145 research outputs found

    Automação de Escritórios e Secretariado

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    O presente projeto tem como objetivo: o estudo das expectativas de expatriados da América Latina em relação ao processo de expatriação. Tais expectativas podem ocasionar dificuldade de adaptação ao país anfitrião e à sua cultura ou até mesmo a repatriação antecipada, significando a falha e rompimento do contrato. A pesquisa apresenta uma discussão inicial com embasamento teórico que contextualiza as dificuldades que podem ser encontradas pelo futuro expatriado no país anfitrião e que muitas vezes são ignoradas devido às expectativas ou à falta de informações suficientes antes da concretização da expatriação. A metodologia é constituída por uma pesquisa bibliográfica e de levantamento utilizando questionários para coleta de dados das pessoas que trabalham com, ou, se tornaram expatriados. Este estudo tem como justificativa contribuir para que as empresas auxiliem o expatriado com todas as informações necessárias antes da mudança para o novo país, evitando assim que expectativas irreais sejam criadas, atrapalhando sua adaptação. Além disso, este trabalho pode tornar-se um referencial aos futuros expatriados que se interessarem em se preparar para este processo longo e desafiador que é a expatriação

    In vitro evaluation of alkaline lignins as antiparasitic agents and their use as an excipient in the release of benznidazole

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    Copyright © 2023. Published by Elsevier B.V.The Amazon rainforest is considered the largest tropical timber reserve in the world. The management of native forests in the Amazon is one of the most sensitive geopolitical issues today, given its national and international dimension. In this work, we obtained and characterized physicochemical lignins extracted from branches and leaves of Protium puncticulatum and Scleronema micranthum. In addition, we evaluated in vitro its potential as an antioxidant, cytotoxic agent against animal cells and antiparasitic against promastigotes of Leishmania amazonensis, trypomastigotes of T. cruzi and against Plasmodium falciparum parasites sensitive and resistant to chloroquine. The results showed that the lignins obtained are of the GSH type and have higher levels of guaiacyl units. However, they show structural differences as shown by spectroscopic analysis and radar charts. As for biological activities, they showed antioxidant potential and low cytotoxicity against animal cells. Antileishmanial/trypanocidal assays have shown that lignins can inhibit the growth of promastigotes and trypomastigotes in vitro. The lignins in this study showed low anti-Plasmodium falciparum activity against susceptible strains of Plasmodium falciparum and were able to inhibit the growth of the chloroquine-resistant strain. And were not able to inhibit the growth of Schistosoma mansoni parasites. Finally, lignins proved to be promising excipients in the release of benznidazole. These findings show the potential of these lignins not yet studied to promote different biological activities.publishersversionpublishe

    Biological activities and physicochemical characterization of alkaline lignins obtained from branches and leaves of Buchenavia viridiflora with potential pharmaceutical and biomedical applications

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    Funding Information: The study was funded by Foundation for the State of Pernambuco (Process - FACE-04.03/19 ), AP Researcher Research Grant - FACEPE (Process BFP-0038-0 ) and National Council for Scientific and Technological Development grant - CNPq (Process 306865/2020-3 ). This research was also funded by the Foundation for Science and Technology (FCT) through the GHTM ( UID/04413/2020 ). Thanks to MR4, who provided us with the Plasmodium falciparum strains that we used in the assays. We also thank the Laboratory of Magnetic Resonance of the Institute of Chemistry and Biotechnology (Federal University of Alagoas- UFAL) for the analysis of NMR. In addition to these, we would also like to thank Mil Madeiras Preciosas, a subsidiary of the Swiss group Precious Woods ( http://preciouswoods.com.br/ ) for providing samples of branches and leaves of Buchenavia viridiflora. Publisher Copyright: © 2022In this work, we investigated in vitro different biological activities of alkaline lignins extracted from the species Buchenavia viridiflora, a tree from the Amazon rainforest used as a wood product. The chemical composition results for the twig and leaves were, respectively (%): cellulose (30.88 and 24. 28), hemicellulose (21.62 and 23.03), lignin (29.93 and 25.46), extractives (13.06 and 20.52), and ash (4.51 and 6.72). The yield was higher for the lignin of the branches (67.9 %) when compared to the leaves (60.2 %). Lignins are of the GSH type, low molecular weight and thermally stable. They promoted moderate to low antioxidant activity, highlighting the lignin of the branches, which presented an IC50 of 884.56 μg/mL for the DPPH assay and an IC50 of 14.08 μg/mL for ABTS. In the cytotoxicity assays, they showed low toxicity against macrophage cells (IC50 28.47 and 22.58 μg/mL). In addition, they were not cytotoxic against splenocytes and erythrocytes at concentrations ranging from 100 to 6.25 μg/mL. These were able to promote splenocyte proliferation and induce the production of anti-inflammatory cytokines. And inhibit the growth of tumor cells with IC50 ranging from 12.63 to values >100 μg/mL and microbial at a concentration of 512 μg/mL. Finally, they showed antiparasitic activity by inhibiting the growth of chloroquine-sensitive and resistant Plasmodium falciparum strains. These findings reinforce that the lignins in this study are promising for potential pharmaceutical and biomedical applications.publishersversionpublishe

