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1.
Antibiotics (Basel) ; 9(9)2020 Sep 21.
Article in English | MEDLINE | ID: mdl-32967114

ABSTRACT

Amphibian skin secretions are abundant in bioactive compounds, especially antimicrobial peptides. These molecules are generally cationic and rich in hydrophobic amino acids, have an amphipathic structure and adopt an α-helical conformation when in contact with microorganisms membranes. In this work, we purified and characterized Figainin 1, a novel antimicrobial and antiproliferative peptide from the cutaneous secretion of the frog Boana raniceps. Figainin 1 is a cationic peptide with eighteen amino acid residues-rich in leucine and isoleucine, with an amidated C-terminus-and adopts an α-helical conformation in the presence of trifluoroethanol (TFE). It displayed activity against Gram-negative and especially Gram-positive bacteria, with MIC values ranging from 2 to 16 µM, and showed an IC50 value of 15.9 µM against epimastigote forms of T. cruzi; however, Figanin 1 did not show activity against Candida species. This peptide also showed cytolytic effects against human erythrocytes with an HC50 of 10 µM, in addition to antiproliferative activity against cancer cells and murine fibroblasts, with IC50 values ranging from 10.5 to 13.7 µM. Despite its adverse effects on noncancerous cells, Figainin 1 exhibits interesting properties for the development of new anticancer agents and anti-infective drugs against pathogenic microorganisms.

2.
Sci Rep ; 10(1): 11680, 2020 07 15.
Article in English | MEDLINE | ID: mdl-32669617

ABSTRACT

Bioactive plant peptides have received considerable interest as potential antihypertensive agents with potentially fewer side effects than antihypertensive drugs. Here, the blood pressure-lowering effects of the Bowman-Birk protease inhibitor, BTCI, and its derived peptides, PepChy and PepTry, were investigated using normotensive (Wistar-WR) and spontaneously hypertensive rats (SHR). BTCI inhibited the proteases trypsin and chymotrypsin, respectively, at 6 µM and 40 µM, a 10-fold greater inhibition than observed with PepTry (60 µM) and PepChy (400 µM). These molecules also inhibited angiotensin converting enzyme (ACE) with IC50 values of 54.6 ± 2.9; 24.7 ± 1.1; and 24.4 ± 1.1 µM, respectively, occluding its catalytic site, as indicated by molecular docking simulation, mainly for PepChy and PepTry. Gavage administration of BTCI and the peptides promoted a decrease of systolic and diastolic blood pressure and an increase of renal and aortic vascular conductance. These effects were more expressive in SHR than in WR. Additionally, BTCI, PepChy and PepTry promoted coronary vasodilation and negative inotropic effects in isolated perfused hearts. The nitric oxide synthase inhibitor blunted the BTCI and PepChy, with no cardiac effects on PepTry. The findings of this study indicate a therapeutic potential of BTCI and its related peptides in the treatment of hypertension.


Subject(s)
Antihypertensive Agents/pharmacology , Blood Pressure/drug effects , Hypertension/drug therapy , Myocardial Contraction/drug effects , Peptides/pharmacology , Trypsin Inhibitor, Bowman-Birk Soybean/pharmacology , Animals , Antihypertensive Agents/chemistry , Binding Sites , Chymotrypsin/chemistry , Chymotrypsin/metabolism , Coronary Vessels/drug effects , Coronary Vessels/physiopathology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Hypertension/enzymology , Hypertension/physiopathology , Male , Molecular Docking Simulation , NG-Nitroarginine Methyl Ester/chemistry , NG-Nitroarginine Methyl Ester/pharmacology , Nitric Oxide Synthase Type III/antagonists & inhibitors , Nitric Oxide Synthase Type III/chemistry , Nitric Oxide Synthase Type III/metabolism , Peptides/chemical synthesis , Peptidyl-Dipeptidase A/chemistry , Peptidyl-Dipeptidase A/metabolism , Protein Binding , Protein Interaction Domains and Motifs , Protein Structure, Secondary , Rats , Rats, Inbred SHR , Rats, Wistar , Trypsin/chemistry , Trypsin/metabolism , Trypsin Inhibitor, Bowman-Birk Soybean/chemistry , Vasodilation/drug effects
3.
Biomolecules ; 10(5)2020 05 20.
Article in English | MEDLINE | ID: mdl-32443921

