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1.
Adv Pharmacol Pharm Sci ; 2023: 1512974, 2023.
Article de Anglais | MEDLINE | ID: mdl-38029230

RÉSUMÉ

Monoterpenes are secondary metabolites of plants belonging to the terpenoid class of natural products. They are the most abundant components of essential oils that are generally considered to have various pharmacological properties. These compounds are reported to have antidiabetic effects in recent years. Due to nature's complex biosynthetic machinery, they also exhibit a reasonable degree of structural complexity/diversity for further analysis in structure-activity studies. Therefore, monoterpenes as antidiabetic agents have been investigated by recent in vitro and in vivo studies extensively reported in the scientific literature and claimed by patent documents. The purpose of this survey is to provide a comprehensive and prospective review concerning the potential applications of monoterpenes in the treatment of diabetes. The data for this research were collected through the specialized databases PubMed, Scopus, Web of Science, and ScienceDirect between the years 2014 and 2022, as well as the patent databases EPO, WIPO, and USPTO. The research used 76 articles published in the leading journals in the field. The main effect observed was the antidiabetic activity of monoterpenes. This review showed that monoterpenes can be considered promising agents for prevention and/or treatment of diabetes as well as have a marked pharmaceutical potential for the development of bioproducts for therapeutics applications.

2.
J Toxicol Environ Health A ; 86(14): 479-490, 2023 07 18.
Article de Anglais | MEDLINE | ID: mdl-37246633

RÉSUMÉ

The development of new drugs through studies of candidate molecules is a complex undertaking; however, computational or in silico approaches aimed at optimizing molecules with greater development potential are being utilized for predictions of pharmacokinetic properties such as absorption, distribution, metabolism and excretion (ADME) as well as toxicological parameters. The objective of this study was to examine in silico and in vivo pharmacokinetic and toxicological properties of the chemical constituents present in the essential oil of Croton heliotropiifolius Kunth leaves. The following Pubchem platform as well as Software SwissADME and PreADMET software were employed for in silico studies while micronucleus (MN) testing for in vivo determination of mutagenicity, using Swiss adult male Mus musculus mice. In silico findings demonstrated that all chemical constituents presented (1) high oral absorption (2) medium cellular permeability and (3) high blood brain permeability. As for toxicity, these chemical constituents exhibited low to medium risk of occurrence of cytotoxicity. Regarding in vivo evaluation, peripheral blood samples obtained from animals tested with the oil showed no significant differences in number of MN compared to negative controls. Data indicate that further investigations are necessary to corroborate the findings of this study. Our data suggest that essential oil extracted from Croton heliotropiifolius Kunth leaves may serve as a candidate for new drug development.


Sujet(s)
Croton , Huile essentielle , Mâle , Animaux , Souris , Huile essentielle/toxicité , Croton/composition chimique , Encéphale , Feuilles de plante/toxicité , Feuilles de plante/composition chimique
3.
Article de Espagnol | LILACS-Express | LILACS | ID: biblio-1559912

RÉSUMÉ

Introducción: Las fracturas del acetábulo constituyen una afección traumática frecuente en el servicio de urgencia. Objetivo: Evaluar la evolución de los pacientes con fracturas de la pared posterior del acetábulo después del manejo quirúrgico. Método: Se realizó un estudio cuasiexperimental en 32 pacientes con fracturas de la pared posterior del acetábulo, intervenidos quirúrgicamente en el Servicio de Ortopedia y Traumatología del Hospital "Calixto García". Se utilizaron métodos de estadística descriptiva e inferencial. Resultados: Predominaron el grupo de 40 a 49 años, el sexo masculino, la fractura tipo ii y, en la etiología, el accidente de tránsito. La técnica de osteosíntesis con placa de reconstrucción más tornillos interfragmentarios se utilizó en la mayoría de los casos. La principal complicación fue la infección de la herida quirúrgica. El 81,2 % de los pacientes evolucionó satisfactoriamente. Conclusiones: Después del tratamiento quirúrgico, las fracturas de la pared posterior del acetábulo evolucionan de forma satisfactoria. La técnica de osteosíntesis con placa de reconstrucción más tornillos interfragmentarios mostró mejores resultados que la de tornillos interfragmentarios solamente.


Introduction: Fractures of the acetabulum are a frequent traumatic condition in the emergency service. Objective: To evaluate the evolution of patients with fractures of the posterior wall of the acetabulum after surgical management. Method: A quasi-experimental study was conducted in 32 patients with fractures of the posterior wall of the acetabulum, whom were surgically operated in the Orthopedics and Traumatology Service of "Calixto García" Hospital. Descriptive and inferential statistical methods were used. Results: The group of 40 to 49 years, the male sex, the type II fracture and, in the etiology, traffic accidents predominated. The osteosynthesis technique with reconstruction plate plus interfragmentary screws was used in most cases. The main complication was surgical wound infection. 81.2 % of patients progressed satisfactorily. Conclusions: After surgical treatment, fractures of the posterior wall of the acetabulum evolve satisfactorily. The osteosynthesis technique with reconstruction plate plus interfragmentary screws showed better results than that of interfragmentary screws alone.

