Low quality of life and life-threatening conditions often demand pharmacological screening of lead compounds. A spectrum of pharmacological activities has been attributed to pyrazole analogs. The ...substitution, replacement, or removal of functional groups on a pyrazole ring appears consistent with diverse molecular interactions, efficacy, and potency of these analogs. This mini-review explores cytotoxic, cytoprotective, antinociceptive, anti-inflammatory, and antidepressant activities of some pyrazole analogs to advance structure-related pharmacological profiles and rational design of new analogs. Numerous interactions of these derivatives at their targets could impact future research considerations and prospects while offering opportunities for optimizing therapeutic activity with fewer adverse effects.
A palma tornou-se uma importante alternativa de forragem à pecuária bovina em meio às condições do semiárido, mas o ataque da cochonilha do carmim tem dificultado o cultivo da planta e a alimentação ...dos rebanhos. O presente estudo trata-se de uma revisão bibliográfica e tem como objetivo sistematizar e analisar os estudos referentes à situação de vulnerabilidade devido ao ataque da cochonilha do carmim no estado da Paraíba. Segundo as referências encontradas o ataque do inseto é caracterizado por prejuízos, a principal medida de controle tem sido o plantio de variedades de palma resistentes e o impacto sobre a pecuária bovina ainda é pouco abordado, demandando atenção dada à forte relação entre a atividade e os efeitos da praga. Por parte dos órgãos competentes as ações se dão de forma isolada e pontual, são insuficientes ao problema que deve ser encarado como demanda de política pública haja vista os severos impactos que a cochonilha do carmim causa à palma forrageira que repercutem nos rebanhos e nas famílias criadoras.
Resumo Fundsamento As sementes de Moringa oleifera , que são utilizadas para clarificação de água, contêm uma lectina chamada WSMoL que tem mostrado atividade antibacteriana e imunomoduladora in ...vitro . Devido ao seu valor nutritivo e potencial terapêutico, as folhas e as sementes dessa árvore são consumidas em algumas comunidades. Algumas lectinas de plantas não são tóxicas para mamíferos, mas tem sido relatado que outras são prejudiciais quando ingeridas ou administradas por outros meios. Objetivo Como um dos passos necessários para determinar a segurança de WSMoL, nós avaliamos os possíveis efeitos cardiotóxicos desta proteína purificada. Métodos Durante 21 dias consecutivos, a WSMoL foi administrada a camundongos por gavagem. Foram investigadas as funções eletrofisiológicas, mecânicas e metabólicas in vivo e ex vivo por meio de registros eletrocardiográficos, ressonância magnética nuclear e respirometria de alta resolução. Resultados O tratamento com WSMoL não induziu alterações nos níveis de glicose no sangue ou peso corporal em comparação com o grupo controle. Adicionalmente, as relações peso cardíaco/peso corporal e peso cardíaco/comprimento tibial estavam semelhantes em ambos os grupos. A ingestão de lectina também não modificou a tolerância à glicose ou resistência à insulina. Não foram observadas alterações nos parâmetros eletrocardiográficos ou na duração do potencial de ação cardíaco. Os corações dos camundongos dos grupos controle e WSMoL mostraram função ventricular esquerda preservada. Além disso, a WSMoL não induziu alterações na função mitocondrial (em todos os casos, p > 0,05). Conclusões A administração de WSMoL demonstrou ter um perfil de segurança cardíaca. Estes resultados contribuem à avaliação de segurança do uso de sementes de M. oleifera para tratar água, visto que essa lectina está presente na preparação empregada por algumas populações com esse fim. (Arq Bras Cardiol. 2020; online.ahead print, PP.0-0)
Circumsporozoite protein (CSP) is the primary pre-erythrocytic vaccine target in Plasmodium species. Knowledge about their genetic diversity can help predict vaccine efficacy and the spread of novel ...parasite variants. Thus, we investigated pvcsp gene polymorphisms in 219 isolates (136 from Brazilian Amazon BA, 71 from Rio de Janeiro Atlantic Forest AF, and 12 from non-Brazilian countries NB). Forty-eight polymorphic sites were detected, 46 in the central repeat region (CR), and two in the C-terminal region. Also, the CR presents InDels and a variable number of repeats. All samples correspond to the VK210 variant, and 24 VK210 subtypes based on CR. Nucleotide diversity (π = 0.0135) generated a significant number of haplotypes (168) with low genetic differentiation between the Brazilian regions (Fst = 0.208). The haplotype network revealed similar distances among the BA and AF regions. The linkage disequilibrium indicates that recombination does not seem to be acting in diversity, reinforcing natural selection's role in accelerating adaptive evolution. The high diversity (low Fst) and polymorphism frequencies could be indicators of balancing selection. Although malaria in BA and AF have distinct vector species and different host immune pressures, consistent genetic signature was found in two regions. The immunodominant B-cell epitope mapped in the CR varies from seven to 19 repeats. The CR T-cell epitope is conserved only in 39 samples. Concerning to C-terminal region, the Th2R epitope presented nonsynonymous SNP only in 6% of Brazilian samples, and the Th3R epitope remained conserved in all studied regions. We conclude that, although the uneven distribution of alleles may jeopardize the deployment of vaccines directed to a specific variable locus, a unique vaccine formulation could protect populations in all Brazilian regions.
