Avaliação do perfil epidemiológico da tuberculose e a sua coinfecção TB-HIV nos estados da Paraíba e Rio Grande do Norte/ Evaluation of the epidemiological profile of tuberculosis and its TB-HIV coinfection in the states of Paraíba and Rio Grande do Norte

Houve o aumento dos casos de Tuberculose (TB) na região nordeste nos últimos anos. Este estudo retrospectivo de caráter epidemiológico tem por objetivos abranger as notificações por ano do diagnóstico sobre a tuberculose e a sua coinfecção TB-HIV nos estados da Paraíba- PB e Rio Grande do Norte- RN no período entre 2014-2018. Trata-se de uma pesquisa qualitativa, quantitativa, descritiva, baseada em coleta de dados secundários, obtidos através do SINAN. O estado da Paraíba teve mais casos de tuberculose notificados em relação ao RN, em relação aos casos de óbitos 4,1% (253) no RN apresentou com maior mortalidade. O dobro de casos na faixa etária de 15-24 anos de 1,13% (68) no RN em relação a PB com apenas 0,56% (36) com a prevalência do sexo masculino em ambos. A confirmação do diagnóstico laboratorial foi predominante na PB com 61,92%, sendo a 1ª baciloscopia que apresentou maior significância nos dois estados. O perfil da Coinfecção TB-HIV foi evidenciado no estado do RN que revelou um número maior de casos positivos com a coinfecção de 10,23% (616). Demonstrou-se que na PB há maiores número de cepas resistentes a Rifampicina (Rifamp) através do Teste Molecular Rápido para Tuberculose (TRM). Uma boa parte dos casos de coinfecção TB-HIV não recebe terapia antirretroviral nestes estados. Sugere-se então, a realização de estudos retrospectivos epidemiológicos posteriores para a validação dos dados disponíveis para a sociedade devido aos desafios e limitações encontrados para reduzir os casos de TB a nível regional e interestados

Avaliação da atividade antifúngica do geraniol sobre candida albicans e candida tropicalis isoladas de conteúdo pulmonar

Recently, an increase in the number of hospital infections caused by Candida yeasts have been occurring, with a notable growing number of infections caused by non-albicans species, in addition to the already frequent cases caused by albicans species. The forms of superficial candidiasis may evolve to its systemic form, affecting different organs and being able to reach the lower airways, composing a condition of disseminated pulmonary candidiasis of complex diagnostic, difficult treatment and high mortality. As a way to obtain new therapeutic options in the combat against these infections, natural products of vegetal origin holds high scientific value due to their wide quantity of different substances of varied phytochemical classes. One of these classes, the monoterpenes, stands out for showing multiple biological activities of medical interest. Up to these premises, the antifungal activity of geraniol, a monoterpene, against strains of Candida albicans and Candida tropicalis was evaluated through in vitro assays: Determination of Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC), study of the substance effect on the fungal micromorphology, evaluation of the substance effect on the kinetics of microbial growth (time-kill) and association assay between geraniol and standard antifungal agent (amphotericin B). On the antifungal activity assays, the geraniol displayed MIC of 64 μg/mL and MFC of 256 μg/mL. The monoterpene also exhibited efficacy in inhibiting the appearance of virulence structures such as pseudohyphae and promote intense decrease of blastoconids in the micromorphology assay. On the time-kill assay, the monoterpene showed dose-dependent fungicide activity by inhibiting the growth of nearly 99% of the yeasts tested by the end of the 24 h period, with growth inhibition efficiency proportional to the concentration used. The association between geraniol and amphotericin B did not displayed synergism nor antagonism, being characterized as indifferent for not showing disparity between the association MIC and the substance’s isolated MIC. In conclusion, the monoterpene geraniol displayed important activity of fungicide character inhibiting the appearance of fungal virulence and resistance structures with efficacy depending directly on the concentration used, but without acting in synergism alongside the standard antifungal agent.NenhumaNas últimas décadas, tem ocorrido um aumento nos casos de infecções hospitalares provocadas por leveduras do gênero Candida, com notável crescimento da ocorrência de espécies não-albicans, além dos casos já frequentes provocados pela espécie albicans. As formas superficiais de candidíase são capazes de evoluir para a forma sistêmica afetando diferentes órgãos, podendo atingir as vias aéreas inferiores, compondo um quadro de candidíase disseminada pulmonar de diagnóstico complexo, difícil tratamento e alta mortalidade. Como meio de se obter novas opções terapêuticas no combate a estas infecções, os produtos naturais de origem vegetal possuem alto valor científico por oferecem uma vasta quantidade de diferentes substâncias de variadas classes fitoquímicas. Uma destas classes, os monoterpenos, se destacam por apresentar múltiplas atividades biológicas de interesse médico. Diante destas premissas, foi avaliada a atividade antifúngica do geraniol, um monoterpeno, contra cepas de Candida albicans e Candida tropicalis por meio de ensaios realizados in vitro: Determinação da Concentração Inibitória Mínima (CIM) e Concentração Fungicida Mínima (CFM), estudo do efeito do fitoconstituinte sobre a micromorfologia fúngica, avaliação do efeito da substância sobre a cinética de crescimento microbiano (time-kill) e ensaio de associação entre o geraniol e antifúngico-padrão (anfotericina B). Nos ensaios de atividade antifúngica, o geraniol apresentou CIM de até 64 μg/mL e CFM de até 256 μg/mL. O monoterpeno também demonstrou eficácia em inibir o aparecimento de estruturas de virulência como pseudo-hifas e causar acentuada diminuição de blastoconídios no ensaio de efeito sobre micromorfologia fúngica. No ensaio de cinética de morte microbiana (time-kill), o monoterpeno demonstrou atividade fungicida concentração-dependente ao inibir o crescimento de aproximadamente 99% das leveduras testadas ao final do período de 24 h, com eficácia de inibição de crescimento diretamente proporcional a concentração utilizada. A associação entre o geraniol e a anfotericina B não apresentou sinergismo ou antagonismo, sendo caracterizada como indiferente por não serem observadas divergências entre a CIM da associação e a CIM de cada substância isolada. Em conclusão, o geraniol apresentou importante atividade fungicida, inibindo surgimento de estruturas de resistência e virulência fúngicas com eficácia dependendo diretamente da concentração utilizada, porém, sem atuar em sinergismo com antifúngico-padrão

