CHEMICAL CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF HYDROETHANOLIC CRUDE EXTRACT OF EUGENIA FLORIDA DC (MYRTACEAE) LEAVES

Objective: The present study aimed to characterize and quantify the total phenolics, flavonoids and tannins in a hydroethanolic crude extract (70% (v/v) (EB)) of the leaves of E. florida DC, as well as to evaluate the antimicrobial activity of the extract against different species of micro-organisms.Methods: EB was characterized using a mass spectrometer equipped with a direct insertion device for in-stream injection (FIA). Quantitative analyses of major compounds were carried out by spectrophotometry. In addition, we evaluated the sensitivity profiles of different strains of yeast and bacteria against different concentrations of EB.Results: The classes found were in agreement with those described in the literature: flavonoids, tannins, phenolic acids and saponins. EB showed levels of phenolic compounds, flavonoids and tannins equal to 25.82 mg gallic acid equivalents per gram of extract (EAG/g), 8.42 mg quercetin equivalents per gram of extract (EQ/g) and 7.30 mg tannic acid equivalents per gram of extract (AT/g), respectively. In the analysis of antimicrobial activity, EB was more active against yeasts but was not effective against the bacteria used in the test.Conclusion: We can conclude that E. florida DC has antimicrobial potential, due to the presence of bioactive secondary metabolites.Keywords: Phenolics, Micro-organisms, Mass spectrometer, Yeasts, Bacteria, PotentialÂ

Antimicrobial properties of membrane-active dodecapeptides derived from MSI-78

Antimicrobial peptides (AMPs) are a class of broad-spectrum antibiotics known by their ability to disrupt bacterial membranes and their low tendency to induce bacterial resistance, arising as excellent candidates to fight bacterial infections. In this study we aimed at designing short 12-mer AMPs, derived from a highly effective and broad spectrum synthetic AMP, MSI-78 (22 residues), by truncating this peptide at the N- and/or C-termini while spanning its entire sequence with 1 amino add (aa) shifts. These designed peptides were evaluated regarding antimicrobial activity against selected gram-positive Staphylococcus strains and the gram-negative Pseudomonas aeruginosa (P. aeruginosa). The short 12-mer peptide CEM1 (GIGMFLKKAKICF) was identified as an excellent candidate to fight P. aeruginosa infections as it displays antimicrobial activity against this strain and selectivity, with negligible toxicity to mammalian cells even at high concentrations. However, in general most of the short 12-mer peptides tested showed a reduction in antimicrobial activity, an effect that was more pronounced for gram-positive Staphylococcus strains. Interestingly, CEM1 and a highly similar peptide differing by only one aa-shift (CEM2: IGKFLKKAKICFG), showed a remarkably contrasting AMP activity. These two peptides were chosen for a more detailed study regarding their mechanism of action, using several biophysical assays and simple membrane models that mimic the mammalian and bacterial lipid composition. We confirmed the correlation between peptide helicity and antimicrobial activity and propose a mechanism of action based on the disruption of the bacterial membrane permeability barrier

O Papel do ensino do português como língua estrangeira na defesa do multicultarismo

