojila za primjenu u prehrambenoj, farmaceutskoj i kozmetičkoj industriji, jer se jednostavno dobiva i ima vrlo malu toksičnost. Novina i znanstveni doprinos. U ovom su radu po prvi put opisana fizikalno-kemijska i biološka svojstva prirodnog bojila dobivenog iz ploda voćke G. americana

Analgesic, Anti-Inflammatory, and Antioxidant Activities of Byrsonima duckeana

Background. Byrsonima is a promising neotropical genus, rich in flavonoids and triterpenes, with several proven pharmacological properties. Nevertheless, Byrsonima duckeana W. R. Anderson is an Amazonian species almost not studied. Objective. To assess the antioxidant, anti-inflammatory, and analgesic activities of Byrsonima duckeana leaves. Materials and Methods. We analyzed an ethanol extract and its fractions for polyphenol content and UHPLC-MS/MS, phosphomolybdenum, DPPH, TBARS antioxidant tests, formalin-induced pain, carrageenan-induced peritonitis, acetic acid-induced abdominal writhings, and hot plate assays. Results. All the samples showed high polyphenol content and antioxidant capacity in the phosphomolybdenum, DPPH, and TBARS tests. We identified ethyl gallate, quinic acid, gallic acid, catechin, epicatechin, quercetrin, and quercetin in the samples. B. duckeana was able to reduce leukocyte migration in the carrageenan-induced peritonitis by 43% and the licking time in the formalin test by 57%. In the acetic acid-induced writhing test, the chloroform (FCL) and ethyl acetate (FEA) fractions were the most active samples. FEA was selected for the hot plate test, where all the dosages tested (5, 50, and 200 mg·kg−1) showed significant analgesic activity. Conclusion. B. duckeana has interesting analgesic and antioxidant activities, due to its high phenolic content, especially phenolic acids

Integrative analysis based on HPLC-DAD-MS/MS and NMR of Bertholletia excelsa Bark Biomass Residues: Determination of ellagic acid derivatives

Bertholletia excelsa Bonpl. (Lecythidaceae) is a South American tree worldwide known for providing the Brazil nuts. In the Amazon Region, B. excelsa is found in monocultures, integrating agroforestries and providing raw materials for food and timber industries. Through the application of an integrative analysis based on high-performance liquid chromatography coupled with diode array detector and tandem mass spectrometry (HPLC-DAD-MS/MS) and nuclear magnetic resonance (NMR) techniques, the present study showed that B. excelsa bark biomass residues contain large quantities of ellagic acid (EA) and its derivatives. Qualitatively, five compounds were characterized for the first time in this species. Quantitations were carried out to determine the total amount of these compounds in outer and inner bark tissues. A total of 4.96 and 44.09 g of EA derivatives per kg of dry residues was determined for the outer and inner barks, respectively. Among the EA derivatives, eschweilenol C, ellagic acid and valoneic acid dilactone were the main compounds. These results pointed B. excelsa barks as a valuable biomass residue with potential to be source of health-promoting compounds. Therefore, a potential raw material as source of valuable bioactive phenolic compounds is described herein. © 2019 Sociedade Brasileira de Química

Novas evidências na abordagem terapêutica da Nefrolitíase em pacientes pediátricos: uma revisão integrativa: New evidence on the therapeutic approach to Nephrolithiasis in pediatric patients: an integrative review

A nefrolitíase possui prevalência mundial situada entre 5% e 15%, além de recorrência em adultos de até 75% em 20 anos entre os pacientes que sofrem recidivas. Já em crianças, a nefrolitíase é relativamente infrequente, com prevalência que varia entre 2 a 2,7%, sendo o tratamento dividido entre medidas farmacológicas e medidas não farmacológicas. O presente estudo de revisão buscou avaliar novas evidências na abordagem terapêutica da nefrolitíase em pacientes pediátricos, documentados por meio de estudos clínicos e randomizados. Trata-se de uma pesquisa de revisão integrativa realizada por meio da base de dados PubMed, que levou em consideração os seguintes critérios de inclusão: ensaios clínicos e testes controlados e aleatórios; artigos publicados nos últimos quatro anos; que possuíam texto completo disponível e que abordassem acerca da terapêutica da nefrolitíase na população pediátrica. Ficou constatado que no âmbito do tratamento farmacológico, o lumasiran se mostrou útil na diminuição da taxa de eventos provocados por cálculos em crianças com hiperoxalúria tipo 1. No que se refere à terapêutica não invasiva, estudos apontaram as frequências intermediárias como as melhores a serem utilizadas durante a LECO em crianças, além do aumento da eficácia deste procedimento quando feito após hidronefrose artificial. Quanto à terapêutica invasiva, foi atestado o aumento da eficácia da NLPC quando feito sob a técnica de dilatação de passo único em crianças com nefrolitíase. Ainda sobre a NLPC, foi observado não haver diferença significativa de complicações ou dor pós-operatória da cirurgia em relação à posição da criança

Avaliação por usuários acometidos pela doença

Funding Information: This research was funded by the Dean of Research and Graduate Studies at the Federal University of Alfenas, MG, No. 002/2020. We thank PhD Isabel Cristina Martins de Freitas for her methodological and statistical support. Publisher Copyright: © 2023 Centro Universitario Sao Camilo. All rights reserved.The coronavirus disease pandemic greatly impacted society, creating unprecedented challenges for science, healthcare systems, and Primary Health Care, which were quickly charged with diversified responses to face this public health emergency. The objective of this study was to evaluate the quality of PHC from the perspective of people affected by COVID-19. This was a cross-sectional study with cases of COVID-19 in a Brazilian municipality. We used an electronic questionnaire with sociodemographic and clinical characteristics (of our own elaboration) and the PCATool-Brazil Instrument ­ for adult patients (reduced version), through the KoBoToolbox resource. After a pre-test and pilot study, data collection took place between January 11 and October 5, 2021. Descriptive statistics were used, calculating the General PHC Score ­ 0 to 10 (mean and standard deviations). 91 participants evaluated the PHC characteristics/ components. The overall PHC score (mean) was 4.4 (SD=1.9). This low overall PHC score obtained indicates weaknesses in the quality of this level of healthcare, in the first six months of the pandemic in 2020. Such a low PHC quality score is unprecedented. It appears that the negative result in the studied municipality reflects the impact of COVID-19 and the strategies adopted to face the pandemic triggered by SARS-CoV-2 in Brazil and in the world.publishersversionpublishe