ABSTRACT

In recent years, the number of new antimicrobial drugs launched on the market has decreased considerably even though there has been an increase in the number of resistant microbial strains. Thus, antimicrobial resistance has become a serious public health problem. Amphibian skin secretions are a rich source of host defense peptides, which generally are cationic and hydrophobic molecules, with a broad-spectrum of activity. In this study, one novel multifunctional defense peptide was isolated from the skin secretion of the Chaco tree frog, Boana raniceps. Figainin 2 (1FLGAILKIGHALAKTVLPMVTNAFKPKQ28) is cationic and hydrophobic, adopts an α-helical structure in 50% (v/v) trifluoroethanol (TFE), and is thermally stable. This peptide exhibited activity against Gram-negative and Gram-positive pathogenic bacteria arboviruses, T. cruzi epimastigotes; however, it did not show activity against yeasts. Figainin 2 also showed antiproliferative activity on cancer cells, is moderately active on human erythrocytes, and activates the oxidative burst in human neutrophils.


Subject(s)
Amphibian Proteins/metabolism , Anura/metabolism , Defensins/metabolism , Skin/metabolism , Amphibian Proteins/chemistry , Amphibian Proteins/pharmacology , Animals , Arboviruses/drug effects , Bacteria/drug effects , Candida/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Cells, Cultured , Defensins/chemistry , Defensins/pharmacology , Hemolysis/drug effects , Humans , Neutrophils/drug effects , Protein Conformation, alpha-Helical , Trypanosoma cruzi/drug effects
4.
REVISA (Online) ; 8(4): 418-426, Out-Dez.2019.
Article in English, Portuguese | LILACS | ID: biblio-1050899

ABSTRACT

Objetivo: compreender o entendimento dos profissionais de saúde básica de um município de Goiás, no que se refere a utilização dos Equipamentos de Proteção Individual, focado nos Técnicos de Enfermagem e Enfermeiros dos postos de saúde. Método: foram elaborados questionários sobre a mesma abordagem para esses profissionais, refletindo na parcialidade de retorno dos questionários entregues, embora não influenciou no estudo pretendido, por se tratar de uma pesquisa por amostragem. Resultados: Foram submetidos ao estudo por meio deste recurso, 13 (treze) Técnicos de Enfermagem e 20 (vinte) Enfermeiros. Diante do recurso utilizado, seguiu-se a pesquisa a luz de autores que abordam o tema em estudo. Conclusão: embora pareça lógico, algumas intervenções precisam ser feitas no sentido de melhorar o uso dos EPIs em meio aos profissionais que constituem o sistema de saúde desde um município até a configuração nacional, pois o entendimento é que o todo se constitui por unidades.


Objective: to know the understanding of basic health professionals in a city of Goias state, regarding the use of Personal Protective Equipment, focused on Nursing Technicians and Nurses in health posts. Method: questionnaires were elaborated on the same approach for these professionals, reflecting on the partial return of the questionnaires delivered, although it did not influence the intended study, as it was a sample survey. Results: Through this resource, 13 (thirteen) Nursing Technicians and 20 (twenty) Nurses were submitted to the study. Given the resource used, the research followed the light of authors addressing the subject under study. Conclusion: although it seems logical, some interventions need to be made in order to improve the use of PPE among professionals who constitute the system. from a municipality to the national configuration, because the understanding is that the whole is constituted by units.