Preparação de derivados do lapachol em meio ácido e em meio básico: uma proposta de experimentos para a disciplina de Química Orgânica Experimental Preparation of lapachol derivatives in acid and base media: proposed experiments for Organic Chemistry laboratory classes

<abstract language="eng">In this educational paper we describe the extraction of lapachol from its natural source according to acid-base concepts in organic chemistry and the use of its derivatives &#946;-lapachone and hydroxy-hydrolapachol to exemplify intramolecular cyclization, carbocation stability, Michael addition reaction and chromatography. The experiments were performed during three different undergraduate organic chemistry laboratory classes using low cost material, while avoiding color reagents for TLC visualization, as well as small-scale column chromatography to isolate the mixture of lapachol and &#946;-lapachone

Preparação de derivados do lapachol em meio ácido e em meio básico: uma proposta de experimentos para a disciplina de Química Orgânica Experimental

In this educational paper we describe the extraction of lapachol from its natural source according to acid-base concepts in organic chemistry and the use of its derivatives &#946;-lapachone and hydroxy-hydrolapachol to exemplify intramolecular cyclization, carbocation stability, Michael addition reaction and chromatography. The experiments were performed during three different undergraduate organic chemistry laboratory classes using low cost material, while avoiding color reagents for TLC visualization, as well as small-scale column chromatography to isolate the mixture of lapachol and &#946;-lapachone

Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis

Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro-N-(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae, evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use

Antibacterial effect of isoeugenol against Pseudomonas aeruginosa

Pseudomonas aeruginosa&nbsp;is an important nosocomial pathogen and its clinical importance is mainly related to nosocomial infections. Increased rates of bacterial resistance in recent years has led WHO to publish a global priority list to guide research and discovery of new antibiotics, where&nbsp;P. aeruginosa&nbsp;is among the group of bacteria for which there is a critical level of priority for new drugs to be discovered.&nbsp;In this context, isoeugenol appears as an interesting alternative and the objective of this study was to investigate its action against&nbsp;P. aeruginosa. Isoeugenol presented significant antibacterial activity, with minimum inhibitory concentration (MIC) of 64µg/mL and minimum bactericidal concentration (MBC) of 128µg/mL, and was considered bactericidal against this species. Molecular docking revealed interactions that suggest that isoeugenol may bind to the enzyme Penicillin-Binding Protein 3 and interfere with the bacterial cell wall synthesis process. This study reinforces the antibacterial potential of this compound and emphasizes that more studies are needed in order to better investigate its mechanism of antibacterial action

(R)-(+)-β-Citronellol and (S)-(−)-β-Citronellol in Combination with Amphotericin B against Candida Spp.

The enantiomers (R)-(+)-&beta;-citronellol and (S)-(&minus;)-&beta;-citronellol are present in many medicinal plants, but little is understood about their bioactivity against Candida yeasts. This study aimed to evaluate the behavior of positive and negative enantiomers of &beta;-citronellol on strains of Candida albicans and C. tropicalis involved in candidemia. The minimum inhibitory concentration (MIC) and minimum fungicide concentration (MFC) were determined. The evaluation of growth kinetics, mechanism of action, and association studies with Amphotericin B (AB) using the checkerboard method was also performed. R-(+)-&beta;-citronellol and S-(&minus;)-&beta;-citronellol presented a MIC50% of 64 &micro;g/mL and a MFC50% of 256 &micro;g/mL for C. albicans strains. For C. tropicalis, the isomers exhibited a MIC50% of 256 &micro;g/mL and a MFC50% of 1024 &micro;g/mL. In the mechanism of action assay, both substances displayed an effect on the fungal membrane but not on the fungal cell wall. Synergism and indifference were observed in the association of R-(+)-&beta;-citronellol and AB, while the association between S-(&minus;)-&beta;-citronellol and AB displayed synergism, additivity, and indifference. In conclusion, both isomers of &beta;-citronellol presented a similar profile of antifungal activity. Hence, they can be contemplated in the development of new antifungal drugs providing that further research is conducted about their pharmacology and toxicity