    an in vitro approach

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    Funding Information: The authors thank the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) for a grant and M.C.A. Lima Fellowship (Process 306865/612020-3); Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES—Finance Code N° 001) and the Fundação de Amparo à Ciência e Tecnologia do Estado de Pernambuco (FACEPE). J.V.R. Rocha and I.J. Cruz Filho would like to thank FACEPE for the Graduate Scholarship (Process PBPG-1832-4.01/22) and Researcher Fixation Scholarships (Process BFP-0038-4.03/21), respectively. In addition, M.C.A. Lima and A.L. Aires would like to thank FACEPE Research Project Aid (Process APQ-0498-4.03/19) and (Process APQ-Emergent 1181-4.03/22), respectively. We would like to thank Mil Madeiras Preciosas, a subsidiary of the Swiss group Precious Woods ( http://preciouswoods.com.br/ ) for supplying the Clarisia racemosa trunks. Thanks to MR4, who provided us with the Plasmodium falciparum MRA-1029 strain provided by Andrew Talman, Robert Sinden that we used in the trials. The work was partially supported by the FCT project reference CIRCNA/BRB/0281/2019_AMAZING and GHTM-UID/Multi/04413/2013. Funding Information: The authors thank the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) for a grant and M.C.A. Lima Fellowship (Process 306865/612020-3); Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES—Finance Code N° 001) and the Fundação de Amparo à Ciência e Tecnologia do Estado de Pernambuco (FACEPE). J.V.R. Rocha and I.J. Cruz Filho would like to thank FACEPE for the Graduate Scholarship (Process PBPG-1832-4.01/22) and Researcher Fixation Scholarships (Process BFP-0038-4.03/21), respectively. In addition, M.C.A. Lima and A.L. Aires would like to thank FACEPE Research Project Aid (Process APQ-0498-4.03/19) and (Process APQ-Emergent 1181-4.03/22), respectively. We would like to thank Mil Madeiras Preciosas, a subsidiary of the Swiss group Precious Woods (http://preciouswoods.com.br/) for supplying the Clarisia racemosa trunks. Thanks to MR4, who provided us with the Plasmodium falciparum MRA-1029 strain provided by Andrew Talman, Robert Sinden that we used in the trials. The work was partially supported by the FCT project reference CIRCNA/BRB/0281/2019_AMAZING and GHTM-UID/Multi/04413/2013. Publisher Copyright: © 2023, King Abdulaziz City for Science and Technology.Clarisia racemosa Ruiz & Pav is a neotropical species found in humid forests from southern Mexico to southern Brazil. There are few studies related to the ethnopharmacological use of C. racemosa. Our objective was to evaluate the hydroalcoholic extract of C. racemosa as a potential antiparasitic agent. For this, we performed in vitro assays against strains of Leishmania amazonensis, Trypanosoma cruzi, Plasmodium falciparum, and Schistosoma mansoni. At the same time, immunomodulatory activity tests were carried out. The results demonstrated that the extract was able to stimulate and activate immune cells. In preliminary antiparasitic tests, structural modifications were observed in the promastigote form of L. amazonensis and in adult worms of S. mansoni. The extract was able to inhibit the growth of trypomastigote form of T. cruzi and finally showed low antiparasitic activity against strains of P. falciparum. It is pioneering work and these results demonstrate that C. racemosa extract is a promising alternative and contributes to the arsenal of possible forms of treatment to combat parasites.publishersversionpublishe