Subject(s)
Humans , Personal Protective Equipment , Nursing Assistants , Health
5.
REVISA (Online) ; 8(4): 505-511, Out-Dez.2019.
Article in English, Portuguese | LILACS | ID: biblio-1051077

ABSTRACT

Objetivo: proporcionar à comunidade acadêmica e social as práticas corretas de armazenamento e descarte dos medicamentos vencidos, em desuso e/ou inapropriados na instituição de ensino superior no DF. Método: A coleta dos medicamentos ocorreu no período de um ano, entre 2018 e 2019. Foi realizada a abertura da caixa de coleta permanente na Instituição de Educação Superior e a contagem manual de todos os medicamentos descartados. Os medicamentos foram relacionados em uma planilha de acordo com a classificação de bioequivalência, vias de administração, formas farmacêuticas, validade, preparação e classe terapêutica. Resultados: Desta forma, o ponto ativo fixo de coleta de medicamentos descartados na Instituição de Educação Superior proporciona um grande impacto social e ambiental, colaborando tanto com orientações na sociedade quanto promovendo uma ação permanente de auxílio aos órgãos governamentais a promoverem ações de correto destinação de medicações que tenham sido descartados. No período de 1 (um) ano, de um total de 922 unidades, sendo 84 medicamentos distintos, a predominância foi de medicamentos similares. Dentre as vias de administração, os medicamentos administrados via oral foram os mais descartados. Além disso, observa-se que esse ponto foi instalado há 1 ano, ou seja, em agosto de 2018, e foram contabilizados medicamentos desde 2012, ou seja, a população tem o hábito em armazenar esses medicamentos mesmo vencidos em domicílio. Conclusão: Constatou-se a necessidade de melhor esclarecimento sobre o assunto através de campanhas de incentivo e orientação, quanto ao destino adequado para resíduos de medicamentos e promoção ao uso racional de medicamentos, a fim de conscientizar a sociedade a utilização moderada dos medicamentos e a implementação de pontos de coleta acessíveis à população.


Objective: To provide the academic and social community with the correct storage and disposal practices for expired, disused and/or inappropriate medicines in the higher education institution in the Federal District. Method: The collection of medicines took place within one year, between 2018 and 2019. The permanent collection box was opened at the Higher Education Institution and the manual counting of all discarded medicines. The drugs were listed in a spreadsheet according to bioequivalence classification, routes of administration, pharmaceutical forms, validity, preparation and therapeutic class. Results: Thus, the fixed active point of collection of discarded medicines in the Higher Education Institution provides a great social and environmental impact, collaborating with orientations in the society as well as promoting a permanent action of assistance to the government agencies to promote actions of correct destination of. medications that have been discarded. In the period of 1 (one) year, out of a total of 922 units, being 84 different drugs, the predominance was similar drugs. Among the routes of administration, the drugs administered orally were the most discarded. In addition, it is observed that this point was installed 1 year ago, that is, in August 2018, and medicines have been counted since 2012, that is, the population has the habit of storing these medicines even at home. Conclusion: There was a need for better clarification on the subject through incentive and orientation campaigns, as to the appropriate destination for drug residues and promotion of the rational use of medicines, in order to make society aware of the moderate use of medicines and implementation of collection points accessible to the population.


Subject(s)
Pharmacy
6.
REVISA (Online) ; 7(1): 54-65, 2018.
Article in Portuguese | LILACS | ID: biblio-1096882

ABSTRACT

O objetivo dessa pesquisa foi relacionar as alterações no sistema hemostático com o uso contínuo dos anticoncepcionais orais e a ocorrência da trombose venosa profunda. Hemostasia é um processo fisiológico que tem como finalidade manter o sangue fluindo dentro dos vasos sanguíneos, assim evitando a formação de coágulos. Trombose venosa profunda é uma doença grave, caracterizada pela formação de coágulos em veias profundas, destacam-se os fatores de risco: hereditários, adquiridos e associação provável. Foi realizado um levantamento bibliográfico nas bases e banco de dados. Para a obtenção dos resultados foram analisados 11 artigos. Esses estudos demostram que estrogênio e progestagenios desencadeiam alterações significantes no sistema hemostático por sua ação androgênica, resultando na formação de fibrina, podendo acontecer à formação de coágulos nas veias. Devido os AOs ser o método mais utilizado no mundo, torna-se se suma importância o conhecimento das reações adversas consideradas graves, como a TVP.