4.
J Biomol Struct Dyn ; 41(6): 2555-2573, 2023 04.
Article de Anglais | MEDLINE | ID: mdl-35132947

RÉSUMÉ

Trypanosoma cruzi is a protozoan transmitted by the insect Triatoma infestans, popularly known as kissing bug. This protozoan causes the Chagas disease, a Neglected Tropical Disease. This study aimed to investigate, through DFT method and B3LYP hybrid functional, the physicochemical, pharmacokinetic, and pharmacodynamic properties of the alkaloids present in the leaves of the species Pilocarpus microphyllus (jaborandi) as a potential inhibitory activity on the protease sterol 14α-demethylase of T. cruzi associated with the techniques of molecular docking, molecular dynamics, MM-PBSA and ADMET predictions. The molecules of isopilosine, epiisopiloturine, epiisopilosine, and pilosine showed up the lowest binding energies by molecular docking, good human intestinal absorption, low penetration in the blood-brain barrier, antiprotozoal and anticarcinogenic activities in ADMET studies. It has been observed a better binding affinity of the sterol 14α-demethylase protease with isopilosine in molecular dynamics and MM-PBSA studies, which indicates it as a potential drug candidate for Chagas disease.Communicated by Ramaswamy H. Sarma.


Sujet(s)
Alcaloïdes , Maladie de Chagas , Pilocarpus , Trypanosoma cruzi , Humains , Pilocarpus/composition chimique , Simulation de docking moléculaire , Peptide hydrolases , Stérols , Alcaloïdes/composition chimique , Maladie de Chagas/traitement médicamenteux , Endopeptidases
5.
J Pharm Sci ; 112(3): 837-843, 2023 03.
Article de Anglais | MEDLINE | ID: mdl-36347357

RÉSUMÉ

In previous work, we reported on the design of biodegradable rhein-loaded PLGA microparticles for the treatment of osteoarthritis. Considering that a formulation designed for intra-articular administration must meet sterility requirements to guarantee its safety, in this study the effect of gamma radiation sterilization on these microparticles was evaluated. The size, morphology, and surface characteristics of the microparticles and the encapsulation efficiency of rhein were not affected by the sterilization process. Although DSC and PXRD analyses suggested otherwise, rhein release profiles were not altered by gamma radiation. The release of rhein from the microparticles was fitted to a Gompertz model. In conclusion, the results of this study suggest that gamma radiation is a suitable method for the sterilization of rhein-loaded PLGA microparticles to enable their intra-articular administration in order to provide a therapeutic solution to patients suffering from chronic joint diseases.


Sujet(s)
Arthrose , Acide polyglycolique , Humains , Copolymère d'acide poly(lactique-co-glycolique) , Acide lactique , Rayons gamma , Arthrose/traitement médicamenteux , Stérilisation , Microsphères , Taille de particule
6.
Chem Biol Interact ; 367: 110161, 2022 Nov 01.
Article de Anglais | MEDLINE | ID: mdl-36116513

RÉSUMÉ

Diminazene aceturate (DIZE), an antiparasitic, is an ACE2 activator, and studies show that activators of this enzyme may be beneficial for COVID-19, disease caused by SARS-CoV-2. Thus, the objective was to evaluate the in silico and in vitro affinity of diminazene aceturate against molecular targets of SARS-CoV-2. 3D structures from DIZE and the proteases from SARS-CoV-2, obtained through the Protein Data Bank and Drug Database (Drubank), and processed in computer programs like AutodockTools, LigPlot, Pymol for molecular docking and visualization and GROMACS was used to perform molecular dynamics. The results demonstrate that DIZE could interact with all tested targets, and the best binding energies were obtained from the interaction of Protein S (closed conformation -7.87 kcal/mol) and Mpro (-6.23 kcal/mol), indicating that it can act both by preventing entry and viral replication. The results of molecular dynamics demonstrate that DIZE was able to promote a change in stability at the cleavage sites between S1 and S2, which could prevent binding to ACE2 and fusion with the membrane. In addition, in vitro tests confirm the in silico results showing that DIZE could inhibit the binding between the spike receptor-binding domain protein and ACE2, which could promote a reduction in the virus infection. However, tests in other experimental models with in vivo approaches are needed.


