The Amazon rainforest has wide and unique biodiversity, which is an important source of natural products for the development of drugs. Neglected tropical diseases (NTDs) represent a major health problem as they affect over 1 billion people, especially vulnerable populations living in tropical and subtropical regions. Currently available drugs are generally inadequate for the majority of these diseases, thus, there is an urgent need for new treatments. The present review aims to summarize up-to-date and comprehensive information on the efficacy of the Amazon plants, about treating certain neglected tropical diseases. According to the literature information, several compounds (phenolics, alkaloids, terpenoids and steroids, among others) which were isolated from plants of the Amazon forest showed in vitro activity against Leishmania sp., Trypanosoma cruzi, the parasites responsible for leishmaniasis and Chagas disease, respectively. Moreover, extracts, and essential oil from certain plants were reported to have mosquito repellent and insecticidal activities against Aedes aegypti, the vector of dengue, and chikungunya. This review demonstrated that the Amazonian rainforest is endowed with pharmacologically active plants which can be used as a starting point for the development of new drugs against NTDs, such as leishmaniasis, Chagas disease, dengue, chikungunya.
Neglected Tropical Diseases (NTDs) and infectious illnesses, such as malaria, tuberculosis and Zika fever, represent a major public health concern in many countries and regions worldwide, especially in developing ones. They cause thousands of deaths per year, and certainly compromise the life of affected patients. The drugs available for therapy are toxic, have considerable adverse effects, and are obsolete, especially with respect to resistance. In this context, targeted peptides are considered promising in the design of new drugs, since they have specific action and reduced toxicity. Indeed, there is a rising interest in these targeted compounds within the pharmaceutical industry, proving their importance to the Pharmaceutical Sciences field. Many have been approved by the Food and Drug Administration (FDA) to be used as medicines, plus there are more than 300 peptides currently in clinical trials. The main purpose of this review is to show the most promising potential targeted peptides acting as hits molecules in NTDs and other infectious illnesses. We hope to contribute to the discovery of medicines in this relatively neglected area, which will be extremely useful in improving the health of many suffering people.
Background: Zika fever affects poor and vulnerable populations, presenting cycles observed in, at least, 86 countries, with no vaccine prevention or treatment available. It is known that genus Flavivirus causes Zika Virus (ZIKV), as Dengue and Yellow Fever, whose genetic material decodes, among other proteins, a series of non-structural (NS) proteins essential for viral replication, such as NS2B-NS3 protease. Additionally, chemical and biological systems are commonly studied using molecular modeling approaches allowing, among several other processes, to elucidate mechanisms of action, molecule reactivity and/or chemical properties and the design of new drugs. Thus, considering the in silico complexes between the biological target and the bioactive molecule, it is possible to understand better experimental results based on molecular properties, which are compared with the findings of the biological activity. Objective: Accordingly, this study aimed to present computational docking simulations of five previously reported active peptides against NS2B-NS3 protease of ZIKV and analyze some quantum chemical properties to identify the main contribution to improve the action. Methods: The compounds were described by Rut and coworkers (2017) and Hill and coworkers (2018), which were submitted to docking simulation in Gold software and quantum chemical properties calculations in Wavefunction Spartan software. Results: Total energy, electrophilicity index (ω) and energy gap (GAP) appeared to be the best properties to justify the peptides biological activity. Moreover, the most promising compound (P1, Km 4.18 M) had the best value of total energy (-2763.04001 au), electrophilicity index (8.04 eV) and GAP (6.49 eV), indicating an energetically favorable molecule with good interaction with the target and, when compared to other peptides, presented moderate reactivity. P4 showed the highest electrophilicity index value (28.64 eV) which was justified the interaction ability visualized in the docking simulation. However, its GAP value (4.24 eV) was the lowest in the series, suggesting high instability, possibly validating its low biological activity value (Km 19 uM). Considering that, GAP was important to understand the chemical instability, and high values can promote damage to biological response. Conclusion: Furthermore, it was also noted that high electron affinity, related to electrophilicity index, promoted electron accepting characteristic, which was important to improve the biological activity of the peptides. A larger compound series have to studied in order to access features more precisely. However, these results have paramount importance to guide future effort in this extremely-need health area.