Açaí (Euterpe oleracea Mart.) has recently emerged as a promising source of natural antioxidants. Despite its claimed pharmacological and nutraceutical value, studies regarding the effects of açaí in ...vivo are limited. In this study, we use the Caenorhabditis elegans model to evaluate the in vivo antioxidant properties of açaí on an organismal level and to examine its mechanism of action. Supplementation with açaí aqueous extract (AAE) increased both oxidative and osmotic stress resistance independently of any effect on reproduction and development. AAE suppressed bacterial growth, but this antimicrobial property did not influence stress resistance. AAE-increased stress resistance was correlated with reduced ROS production, the prevention of sulfhydryl (SH) level reduction and gcs-1 activation under oxidative stress conditions. Our mechanistic studies indicated that AAE promotes oxidative stress resistance by acting through DAF-16 and the osmotic stress response pathway OSR-1/UNC-43/SEK-1. Finally, AAE increased polyglutamine protein aggregation and decreased proteasome activity. Our findings suggest that natural compounds available in AAE can improve the antioxidant status of a whole organism under certain conditions by direct and indirect mechanisms.
Chitosan comprises polymeric macromolecules with technical and biological properties that have been used in biomedical healing applications requiring anti-microbial and anti-inflammatory capacities ...worldwide. In the tropical regions, green banana peel extract and andiroba oil are considered natural products with wound healing properties. The present study, for the first time, synthesized chitosan/green banana peel extract/andiroba oil (CGA) membranes and analyzed them using scanning electron microscopy (SEM) and the swelling and moisture tests. The CGA membranes together with control membranes of plain chitosan and chitosan plus green banana peel extract, were characterized by contact angle measurement, X-ray diffraction (XRD) and differential scanning calorimetry (DSC). Macroscopic analysis showed significant differences in color and transparency caused by the number of decoction days used for extract preparation and the oil content. SEM observations disclosed the formation of two phases, lipid and polymer, in the CGA. The number of decoction days and the andiroba oil content were inversely related to the swelling moisture uptake. All membranes were found to be hydrophilic with contact angles less than 90°. The incorporation of plant extract and oil promoted the appearance of related XRD peaks. DSC curves revealed a reduction in the enthalpy of the CGA membranes compared with plain chitosan, which might be attributed to the evaporation of the natural extract and oil. Based on these findings, the studied newly synthesized membranes demonstrated a potential for healing epithelial lesions.
O presente artigo investiga as concepções sobre Alfabetização Científica (AC) de professores de Ciências de 6º ao 9º ano da rede pública de um município do interior paulista em um contexto de ...formação continuada. Os dados foram coletados através de um questionário com perguntas abertas sobre a atividade da formação, as concepções dos professores antes e depois dessas atividades. Como resultados, alguns professores apresentaram mudanças de suas concepções sobre Alfabetização Científica no que diz respeito à necessidade de métodos científicos, nos permitindo apontar a necessidade de continuidade de pesquisas que contemplem esse tipo de abordagem bem como as formações continuadas de professores
Malaria was eliminated from southern and southeastern Brazil over 50 years ago. However, an increasing number of autochthonous episodes attributed to Plasmodium vivax have recently been reported from ...the Atlantic Forest region of Rio de Janeiro state. As the P vivax-like non-human primate malaria parasite species Plasmodium simium is locally enzootic, we performed a molecular epidemiological investigation to determine whether zoonotic malaria transmission is occurring.
We examined blood samples from patients presenting with signs or symptoms suggestive of malaria as well as from local howler monkeys by microscopy and PCR. Samples were included from individuals if they had a history of travel to or resided in areas within the Rio de Janeiro Atlantic Forest, but not if they had malaria prophylaxis, blood transfusion or tissue or organ transplantation, or had travelled to known malaria endemic areas in the preceding year. Additionally, we developed a molecular assay based on sequencing of the parasite mitochondrial genome to distinguish between P vivax and P simium, and applied this assay to 33 cases from outbreaks that occurred in 2015, and 2016.