Sujet(s)
Traitements médicamenteux de la COVID-19 , SARS-CoV-2 , Angiotensin-converting enzyme 2 , Antiparasitaires , Antiviraux/composition chimique , Antiviraux/pharmacologie , Diminazène/analogues et dérivés , Humains , Simulation de docking moléculaire , Peptide hydrolases , Peptidyl-Dipeptidase A/composition chimique , Protéine S
7.
Environ Monit Assess ; 194(6): 417, 2022 May 10.
Article de Anglais | MEDLINE | ID: mdl-35536333

RÉSUMÉ

Resilience is the ability of a system to absorb disturbances, rearrange itself, and adapt in order to maintain its functionality, structure, identity, and feedback. Research involving fire resilience in subtropical wetlands (SW) allows us to understand the dynamics of these ecosystems, measure impacts on fauna and flora, and promote policies for the management and protection. The aim of the present study is to assess the fire resilience of SW. The study was divided into three steps: (i) burned area classification, (ii) vegetation pattern classification, and (iii) temporal analysis of SW fire resilience based on NDVI calculation. Our results show that (a) high resilience potential of emerging plants, which developed green leaves in less than 90 days after the fire; (b) poor recovery of peatlands with underground fire history. Daily coverage of high spatial resolution PlanetScope images has great potential for classification and monitoring of land use in areas where there are rapid changes, such as after a fire event, explosions, and dam ruptures with ore tailings, for example.


Sujet(s)
Incendies , Feux de friches , Écosystème , Surveillance de l'environnement , Zones humides
8.
J Insect Physiol ; 136: 104344, 2022 01.
Article de Anglais | MEDLINE | ID: mdl-34896373

RÉSUMÉ

The Irre Cell Recognition Module (IRM) is an evolutionarily conserved group of transmembrane glycoproteins required for cell-cell recognition and adhesion in metazoan development. In Drosophila melanogaster ovaries, four members of this group - Roughest (Rst), Kin of irre (Kirre), Hibris (Hbs) and Sticks and stones (Sns) - play important roles in germ cell encapsulation and muscle sheath organization during early pupal stages, as well as in the progression to late oogenesis in the adult. Females carrying some of the mutant rst alleles are viable but sterile, and previous work from our laboratory had identified defects in the organization of the peritoneal and epithelial muscle sheaths of these mutants that could underlie their sterile phenotype. In this study, besides further characterizing the sterility phenotype associated with rst mutants, we investigated the role of the IRM molecules Rst, Kirre and Hbs in maintaining the functionality of the ovarian muscle sheaths. We found that knocking down any of the three genes in these structures, either individually or in double heterozygous combinations, not only decreases contraction frequency but also irregularly increases contraction amplitude. Furthermore, these alterations can significantly impact the morphology of eggs laid by IRM-depleted females demonstrating a hitherto unknown role of IRM molecules in egg morphogenesis.


Sujet(s)
Protéines de Drosophila , Drosophila , Animaux , Molécules d'adhérence cellulaire , Drosophila/génétique , Protéines de Drosophila/génétique , Drosophila melanogaster/génétique , Femelle , Protéines membranaires , Contraction musculaire , Ovogenèse , Ovaire , Ovule
9.
Hum Immunol ; 82(1): 8-10, 2021 Jan.
Article de Anglais | MEDLINE | ID: mdl-33129577

RÉSUMÉ

To improve the availability of three-dimensional (3D) structures of HLA molecules, we created the pHLA3D database. In its first version, we modeled and published 106 3D structures of HLA class I molecules from the HLA-A, HLA-B, and HLA-C loci. This paper presents an update of this database, providing more 127 3D structures of HLA class II molecules (41 DR, 42 DQ, and 44 DP), predicted via homology modeling with MODELLER and SWISS-MODEL. These new 3D structures of HLA class II molecules are now freely available at pHLA3D (www.phla3d.com.br) for immunologists and other researchers working with HLA molecules.


Sujet(s)
Antigènes HLA-DP/ultrastructure , Antigènes HLA-DQ/ultrastructure , Antigènes HLA-DR/ultrastructure , Biologie informatique , Bases de données de protéines , Humains , Structure tertiaire des protéines , Similitude de séquences d'acides aminés , Logiciel
10.
BMC Med Res Methodol ; 20(1): 286, 2020 11 30.
Article de Anglais | MEDLINE | ID: mdl-33256642

RÉSUMÉ

BACKGROUND: Systematic reviews allow health decisions to be informed by the best available research evidence. However, their number is proliferating quickly, and many skills are required to identify all the relevant reviews for a specific question. METHODS AND FINDINGS: We screen 10 bibliographic databases on a daily or weekly basis, to identify systematic reviews relevant for health decision-making. Using a machine-based approach developed for this project we select reviews, which are then validated by a network of more than 1000 collaborators. After screening over 1,400,000 records we have identified more than 300,000 systematic reviews, which are now stored in a single place and accessible through an easy-to-use search engine. This makes Epistemonikos the largest database of its kind. CONCLUSIONS: Using a systematic approach, recruiting a broad network of collaborators and implementing automated methods, we developed a one-stop shop for systematic reviews relevant for health decision making.


