Potencial alelopático de ésteres derivados do ácido cinâmico

Resumo A síntese e determinação estrutural de ésteres derivados do ácido cinâmico permitiu obter análogos dos ésteres naturais isolados de Lafoensia glyptocarpa Koehne e avaliar o potencial alelopático dos mesmos através de bioensaios de germinação de sementes de alface e tomate. As substâncias que promoveram maior inibição da germinação das sementes analisadas foram: 3,4-metilenodioxifenil acrilato de hexadecila; 3,4-metilenodioxifenil propionato de hexadecila; 3,4-metilenodioxi-6-nitrofenil propionato de hexadecila; e ferrulato de sitosterila. As estruturas foram determinadas através da análise de dados fornecidos por espectrometria de infravermelho, de massas e de RMN de 1H e 13C

CURCUMIN, THE GOLDEN POWDER FROM TURMERIC: INSIGHTS INTO CHEMICAL AND BIOLOGICAL ACTIVITIES

Turmeric, obtained from the dried rhizomes of Curcuma longa (Zingiberaceae), is a golden colored material, commonly used around the world for seasoning and coloring food dishes. Since antiquity, turmeric has been widely used in the treatment of several diseases in traditional Chinese and Indian medicine (Ayurveda), where it is also known by other names such as Kanchani (goddess gold) or also Gauri (having a bright and luminous face), a designation stemming from the gilded appearance of the plant material. Curcumin, the main chemical component of turmeric, is responsible both for its properties as dyes as well as its biological activities. This diarylheptanoid was first isolated almost two centuries ago and had its chemical structure determined in 1910 as being diferuloylmethane. Subsequently, more detailed and relevant data were obtained furthering the understanding of structural features of curcumin. The classical methodology for the synthesis of curcumin and other curcuminoids was described in 1960 by Pabon. Subsequently, different variations on this methodology have been developed, culminating with the synthesis of different curcuminoids. Several studies have been published in recent years on the biological activities exhibited by curcumin including its antioxidant, antitumor, anti-inflammatory, antiviral, antibacterial, antifungal, antimalarial and leishmanicidal activities

Design, Synthesis and Trypanocidal Evaluation of Novel 1,2,4-Triazoles-3-thiones Derived from Natural Piperine

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Piperina como suplemento fitogênico na dieta de frangos de corte

The objective of this work was to determine the effect of piperine as a phytogenic additive in chicken broiler diet. Seven‑day‑old male chicks were randomly allocated in four experimental treatments (n = 24), with four replicates (n = 6). The piperine was added to diets at concentrations of 0, 60, 120, and 180 mg kg-1 for 35 consecutive days. The following were evaluated: biochemical, hematological and histopathological parameters; performance and carcass yield. Histomorphometric analyses were also carried out. The addition of 120 and 180 mg kg-1 of piperine did not alter broiler body weight and feed conversion, whereas 60 mg kg-1 of piperine interfered positively in both parameters from 36 to 42 days of age and significantly increased the absorption surface of the duodenum and the ileum. No macroscopic alteration in organ size and color was observed in the broilers fed diets with the evaluated concentrations of piperine. The supplementation of 120 and 180 mg kg-1 of piperine is toxic to liver tissue and reduces the absorption surface of the jejune. The diet supplemented with 60 mg kg-1 of piperine is safe.O objetivo deste trabalho foi determinar o efeito da piperina, como suplemento fitogênico, na dieta de frangos de corte. Pintos com sete dias de idade foram distribuídos aleatoriamente em quatro tratamentos (n = 24), com quatro repetições (n = 6). A piperina foi adicionada na ração nas concentrações de 0, 60, 120 e 180 mg kg-1 por 35 dias consecutivos. Foram avaliados: parâmetros bioquímicos, hematológicos e histopatológicos; desempenho e rendimento de carcaça. Também foram realizadas análises histomorfométricas. A adição de 120 e 180 mg kg-1 de piperina não alterou o peso corpóreo e a conversão alimentar dos frangos, enquanto 60 mg kg-1 de piperina interferiram positivamente em ambos os parâmetros, de 36 a 42 dias de idade, e aumentaram significativamente a superfície de absorção do duodeno e do íleo. Não foi observada alteração macroscópica no tamanho e na coloração dos órgãos dos frangos alimentados com as rações com as concentrações de piperina avaliadas. A suplementação com 120 e 180 mg kg-1 de piperina é tóxica ao tecido hepático e reduz a superfície de absorção do jejuno. A dieta suplementada como 60 mg kg-1 de piperina é segura

2-Chloro-4,6-bis{(E)-3-methoxy-4-[(4-methoxybenzyl)oxy]styryl}pyrimidine: Synthesis, Spectroscopic and Computational Evaluation