    Estrutura, reatividade e propriedades biológicas de hidantoínas

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    Hydantoin (imidazolidine-2,4-dione) is a 2,4-diketotetrahydroimidazole discovered by Baeyer in 1861. Thiohydantoins and derivatives were prepared, having chemical properties similar to the corresponding carbonyl compounds. Some biological activities (antimicrobial, anticonvulsant, schistosomicidal) are attributed to the chemical reactivity and consequent affinity of hydantoinic rings towards biomacromolecules. Therefore, knowledge about the chemistry of hydantoins has increased enormously. In this review, we present important aspects such as reactivity of hydantoins, acidity of hydantoins, spectroscopy and cristallographic properties, and biological activities of hydantoin and its derivatives

    Anti-inflammatory and antinociceptive activities of indole–imidazolidine derivatives

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    AbstractNon-steroidal anti-inflammatory drugs (NSAIDs) represent a group of approximately 50 different medicines that are widely prescribed for the management of inflammation and that exhibit variable anti-inflammatory, anti-pyretic and analgesic activities. Most NSAIDs also exhibit a shared set of adverse effects, particularly related to gastrointestinal complications; thus, the development of new drugs for the treatment of chronic inflammation and pain continues to be an issue of high interest. Hydantoin and indole derivatives are reported to possess various pharmacological effects, including anti-inflammatory and analgesic activities. Therefore, the aim of this study was to evaluate the potential anti-inflammatory and antinociceptive activities of hybrid molecules containing imidazole and indole nuclei. The anti-inflammatory activities of 5-(1H-Indol-3-yl-methylene)-2-thioxo-imidazolidin-4-one (LPSF/NN-56) and 3-(4-Bromo-benzyl)-5-(1H-indol-3-yl-methylene)-2thioxo-imidazolidin-4-one (LPSF/NN-52) were evaluated using air pouch and carrageenan-induced peritonitis models as well as an acetic acid-induced vascular permeability model followed by IL-1β and TNF-α quantification. To evaluate the antinociceptive activities of the compounds, acetic acid-induced nociception, formalin and hot plate tests were also performed. The anti-inflammatory activities of the compounds were evidenced by a reduction in both leukocyte migration and the release of TNF-α and IL-1β in air pouch and peritonitis models. Upon acetic acid-induced nociception, a decrease in the level of abdominal writhing in the groups treated with LPSF/NN-52 (52.1%) or LPSF/NN-56 (63.1%) was observed. However, in the hot plate test, none of the derivatives tested exhibited an inhibition of nociception. These results indicate that the compounds tested exhibited promising anti-inflammatory and antinociceptive activities that likely involved the modulation of the immune system

    In silico studies (ADME) and in vitro evaluation of the cytotoxic and antimicrobial properties of thiosemicarbazones and thiazole compounds

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    The thiosemicarbazones and thiazoles are known for their versatility of biological activities, among which we can mention: antioxidant, antimicrobial, anticancer activity and the ability to interact with biological macromolecules, HSA and DNA. This study presented two series of molecules 4-(3-(4-nitrophenyl)-4-phenylthiazol-2(3H)-ylidene)-hydrazine)-methyl)-phenol and 4-(3-(4-chlorophenyl)-4 -phenylthiazol-2(3H)-ylidene)-hydrazine)-methyl)-phenol with biological potential against different microorganisms. The in silico ADME profile showed that thiosemicarbazones and thiazoles have good oral bioavailability. The cytotoxicity results in J774 macrophages cells showed that the compounds showed toxicity ranging from 49.15 to 61.28 µM for thiosemicarbazones and from 10.75 to 39.76 µM for thiazoles. Finally, all thiosemicarbazones and thiazoles synthesized were also able to inhibit microbial growth. In yeasts of the genus Candidas sp. we obtained close results ranging from 12.5 to 50 µg/mL. This study demonstrates that the compounds assessed have the potential to be antimicrobial agents in vitr

    Study of the Activity of 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one against Schistosomiasis Mansoni in Mice