Sujet(s)
Prestations des soins de santé , Moteur de recherche , Bases de données bibliographiques , Bases de données factuelles , Humains , Revues systématiques comme sujet
11.
Int. j. odontostomatol. (Print) ; 14(4): 701-704, dic. 2020. graf
Article de Espagnol | LILACS | ID: biblio-1134560

RÉSUMÉ

RESUMEN: El objetivo de este artículo es presentar algunas consideraciones odontológicas y un protocolo de mantención para el manejo y cuidado de cavidad oral en pacientes en ventilación mecánica invasiva (VMI) en unidades de cuidados intensivos hospitalarios. Además, presentar recomendaciones para la implementación de estas. Desde el desarrollo del COVID-19 en el mundo, los casos de VMI prolongada han aumentado y junto con ellos, se ha visibilizado las complicaciones propias de este tipo de terapia, dentro de las cuales encontramos aquellas que afectan la cavidad oral. Los centros hospitalarios normalmente cuentan con servicios dentales conformados por distintas especialidades, las cuales en un trabajo mancomunado pueden entregar herramientas y educar al personal encargado para el cuidado de la cavidad oral en estos pacientes si es que son requeridos, siendo el odontólogo el encargado de evaluar las distintas situaciones clínicas y entregar directrices para la prevención y tratamiento de patología de la cavidad oral. En este trabajo se describen los pasos a seguir para realizar una correcta higiene oral de estos pacientes y el manejo de las distintas complicaciones posibles de observar, junto con la experiencia local de cómo solucionarlos de la mejor manera. Consideramos importante que las unidades de cuidados intensivos (UCI) conozcan el rol del odontólogo y las acciones que este equipo puede aportar en el cuidado de los pacientes hospitalizados para disminuir los riesgos asociados a ventilación prolongada, basados principalmente en el manejo de la higiene oral y lesiones asociadas.


ABSTRACT: The aim of this sutudy dental considerations and an oral cavity maintenance and care protocol in patients on invasive mechanical ventilation (IMV) in hospital intensive care units. Since the development of COVID-19 in the world, cases of prolonged IMV have increased and together with them, the complications of this type of therapy have been made visible, among which we find those that affect the oral cavity. Hospital centers normally have dental services made up of different specialties, which in a joint effort can provide tools and educate the personnel in charge of the care of the oral cavity in these patients if they are required, being the dentist the one in charge of evaluating and deliver guidelines for the prevention and treatment of pathology of the oral cavity. This work describes the steps to be followed to carry out correct oral hygiene in these patients and the management of the different complications that may be observed, along with local experience on how to best solve them. We consider important that the intensive care units (ICU) get to know the role of the dentist in the hospital environment and that they become part of the care of hospitalized patients to reduce the risks associated with prolonged ventilation, based mainly on oral hygiene management and associated injuries.


Sujet(s)
Humains , Équipe soignante , Ventilation artificielle/effets indésirables , Soins dentaires/instrumentation , COVID-19 , Intubation trachéale/effets indésirables , Protocoles cliniques , Unités de soins intensifs
12.
J Proteome Res ; 19(11): 4567-4575, 2020 11 06.
Article de Anglais | MEDLINE | ID: mdl-32786890

RÉSUMÉ

The world is currently facing the COVID-19 pandemic caused by the SARS-CoV-2 virus. The pandemic is causing the death of people around the world, and public and social health measures to slow or prevent the spread of COVID-19 are being implemented with the involvement of all members of society. Research institutions are accelerating the discovery of vaccines and therapies for COVID-19. In this work, molecular docking was used to study (in silico) the interaction of 24 ligands, divided into four groups, with four SARS-CoV-2 receptors, Nsp9 replicase, main protease (Mpro), NSP15 endoribonuclease, and spike protein (S-protein) interacting with human ACE2. The results showed that the antimalarial drug Metaquine and anti-HIV antiretroviral Saquinavir interacted with all the studied receptors, indicating that they are potential candidates for multitarget drugs for COVID-19.


Sujet(s)
Betacoronavirus , Infections à coronavirus , Découverte de médicament/méthodes , Simulation de docking moléculaire , Pandémies , Pneumopathie virale , Antiviraux/composition chimique , Antiviraux/métabolisme , Betacoronavirus/composition chimique , Betacoronavirus/métabolisme , COVID-19 , Infections à coronavirus/traitement médicamenteux , Infections à coronavirus/virologie , Humains , Pneumopathie virale/traitement médicamenteux , Pneumopathie virale/virologie , Liaison aux protéines , SARS-CoV-2 , Protéines virales/composition chimique , Protéines virales/métabolisme
13.
Rev. crim ; 62(1): 9-43, ene.-abr. 2020. graf
Article de Espagnol | LILACS | ID: biblio-1138838