A novel curcumin analog namely 2-chloro-4,6-bis{(E)-3-methoxy-4-[(4-methoxybenzyl)oxy]- styryl}pyrimidine (compound 7) was synthesized by three-step reaction. The condensation reaction of protected vanillin with 2-chloro-4,6-dimethylpyrimidine (6) was the most efficient step, resulting in a total yield of 72%. The characterization of compound 7was performed by 1Hand 13C nuclearmagnetic resonance (NMR), as well as high-resolution mass spectrometry. The experimental spectrometric data were compared with the theoretical spectra obtained by the density functional theory (DFT) method, showing a perfectmatch between them.UV-visible spectroscopy and steady-state fluorescence emission studies were performed for compound 7 in solvents of different polarities and the results were correlated with DFT calculations. Compound 7 showed a solvatochromism effect presenting higher molar extinction coefficient (log " = 4.57) and fluorescence quantum yield ( = 0.38) in toluene than in acetonitrile or methanol. The simulation of both frontier molecular orbitals (FMOs) and molecular electrostatic potential (MEP) suggested that the experimental spectra profile in toluene was not interfered by a possible charge transfer. These results are an indication of a low probability of compound 7 in reacting with unsaturated phospholipids in future applications as a fluorescent dye in biological systems

COVID-19 Infection and Neuropathological Features

The pathology associated with COVID-19 infection is progressively being revealed. Recent postmortem assessments have revealed acute airway inflammation as well as diffuse alveolar damage, which bears resemblance to severe acute respiratory syndromes induced by both SARS-CoV and MERS-CoV infections. Although recent papers have highlighted some neuropathologies associated with COVID-19 infection, little is known about this topic of great importance in the area of public health. Here, we discuss how neuroinflammation related to COVID-19 could be triggered by direct viral neuroinvasion and/or cytokine release over the course of the infection

2-Nitro-1-vinyl-1H-imidazole

Nitroimidazoles are pharmacophoric groups responsible for important antiparasitic activity against several infectious diseases. 2-Nitroimidazoles are found in some antiparasitic drugs and are one of the main moieties responsible for the biological activities exhibited. As an example, we can mention the drug benznidazole, the only drug available in Brazil for the treatment of Chagas disease. This work describes an efficient methodology for the synthesis of 2-nitro-1-vinyl-1H-imidazole through a simple and direct approach, as well as its full characterization and biological assessment. The antiparasitic evaluation of 2-nitro-1-vinyl-1H-imidazole against Trypanosoma cruzi (Tulahuen C2C4-LacZ strain) showed IC50 = 4.8 μM on amastigotes and low cytotoxicity against LLC-MK2 cells (IC50 > 500 μM), validating 2-nitro-1-vinyl-1H-imidazole as a biologically active structural subunit for anti-T. cruzi activity. The results presented herein demonstrate that 2-nitro-1-vinyl-1H-imidazole can be easily obtained, possessing great potential for use in the design of new antichagasic drugs through a molecular hybridization strategy using known coupling reactions

2-Nitro-1-vinyl-1<i>H</i>-imidazole

Nitroimidazoles are pharmacophoric groups responsible for important antiparasitic activity against several infectious diseases. 2-Nitroimidazoles are found in some antiparasitic drugs and are one of the main moieties responsible for the biological activities exhibited. As an example, we can mention the drug benznidazole, the only drug available in Brazil for the treatment of Chagas disease. This work describes an efficient methodology for the synthesis of 2-nitro-1-vinyl-1H-imidazole through a simple and direct approach, as well as its full characterization and biological assessment. The antiparasitic evaluation of 2-nitro-1-vinyl-1H-imidazole against Trypanosoma cruzi (Tulahuen C2C4-LacZ strain) showed IC50 = 4.8 μM on amastigotes and low cytotoxicity against LLC-MK2 cells (IC50 > 500 μM), validating 2-nitro-1-vinyl-1H-imidazole as a biologically active structural subunit for anti-T. cruzi activity. The results presented herein demonstrate that 2-nitro-1-vinyl-1H-imidazole can be easily obtained, possessing great potential for use in the design of new antichagasic drugs through a molecular hybridization strategy using known coupling reactions

The Sweet Side of Fungal Infections: Structural Glycan Diversity and Its Importance for Pathogenic Adaptation

Fungal infections are the most common secondary infections in debilitated individuals in a state of chronic disease or immunosuppression. Despite this, most fungal infections are neglected, mainly due to the lower frequency of their more severe clinical forms in immunocompetent individuals with a healthy background. However, over the past few years, several cases of severe fungal infections in healthy individuals have provoked a change in the epidemiological dynamics of fungal infections around the world, both due to recurrent outbreaks in previously infrequent regions and the greater emergence of more pathogenic fungal variants affecting healthy individuals, such as in the Cryptococcus genus. Therefore, before the arrival of a scenario of prevalent severe fungal infections, it is necessary to assess more carefully what are the real reasons for the increased incidence of fungal infection globally. What are the factors that are currently contributing to this new possible epidemiological dynamic? Could these be of a structural nature? Herein, we propose a discussion based on the importance of the virulence factors of glycoconjugate composition in the adaptation of pathogenic fungal species into the current scenario of increasing severity of these infections