Subject(s)
Venous Thrombosis
7.
Carbohydr Polym ; 134: 700-8, 2015 Dec 10.
Article in English | MEDLINE | ID: mdl-26428175

ABSTRACT

Two endo-ß-1,4-xylanases named XylT1 and XylT2, previously purified from Aspergillus terreus, were structurally investigated by fluorescence quenching and characterized with respect to their binding properties with phenolic compounds. Neutral and charged quenchers had access to both enzymes in neutral and alkaline pHs. The greatest access was noted for the negative quencher, possibly due to positive amino acid residues in the vicinity of tryptophan. These tryptophan environments may partially explain the conformational differences and lower binding constants of phenolic compounds for XylT2 than XylT1Phenolic compounds had lower binding constants for XylT2 than XylT1. These results show that xylanases present structural and functional differences, despite belonging to similar families. XylT1 and XylT2 were also evaluated for their ability to hydrolyze cellulose pulp in different stages of bleaching. Both enzymes promoted hydrolysis of cellulose pulps, which was confirmed by the release of total reducing sugars, pentoses and chromophoric material. Analysis of released xylooligosaccharides demonstrated a preferential release of xylobiose. None of xylanases released glucose, showing that they do not hydrolyze the cellulose present in the pulp, making both enzymes excellent choices for bio-bleaching applications.


Subject(s)
Aspergillus/enzymology , Cellulose/metabolism , Chemical Phenomena , Endo-1,4-beta Xylanases/chemistry , Endo-1,4-beta Xylanases/metabolism , Xylans/metabolism , Hydrolysis , Phenols/metabolism , Protein Conformation , Spectrometry, Fluorescence
8.
Biomed Res Int ; 2013: 148317, 2013.
Article in English | MEDLINE | ID: mdl-24294596

ABSTRACT

Hepatitis B is a liver inflammation caused by hepatitis B virus (HBV) and can be diagnosed in clinical stage by hepatitis B core antibody from IgM class (anti-HBcIgM). Hepatitis B core antibody from IgG class (Anti-HBcIgG) appears quickly after IgM, reaching high titers in chronic hepatitis, and remains even after cure. Since hepatitis B core antibody (anti-HBc) is the first antibody identified and sometimes the only marker detected during the course of infection, it can be used both to indicate HBV acute infection (anti-HBc-IgM) and to identify individuals who have come into contact with the virus (anti-HBc-IgG). In this work we propose a recombinant hepatitis B core multiepitope antigen (rMEHB) to be used for diagnosis of hepatitis B. For this purpose, a synthetic gene coding for rMEHB was designed and cloned into vector pET21a with a 6xHis tag at the C-terminal. Time course induction in E. coli showed an induced protein with an apparent molecular mass of ~21 kDa. Protein purification was performed by a single step with affinity chromatography Ni-NTA. Circular dichroism spectroscopy indicated rMEHB as a thermal stable protein at pH 7.0 and 8.0. In these conditions rMEHB was successfully used to perform an enzyme linked immuno sorbent assay (ELISA) with positive and negative sera.


Subject(s)
Epitopes , Hepatitis B/diagnosis , Recombinant Proteins , Amino Acid Sequence , Base Sequence , Circular Dichroism , Electrophoresis, Polyacrylamide Gel , Enzyme-Linked Immunosorbent Assay , Epitopes/chemistry , Epitopes/isolation & purification , Hepatitis B/immunology , Hepatitis B Core Antigens/chemistry , Hepatitis B Core Antigens/immunology , Hot Temperature , Humans , Immunoassay , Molecular Sequence Data , Protein Structure, Secondary , Protein Unfolding , Recombinant Proteins/chemistry , Recombinant Proteins/isolation & purification , Time Factors
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