RÉSUMÉ

Resumen Son variados los estudios que intentan explicar la violencia en las ciudades latinoamericanas, la mayoría abordados desde un único campo disciplinar como la sociología o la criminología. El presente artículo intenta, desde la perspectiva de la complejidad, aportar herramientas que permitan comprender las dinámicas de la violencia en los contextos urbanos. El carácter del estudio es cuantitativo; este es un caso de estudio que compara los homicidios de dos ciudades intermedias colombianas. Para ello se procesó la base de datos que recopila la Policía Nacional de Colombia por medio de su sistema estadístico, se espacializaron los datos de la ventana temporal 2010- 2016, se crearon mapas hotspots donde se evidenció la distribución de los homicidios en ciertos sectores de las ciudades estudiadas y, fi nalmente, se realizaron métricas topológicas que permitieron visualizar patrones de estos eventos violentos. Entre los hallazgos importantes que se obtuvieron con esta Metodología están (1) que los patrones de distribución y difusión son muy diferentes en espacio y tiempo porque la evolución topológica de los subgrafos que componen las redes complejas de los sistemas estudiados sigue comportamientos diferentes pese a tener una serie de variables sociales, económicas y ambientales similares; (2) que los homicidios tienden a concentrarse y coincidir con las centralidades de las ciudades estudiadas; y (3) que las herramientas de la complejidad, así como los estudios interdisciplinares, son innovadores y útiles para comprender las dinámicas de la violencia urbana.


Resumo São variados os estudos que tentam explicar a violencia nas cidades latino-americanas, a maioria abordados de um único campo disciplinar como a sociologia ou a criminologia. O presente artigo tenta, da perspectiva da complexidade, fornecer ferramentas que permitam compreender as dinâmicas da violência nos contextos urbanos. O carácter do estudo é quantitativo; este é um caso de estudo que compara os homicídios de dois cidades intermédias colombianas. Para isso foi processada a base de dados que coleta a Policia Nacional da Colômbia por meio do seu sistema estadístico, se especializaram os dados da janela temporária 2010-2016, foram criados mapas hotspots onde foi evidenciada a distribuição dos homicídios em certos setores das cidades estudadas e, finalmente, realizaram-se métricas topológicas que permitiram visualizar padres destes eventos violentos. Entre os achados importantes que foram obtidos com esta metodologia estão (1) que os padrões de distribuição e difusão são muito diferentes em espaço e tempo porque a evolução topológica dos subgrafos que compõem as redes complexas dos sistemas estudados segue comportamentos diferentes apesar a ter uma série de variáveis sociais, econômicas e ambientais similares; (2) que os homicídios tendem a se concentrar e coincidir com as centralidades das cidades estudadas; e (3) que as ferramentas da complexidade, assim como os estudos interdisciplinares, são inovadores e úteis para compreender as dinâmicas da violência urbana.


Abstract There are varied studies that attempt to explain violence in Latin American cities, most approached from a single disciplinary field such as sociology and criminology. This article tries, from the perspective of complexity, to provide tools that allow us to understand the dynamics of violence in urban contexts. The nature of the study is quantitative; this is a case study that compares the homicides of two intermediate Colombian cities. For this, the database that compiles the National Police of Colombia through its statistical system was processed, the data of the 2010-2016 time window was spatialized, hotspots maps, where we could evidence the distribution of homicides in certain sectors of the cities studied were created and, finally, topological metrics that allowed us to visualize patterns of these violent events were performed. Among the important findings that were obtained through this methodology are (1) that the distribution and diffusion patterns are very different in space and time because the topological evolution of the subgraphs that compose the complex networks of the systems studied follows different behaviors despite having a series of similar social, economic and environmental variables; (2) that homicides tend to concentrate and coincide with the centralities of the cities studied; and (3) that the tools of complexity, as well as interdisciplinary studies, are innovative and useful for understanding the dynamics of urban violence.


Sujet(s)
Humains , Violence , Sociologie , Police , Homicide
14.
J Ethnopharmacol ; 247: 112259, 2020 Jan 30.
Article de Anglais | MEDLINE | ID: mdl-31577938