Os Cursos de Férias de Morfofisiologia Humana têm sido realizados desde 2012 para estudantes do ensino médio das escolas públicas do Trairi, no estado do Rio Grande do Norte. O presente trabalho objetivou demonstrar os seus resultados positivos no auxílio à educação. Métodos criativos, participativos e inovadores foram utilizados, a partir do desenvolvimento de jogos, dinâmicas e peça teatral. Foram aplicados questionários aos participantes para avaliar quais temas os alunos gostariam de conhecer durante o curso, e o método empregado. Na edição de 2017, participaram 32 alunos, os quais demonstraram preferências em estudar o funcionamento do coração, do cérebro, das células e tecidos. A maioria avaliou como “muito bom” (> 70%) os itens: ambiente do laboratório, incentivo à criatividade, desempenho dos monitores e metodologia do curso. Esses cursos estimularam o desenvolvimento de competências e habilidades dos estudantes, contribuindo para o desenvolvimento social e o espírito crítico na formação do indivíduo.
Background: Arylindole derivatives are promising scaffolds in the design of new drugs. These scaffolds exhibit a wide biological activity, including inhibition of COX-2, antitumor activity, receptor GABA agonism, and estrogen receptor modulation. Objective: Taking this into account, this paper presents a study to understand the inhibitory action of certain 2-arylindole derivatives, specifically a series of 2,3-diarylindoles with IC50 values from 0.006 nM to 100 nM, on the COX-2 enzyme and supports its structural-activity relationship (SAR) through molecular docking simulations. Methods: Applying molecular modelling, especially molecular docking, we assessed the SAR of a series of 2,3-arylindoles derivatives in the COX-2 enzyme. Results: The results indicated that Gly 526 and Phe 381 residues are relevant for improving inhibitory activity on para-substituted 3-phenyl- compounds. Arg 120 was also demonstrated to be an important residue for COX-2 inhibition since it enables a π-cation interaction with the best compound in series A5 (experimental IC50 = 0.006 nM determined in advance). Furthermore, COX-2 presents flexibility in some regions of the active site to adequately accommodate 5-substituted compounds containing an indole ring. Conclusion: Therefore, such structural features can be used as support for further Structural-Based Drug Design (SBDD) and/or Ligand-Based Drug Design (LBDD) studies on new selective COX-2 inhibitors. other: Not applicable.
Resumo: O presente trabalho tem como objetivo discutir a presença de unidades de conservação em Goiás e no Distrito Federal como ferramenta para atividades no âmbito da educação ambiental no Cerrado, com ênfase nas unidades de conservação do tipo parque nacional. Sabe-se que a apropriação do Cerrado acontece há tempos e por diferentes atores. Parte significante dessa apropriação é realizada por atores que degradam o ambiente do Cerrado, como a agropecuária. Este trabalho visa analisar a prática da educação ambiental em unidades de conservação e a importância para a conservação do Cerrado. Foi realizada uma fundamentação teórica acerca do conceito de Cerrado e suas características, assim como uma discussão sobre unidades de conservação e educação ambiental. Além disso, há uma breve análise histórica, social e física das características das unidades de conservação selecionadas e do Cerrado. Palavras-chave: unidade de conservação; Cerrado; educação ambiental. Summary: This paper aims to discuss the creation of conservation units in Goiás and the Federal District as a tool for activities in the field of Environmental Education in the Cerrado, with emphasis on national park type conservation units. It is known that the appropriation of the Cerrado has been happening for a long time and by different actors. A significant part of this appropriation is performed by actors that degrade the Cerrado environment, such as agriculture. This paper aims to analise the practice of environmental education in conservations units and the importance to Cerrado's conservation. A theoretical basis was made about the concept of Cerrado and its characteristics, as well as a discussion about conservation units and environmental education. In addition, there is a brief historical, social and physical analysis of the characteristics of selected protected areas and the Cerrado.
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