A total of 49 autochthonous malaria cases were reported in 2015–16. Most patients were male, with a mean age of 44 years (SD 14·6), and 82% lived in urban areas of Rio de Janeiro state and had visited the Atlantic Forest for leisure or work-related activities. 33 cases were used for mitochondrial DNA sequencing. The assay was successfully performed for 28 samples, and all were shown to be P simium, indicative of zoonotic transmission of this species to human beings in this region. Sequencing of the whole mitochondrial genome of three of these cases showed that P simium is most closely related to P vivax parasites from South America. The malaria outbreaks in this region were caused by P simium, previously considered to be a monkey-specific malaria parasite, related to but distinct from P vivax, and which has never conclusively been shown to infect people before.
This unequivocal demonstration of zoonotic transmission, 50 years after the only previous report of P simium in people, leads to the possibility that this parasite has always infected people in this region, but that it has been consistently misdiagnosed as P vivax because of an absence of molecular typing techniques. Thorough screening of local non-human primates and mosquitoes (Anopheline) is required to evaluate the extent of this newly recognised zoonotic threat to public health and malaria elimination in Brazil.
Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado de Rio de Janeiro, The Brazilian National Council for Scientific and Technological Development (CNPq), JSPS Grant-in-Aid for scientific research, Secretary for Health Surveillance of the Brazilian Ministry of Health, Global Fund, Fundaçao de amparo à pesquisa do estado de Minas Gerais (Fapemig), and PRONEX Program of the CNPq.
O interesse na utilização de águas residuárias tem crescido, devido a limitação de água de boa qualidade, em destaque para o semiárido. Este trabalho teve por objetivo analisar as alterações químicas ...do solo irrigado com águas residuárias e da adubação fosfatada, na produção de muda de Moringa oleifera Lam. O experimento foi instalado em estufa, do viveiro florestal da Estação Experimental Prof. Ignácio Salcedo do Instituto Nacional do Semiárido – INSA, Campina Grande – Paraíba. Adotou-se o delineamento de blocos casualizados, arranjo fatorial 5 x 2, com quatro repetições, com cinco percentuais de água residual doméstica tratada, diluída em água de abastecimento (25%; 50%; 75%; 100% e água de abastecimento tratada), associados a dois fatores nutricionais (AF – adubação fosfatada e SA – sem adubação). Aos 110 dias após condução dos tratamentos, avaliaram-se as seguintes características do solo: potencial hidrogeniônico, condutividade elétrica, cálcio, magnésio, sódio, fósforo, potássio, soma de bases, alumínio, hidrogênio, sulfato, capacidade de troca catiônica e matéria orgânica. O uso da adubação fosfatada contribuiu de maneira positiva nos teores de fósforo, carbono, matéria orgânica e capacidade de troca catiônica do solo. Os percentis crescente de água residuária alavancaram a soma de bases e a capacidade de troca catiônica, simultaneamente promoveu o aumento nos teores de Na+, Al, H+Al e na condutividade elétrica do extrato de saturação do solo.
Leprosy is an infectious disease caused by Mycobacterium leprae and frequently resulting in irreversible deformities and disabilities. Ticks play an important role in infectious disease transmission ...due to their low host specificity, worldwide distribution, and the biological ability to support transovarial transmission of a wide spectrum of pathogens, including viruses, bacteria and protozoa. To investigate a possible role for ticks as vectors of leprosy, we assessed transovarial transmission of M. leprae in artificially-fed adult female Amblyomma sculptum ticks, and infection and growth of M. leprae in tick cell lines. Our results revealed M. leprae RNA and antigens persisting in the midgut and present in the ovaries of adult female A. sculptum at least 2 days after oral infection, and present in their progeny (eggs and larvae), which demonstrates the occurrence of transovarial transmission of this pathogen. Infected tick larvae were able to inoculate viable bacilli during blood-feeding on a rabbit. Moreover, following inoculation with M. leprae, the Ixodes scapularis embryo-derived tick cell line IDE8 supported a detectable increase in the number of bacilli for at least 20 days, presenting a doubling time of approximately 12 days. As far as we know, this is the first in vitro cellular system able to promote growth of M. leprae. Finally, we successfully transformed a clinical M. leprae isolate by inserting the reporter plasmid pCHERRY3; transformed bacteria infected and grew in IDE8 cells over a 2-month period. Taken together, our data not only support the hypothesis that ticks may have the potential to act as a reservoir and/or vector of leprosy, but also suggest the feasibility of technological development of tick cell lines as a tool for large-scale production of M. leprae bacteria, as well as describing for the first time a method for their transformation.
PDF