RÉSUMÉ

ETHNOPHARMACOLOGICAL RELEVANCE: Ximenia americana L. is popularly known as yellow plum, brave plum or tallow wood. All the parts of this plant are used in popular medicine. Its reddish and smooth bark are used to treat skin infections, inflammation of the mucous membranes and in the wound healing process. OBJECTIVE: Verification of phytochemical profile, the molecular interaction between flavonoid, (-) epi-catechin and 5-LOX enzyme, by means of in silico study, the genotoxic effect and to investigate the pharmacological action of the aqueous extract of the stem bark of X. americana in pulmonary alterations caused by experimental COPD in Rattus norvegicus. MATERIALS AND METHODS: The identification of secondary metabolites was carried out by TLC and HPLC chromatographic methods, molecular anchoring tests were applied to analyze the interaction of flavonoid present in the extract with the enzyme involved in pulmonary inflammation process and the genotoxic effect was assessed by comet assay and micronucleus test. For induction of COPD, male rats were distributed in seven groups. The control group was exposed only to ambient air and six were subjected to passive smoke inhalations for 20 min/day for 60 days. One of the groups exposed to cigarette smoke did not receive treatment. The others were treated by inhalation with beclomethasone dipropionate (400 mcg/kg) and aqueous and lyophilized extracts of X. americana (500 mg/kg) separately or in combination for a period of 15 days. The structural and inflammatory pulmonary alterations were evaluated by histological examination. Additional morphometric analyses were performed, including the alveolar diameter and the thickness of the right ventricle wall. RESULTS: The results showed that the aqueous extract of the bark of X. americana possesses (-) epi -catechin, in silico studies with 5-LOX indicate that the EpiC ligand showed better affinity parameters than the AracA ligand, which is in accordance with the results obtained in vivo studies. Genotoxity was not observed at the dose tested and the extract was able to stagnate the alveolar enlargement caused by the destruction of the interalveolar septa, attenuation of mucus production and decrease the presence of collagen fibers in the bronchi of animals submitted to cigarette smoke. CONCLUSION: Altogether, the results proved that the aqueous extract of X. americana presents itself as a new option of therapeutic approach in the treatment of COPD.


Sujet(s)
Altération de l'ADN/effets des médicaments et des substances chimiques , Inhibiteurs de la lipoxygénase/pharmacologie , Olacaceae/composition chimique , Extraits de plantes/pharmacologie , Broncho-pneumopathie chronique obstructive/traitement médicamenteux , Animaux , Arachidonate 5-lipoxygenase/composition chimique , Arachidonate 5-lipoxygenase/pharmacologie , Brésil , Modèles animaux de maladie humaine , Ethnopharmacologie , Femelle , Humains , Inhibiteurs de la lipoxygénase/composition chimique , Inhibiteurs de la lipoxygénase/isolement et purification , Inhibiteurs de la lipoxygénase/usage thérapeutique , Mâle , Simulation de docking moléculaire , Tests de mutagénicité , Écorce/composition chimique , Extraits de plantes/composition chimique , Extraits de plantes/isolement et purification , Extraits de plantes/usage thérapeutique , Tiges de plante/composition chimique , Broncho-pneumopathie chronique obstructive/étiologie , Rats , Rat Wistar , Pollution par la fumée de tabac/effets indésirables , Résultat thérapeutique
15.
Int J Mol Sci ; 20(18)2019 Sep 12.
Article de Anglais | MEDLINE | ID: mdl-31547230

RÉSUMÉ

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.


Sujet(s)
Analgésiques/composition chimique , Anti-inflammatoires/composition chimique , Inhibiteurs des cyclooxygénases/composition chimique , Extraits de plantes/composition chimique , Pollen/composition chimique , Analgésiques/pharmacologie , Animaux , Anti-inflammatoires/pharmacologie , Abeilles , Brésil , Inhibiteurs des cyclooxygénases/pharmacologie , Acides gras/composition chimique , Acides gras/pharmacologie , Mâle , Souris , Extraits de plantes/pharmacologie , Plantes/composition chimique , Polyphénols/composition chimique , Polyphénols/pharmacologie
16.
Hum Immunol ; 80(10): 834-841, 2019 Oct.
Article de Anglais | MEDLINE | ID: mdl-31239187

RÉSUMÉ

HLA epitope analysis emerged as a strategy to determine alloimmune risk in solid organ transplantation. However, it requires not only knowledge on HLA amino acids sequences, but also on HLA three-dimensional structures. Unfortunately, the number of structures available is still unsatisfactory. This work reports the modelling of 106 heterotrimeric (alpha chain + ß2M + peptide) HLA class I molecules. The models were generated by homology modelling using Modeller, refined using GalaxyRefine server, heterodimerized with Swiss-PDB Viewer and, finally, assessed as to their structural quality through Dali server. The final structures were made available through a free online database, pHLA3D (www.phla3d.com.br), developed in Ruby language using the Ruby on Rails web framework. Structural parameters were similar between refined molecules and their templates. The new database may improve HLA epitope analysis and better guide risk assessment in solid organ transplantation setting.