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    Previous studies conducted with the imidazolidinic derivative 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one (LPSF-PT05) show outstanding activity against adult Schistosoma mansoni worms in vitro. In the first phase of this study, S. mansoni-infected mice were treated, orally, with 100 mg/Kg of the LPSF-PT05 in three formulations: Tween 80 and saline solution, oil/water (70 : 30) emulsion, and solid dispersion with polyethylene glycol (PEG). In the second phase, three other doses of the LPSF-PT05 in PEG were tested: 3, 10, 30 mg/kg. These treatment regimens significantly reduced the number of recovered worms due to increases in the solubility of the compound in this formulation; the greatest reduction (70.5%) was observed at the dose of 100 mg/kg. There was no changes in the pattern of mature egg compared to immature eggs; however there was a significant increase in the number of dead eggs. Histopathological analysis of liver tissue showed changes in morphological aspects of the hepatic parenchyma with decrease exudative-productive hepatic granuloma stages, although we found no significant differences in IFN-γ, IL-4, IL-10, or NO production in response to the specific antigen SEA. The results show the derivative LPSF-PT05 to be a potential candidate in the etiological treatment of schistosomiasis with a possible dampening effect of the granulomatous process

    GQ-16, a TZD-derived partial PPARγ agonist, induces the expression of thermogenesis- related genes in brown fat and visceral white fat and decreases visceral adiposity in obese and hyperglycemic mice

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    Background Beige adipocytes comprise a unique thermogenic cell type in the white adipose tissue (WAT) of rodents and humans, and play a critical role in energy homeostasis. In this scenario, recruitment of beige cells has been an important focus of interest for the development of novel therapeutic strategies to treat obesity. PPARγ activation by full agonists (thiazolidinediones, TZDs) drives the appearance of beige cells, a process so-called browning of WAT. However, this does not translate into increased energy expenditure, and TZDs are associated with weight gain. Partial PPARγ agonists, on the other hand, do not induce weight gain, but have not been shown to drive WAT browning. The present study was designed to investigate the effects of GQ-16 on BAT and on browning of WAT in obese mice. Methods Male Swiss mice with obesity and hyperglycemia induced by high fat diet were treated with vehicle, rosiglitazone (4 mg/kg/d) or the TZD-derived partial PPARγ agonist GQ-16 (40 mg/ kg/d) for 14 days. Fasting blood glucose, aspartate aminotransferase, alanine aminotransferase and lipid profile were measured. WAT and brown adipose tissue (BAT) depots were excised for determination of adiposity, relative expression of Ucp-1, Cidea, Prdm16, Cd40 and Tmem26 by RT-qPCR, histological analysis, and UCP-1 protein expression analysis by immunohistochemistry. Liver samples were also removed for histological analysis and determination of hepatic triglyceride content. Results GQ-16 treatment reduced high fat diet-induced weight gain in mice despite increasing energy intake. This was accompanied by reduced epididymal fat mass, reduced liver triglyceride content, morphological signs of increased BAT activity, increased expression of thermogenesis- related genes in interscapular BAT and epididymal WAT, and increased UCP-1 protein expression in interscapular BAT and in epididymal and inguinal WAT. Conclusion This study suggests for the first time that a partial PPARγ agonist may increase BAT activity and induce the expression of thermogenesis-related genes in visceral WAT. General Significance These findings suggest that PPARγ activity might be modulated by partial agonists to induce WAT browning and treat obesity

    Synthesis, Dna Binding, And Antiproliferative Activity Of Novel Acridine-thiosemicarbazone Derivatives.

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    In this work, the acridine nucleus was used as a lead-compound for structural modification by adding different substituted thiosemicarbazide moieties. Eight new (Z)-2-(acridin-9-ylmethylene)-N-phenylhydrazinecarbothioamide derivatives (3a-h) were synthesized, their antiproliferative activities were evaluated, and DNA binding properties were performed with calf thymus DNA (ctDNA) by electronic absorption and fluorescence spectroscopies. Both hyperchromic and hypochromic effects, as well as red or blue shifts were demonstrated by addition of ctDNA to the derivatives. The calculated binding constants ranged from 1.74 × 10(4) to 1.0 × 10(6) M(-1) and quenching constants from -0.2 × 10(4) to 2.18 × 10(4) M(-1) indicating high affinity to ctDNA base pairs. The most efficient compound in binding to ctDNA in vitro was (Z)-2-(acridin-9-ylmethylene)-N- (4-chlorophenyl) hydrazinecarbothioamide (3f), while the most active compound in antiproliferative assay was (Z)-2-(acridin-9-ylmethylene)-N-phenylhydrazinecarbothioamide (3a). There was no correlation between DNA-binding and in vitro antiproliferative activity, but the results suggest that DNA binding can be involved in the biological activity mechanism. This study may guide the choice of the size and shape of the intercalating part of the ligand and the strategic selection of substituents that increase DNA-binding or antiproliferative properties.1613023-1304
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