As política actuais existentes a nível oficial para a implementação e defesa do ensino da Língua Portuguesa como Língua Estrangeira (L. E.) na Europa e no resto do mundo levam-nos a pensar que são, sobretudo, os casos isolados de leitores portugueses pioneiros, inspirados e marginais que na sua missão individual e afastada lutam pela implementação e defesa desta língua nos seus países de acolhimento. Segundo Volfgram, “cabe ensinar a alguns que o multiculturalismo não está apenas na teoria e sim ao nosso redor, nos elevando realmente à condição de seres humanos” (2005), e o mesmo é dizer que o multiculturalismo começa nas suas bases pela aprendizagem desinteressada e não interesseira das crianças na sua mais tenra idade. Não é impunemente que em países multiculturais como a Bélgica, a Língua Portuguesa ensinada como segunda língua ou como língua estrangeira desempenha um papel preponderante na defesa e na preservação do Português e, em simultâneo, pugna pela defesa incontestável da necessidade incontornável que o multiculturalismo é hoje. É indubitável que a luta contra a xenofobia, a luta pela tolerância e o respeito mútuo, bem como o diálogo profícuo biunívoco não podem sobreviver actualmente sem uma consciencialização da importância das línguas minoritárias, da crioulização, da relação com as línguas maioritárias e da conquista da defesa do multiculturalismo hic et nunc. Abordando algumas opiniões avisadas, esperamos trazer à discussão temas importantes, tais como, a necessidade de articulação de políticas de difusão da língua portuguesa na Europa e no Mundo concertadamente com o Brasil e outros Países Lusófonos, a necessidade de implementação de medidas concretas no terreno para defesa da Língua de Camões fora de Portugal, a sobrevivência do Português que embora sendo minoritária na Europa é uma das línguas mais faladas no mundo, a necessidade da consciencialização para a crescente importância geo-estratégica do Português paralelamente com o recrudescimento do multiculturalismo à escala global

Genotoxic and Cytotoxic Safety Evaluation of Papain (Carica papaya L.) Using In Vitro Assays

Papain, a phytotherapeutic agent, has been used in the treatment of eschars and as a debriding chemical agent to remove damaged or necrotic tissue of pressure ulcers and gangrene. Its benefits in these treatments are deemed effective, since more than 5000 patients, at the public university hospital at Rio de Janeiro, Brazil, have undergone papain treatment and presented satisfactory results. Despite its extensive use, there is little information about toxic and mutagenic properties of papain. This work evaluated the toxic and mutagenic potential of papain and its potential antioxidant activity against induced-H2O2 oxidative stress in Escherichia coli strains. Cytotoxicity assay, Growth inhibition test, WP2-Mutoxitest and Plasmid-DNA treatment, and agarose gel electrophoresis were used to investigate if papain would present any toxic or mutagenic potential as well as if papain would display antioxidant properties. Papain exhibited negative results for all tests. This agent presented an activity protecting cells against H2O2-induced mutagenesis

Potential application of gelatin scaffolds prepared through in situ gas foaming in skin tissue engineering

Gelatin’s excellent foaming ability allows the application of in situ gas foaming as a preparation technique for porous scaffold development. Here, a new iterative experimental design for in situ gas foaming method is reported. The prepared scaffolds were studied for applying the findings to the future skin tissue engineering scaffolds. The thermal stability, mechanical properties, and pore structure of the scaffolds are reported and their degradation resistance by using collagenase enzyme and their cytotoxicity by using fibroblasts were studied. The results of this study demonstrated that gas foaming method can be modified to produce an interconnected porous structure with enhanced mechanical properties

A 17-mer Membrane-Active MSI-78 Derivative with Improved Selectivity toward Bacterial Cells

Antimicrobial peptides are widely recognized as an excellent alternative to conventional antibiotics. MSI-78, a highly effective and broad spectrum AMP, is one of the most promising AMPs for clinical application. In this study, we have designed shorter derivatives of MSI-78 with the aim of improving selectivity while maintaining antimicrobial activity. Shorter 17-mer derivatives were created by truncating MSI-78 at the N- and/or C-termini, while spanning MSI-78 sequence. Despite the truncations made, we found a 17-mer peptide, MSI-78(4-20) (KFLKKAKKFGKAFVKIL), which was demonstrated to be as effective as MSI-78 against the Gram-positive Staphylococcus strains tested and the Gram-negative Pseudomonas aeruginosa. This shorter derivative is more selective toward bacterial cells as it was less toxic to erythrocytes than MSI-78, representing an improved version of the lead peptide. Biophysical studies support a mechanism of action for MSI-78(4-20) based on the disruption of the bacterial membrane permeability barrier, which in turn leads to loss of membrane integrity and ultimately to cell death. These features point to a mechanism of action similar to the one described for the lead peptide MSI-78