Sujet(s)
Systèmes de gestion de bases de données , Bases de données de protéines , Antigènes d'histocompatibilité de classe I/composition chimique , Structure secondaire des protéines , Similitude structurale de protéines , Allèles , Séquence d'acides aminés , Épitopes/immunologie , Histocompatibilité , Humains , Modèles moléculaires , Navigateur
17.
Rev. cuba. enferm ; 34(4): e1525, oct.-dic. 2018. tab, graf
Article de Portugais | CUMED, LILACS | ID: biblio-1126466

RÉSUMÉ

RESUMO Introdução: Pessoas acamadas estão susceptíveis as úlceras por pressão, embora as causas possam ser multifatoriais, a manutenção do microclima da pele constitui importante fator de prevenção dessas injúrias. Objetivo: Demonstrar as vantagens térmicas da Rede de dormir em relação ao Colchão hospitalar. Métodos: Experimental com seres humanos, amostra de 40 participantes, cada indivíduo foi seu próprio controle. O repouso em cada superfície de apoio foi de 30 minutos. Materiais: Colchão hospitalar D-28 revestido com capa em napa azul, Rede de dormir em algodão cru, termo higrômetro Minipa MT 242, termômetro digital infravermelho com mira laser e balança antropométrica. Para estatística utilizou-se Software R. Resultados: A temperatura de interface na Rd após os 15 minutos de repouso estabilizou na média de 1 ºC de elevação da temperatura inicial, no Colchão hospitalar ao término dos 30 minutos, a temperatura continuou em elevação, na média de 3 ºC. As variáveis não seguiram distribuição normal. O teste de Wilkoxon demonstrou diferença significativa para p<0,05. Conclusões: Demonstrou-se, em laboratório, que a Rede de dormir, em relação ao Colchão hospitalar, dissipa, significativamente, com maior eficiência o calor do corpo. O fato da Rede de dormir alterar minimamente um componente do microclima da pele sob pressão, fortalece a afirmativa que o seu uso contribui na prevenção da úlceras por pressão(AU)


RESUMEN Introducción: Las personas encamadas son susceptibles a úlceras por presión. Aunque las causas de estos padecimientos son multifactoriales, el mantenimiento del microclima de la piel constituye un factor importante de prevención. Objetivo: Demostrar las ventajas térmicas de la red de dormir en relación con el colchón hospitalario. Métodos: Estudio experimental con seres humanos. La muestra quedó conformada por 40 participantes; cada uno de ellos fue su propio control. El reposo en cada superficie de apoyo fue de 30 minutos. Materiales: colchón hospitalario D-28 revestido con capa impermeable azul; red en algodón 100 %-Minipa MT 242, termómetro laser digital infrarrojo y balanza antropométrica. Para el procesamiento estadístico se utilizó el software R. Resultados: La temperatura de interface en red de dormir, después de los 15 minutos de reposo, subió en promedio 1 °C con respecto a la temperatura inicial; en el colchón hospitalario, al término de los 30 minutos, la temperatura continuó elevándose con una media de 3 °C. Las variables no siguieron una distribución normal. El test de Wilkoxon demostró diferencia significativa con p<0,05. Conclusiones: Se demostró en prueba de laboratorio que la red disipa con mayor eficacia el calor del cuerpo. El que la red altere mínimamente un componente del microclima sobre la piel, confirma su utilidad en la prevención de úlceras por presión(AU)


ABSTRACT Introduction: People bedridden are likely to Pressure Ulcers, although the causes may be multifactorial, the maintenance of the skin microclimate is an important factor for preventing these injuries. Objective: To demonstrate the advantages of thermal sleeping hammock in relation to the hospital mattress. Methods: Experimental with humans, sample of 40 participants, each individual has their own control. Resting on each support surface was 30 minutes. Methods: Hospital mattress D-28 coated with blue cover in nappa, sleeping hammock in raw cotton, thermo hygrometer Minipa MT 242, infrared digital thermometer with laser sight and anthropometric scale. Statistical software was used sleeping hammock. Results: The interface temperature at sleeping hammock after 15 minutes of rest stabilized average elevation of 1 °C initial temperature, at hospital mattress at the end of 30 minutes, the temperature continued to rise, the average of 3 °C. The variables did not follow normal distribution. The Wilkoxon test showed a significant difference at p <0.05. Conclusions: It has been demonstrated in the laboratory that sleeping hammock in relation to hospital mattress dissipates significantly more efficiently the heat of the body. The fact of sleeping hammock minimally change a microclimate component of the skin under pressure, strengthens the claim that their use contributes to the prevention of Pressure Ulcers(AU)


Sujet(s)
Humains , Soins infirmiers intégraux/méthodes , Prévention des Maladies , Personnes grabataires , Escarre/épidémiologie
18.
Genesis ; 56(9): e23242, 2018 09.
Article de Anglais | MEDLINE | ID: mdl-30114331

RÉSUMÉ

The Irre cell-recognition module (IRM) is a group of evolutionarily conserved and structurally related transmembrane glycoproteins of the immunoglobulin superfamily. In Drosophila melanogaster, it comprises the products of the genes roughest (rst; also known as irreC-rst), kin-of-irre (kirre; also known as duf), sticks-and-stones (sns), and hibris (hbs). In this model organism, the behavior of this group of proteins as a partly redundant functional unit mediating selective cell recognition was demonstrated in a variety of developmental contexts, but their possible involvement in ovarian development and oogenesis has not been investigated, notwithstanding the fact that some rst mutant alleles are also female sterile. Here, we show that IRM genes are dynamically and, to some extent, coordinately transcribed in both pupal and adult ovaries. Additionally, the spatial distribution of Hbs, Kirre, and Rst proteins indicates that they perform cooperative, although largely nonredundant, functions. Finally, phenotypical characterization of three different female sterile rst alleles uncovered two temporally separated and functionally distinct requirements for this locus in ovarian development: one in pupa, essential for the organization of peritoneal and epithelial sheaths that maintain the structural integrity of the adult organ and another, in mature ovarioles, needed for the progression of oogenesis beyond stage 10.


Sujet(s)
Molécules d'adhérence cellulaire neuronale/génétique , Protéines de Drosophila/génétique , Drosophila melanogaster/génétique , Protéines de l'oeil/génétique , Protéines membranaires/génétique , Protéines du muscle/génétique , Ovogenèse/génétique , Ovaire/croissance et développement , Animaux , Drosophila melanogaster/cytologie , Femelle , Expression des gènes , Mutation
19.
Front Microbiol ; 9: 1351, 2018.
Article de Anglais | MEDLINE | ID: mdl-30018595

RÉSUMÉ

The Candida genus comprises opportunistic fungi that can become pathogenic when the immune system of the host fails. Candida albicans is the most important and prevalent species. Polyenes, fluoropyrimidines, echinocandins, and azoles are used as commercial antifungal agents to treat candidiasis. However, the presence of intrinsic and developed resistance against azole antifungals has been extensively documented among several Candida species. The advent of original and re-emergence of classical fungal diseases have occurred as a consequence of the development of the antifungal resistance phenomenon. In this way, the development of new satisfactory therapy for fungal diseases persists as a major challenge of present-day medicine. The design of original drugs from traditional medicines provides new promises in the modern clinic. The urgent need includes the development of alternative drugs that are more efficient and tolerant than those traditional already in use. The identification of new substances with potential antifungal effect at low concentrations or in combination is also a possibility. The present review briefly examines the infections caused by Candida species and focuses on the mechanisms of action associated with the traditional agents used to treat those infections, as well as the current understanding of the molecular basis of resistance development in these fungal species. In addition, this review describes some of the promising alternative molecules and/or substances that could be used as anticandidal agents, their mechanisms of action, and their use in combination with traditional drugs.

20.
Mech Dev ; 154: 193-202, 2018 12.
Article de Anglais | MEDLINE | ID: mdl-30030087

RÉSUMÉ

Cell adhesion molecules play a central role in morphogenesis, as they mediate the complex range of interactions between different cell types that result in their arrangement in multicellular organs and tissues. How their coordinated dynamic expression in space and time - an essential requirement for their function - is regulated at the genomic and transcriptional levels constitutes an important, albeit still little understood question. The Irre Cell Recognition Module (IRM) is a highly conserved phylogenetically group of structurally related single pass transmembrane glycoproteins belonging to the immunoglobulin superfamily that in Drosophila melanogaster are encoded by the genes roughest (rst), kin-of-irre (kirre), sticks-and-stones (sns) and hibris (hbs). Their cooperative and often partly redundant action are crucial to major developmental processes such axonal pathfinding, myoblast fusion and patterning of the pupal retina. In this latter system rst and kirre display a tightly regulated complementary transcriptional pattern so that lowering rst mRNA levels leads to a concomitant increase in kirre mRNA concentration. Here we investigated whether other IRM components are similarly co-regulated and the extent changes in their mRNA levels affect each other as well as their collective function in retinal patterning. Our results demonstrate that silencing any of the four IRM genes in 24% APF retinae changes the levels all other group members although only kirre and hbs mRNA levels are increased. Furthermore, expression, in a rst null background, of truncated versions of rst cDNA in which the portion encoding the intracellular domain has been partially or completely removed not only can still induce changes in mRNA levels of other IRM members but also result in Kirre mislocalization. Taken together, our data point to the presence of a highly precise and fine-tuned control mechanism coordinating IRM expression that may be crucial to the functional redundancy shown by its components during the patterning of the pupal retina.


Sujet(s)
Protéines de Drosophila/génétique , Drosophila melanogaster/génétique , Protéines de l'oeil/génétique , Pupe/génétique , Rétine/physiologie , Transcription génétique/génétique , Animaux , Molécules d'adhérence cellulaire/génétique , Régulation de l'expression des gènes/génétique , Glycoprotéines/génétique , Protéines membranaires/génétique , Morphogenèse/génétique , ARN messager/génétique
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