Chemical Composition and Evaluation of Antitumoral Activity of Leaf and Root Essential Oils of Conyza canadensis (Asteraceae)

The leaf and root oils of Conyza canadensis were studied for chemical composition and antitumor activity. The results showed that there is great variation in the composition of the oils obtained from different parts. The main components in the leaf oil were limonene, caryophyllene oxide and espatulenol. In the root oil the major component was the acetylenic ester lachnophyllum methyl ester. It was observed that according to the collection time (6 and 16 hours), significant variations in the content of the main components of this essential oil of leaves can occur. Limonene, spatulenol and caryophyllene oxide presented a distribution of 61% / 5.4% / 12.5% ​​and 38% / 10.7% / 22.3% in oils obtained from plants collected at 6 and 16 hours, respectively. The antitumor activity of the oils showed that leaf oil had a greater potential for inhibition, and this oil was distinguished by the activity against neoplastic cell lines K562 (leukemia) and NCI-ADR / RES (ovary with multidrug resistance phenotype ) with TGI values ​​of 16.8 and 19.0 mg.mL-1, respectively. Comparing the leaf oils and their tumor cell inhibition potentials, it was noted that this activity is higher in the oil with higher contents of monoterpene limonene. DOI: http://dx.doi.org/10.17807/orbital.v11i5.137

It Takes Two to Tango, Part II : Synthesis of A-Ring Functionalised Quinones Containing Two Redox-Active Centres with Antitumour Activities

In 2021, our research group published the prominent anticancer activity achieved through the successful combination of two redox centres (ortho-quinone/para-quinone or quinone/seleniumcontaining triazole) through a copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. The combination of two naphthoquinoidal substrates towards a synergetic product was indicated, but not fully explored. Herein, we report the synthesis of 15 new quinone-based derivatives prepared from click chemistry reactions and their subsequent evaluation against nine cancer cell lines and the murine fibroblast line L929. Our strategy was based on the modification of the A-ring of paranaphthoquinones and subsequent conjugation with different ortho-quinoidal moieties. As anticipated, our study identified several compounds with IC50 values below 0.5 µM in tumour cell lines. Some of the compounds described here also exhibited an excellent selectivity index and low cytotoxicity on L929, the control cell line. The antitumour evaluation of the compounds separately and in their conjugated form proved that the activity is strongly enhanced in the derivatives containing two redox centres. Thus, our study confirms the efficiency of using A-ring functionalized para-quinones coupled with ortho-quinones to obtain a diverse range of two redox centre compounds with potential applications against cancer cell lines. Here as well, it literally takes two for an efficient tango

Cross-cultural adaptation of the City Birth Trauma Scale for the Brazilian context

Background: Posttraumatic stress disorder consists of a set of symptoms that occurs in response to one or more traumatic events and can occur in postpartum, from traumatic situations related to the birth or to the baby’s health in the first days of life. It is important tracking the presence of birth trauma, but there is not available instruments in the Brazilian context for this purpose. Objectives: To present the cross-cultural adaptation of City Birth Trauma Scale (BiTS) into Brazilian portuguese. Methods: Cross-cultural adaptation involved independent translations, synthesis,back-translation, and submission to the original author’s appreciation. After the scale was subjected to face validity, followed by a pilot study with postpartum mothers. Results: All steps were performed for the cross-cultural adaptation. Regarding face validity, items evaluated concerning different types of equivalence, presented satisfactory agreement values (≥4.20). Most of the expert’s suggestions were followed, being the main ones related to adjustments in prepositions, pronouns and verbal subjects. Pilot study showed that the mothers had been able to understand and respond to the instrument without adjustments. Discussion: BiTS’s Brazilian version proved to be cross-culturally adapted, ensuring the possibility of intercultural data comparison from the semantic, idiomatic, cultural, and conceptual perspectives. New studies are being conducted to attest its psychometric adequac