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Metal oxide engineered nanomaterials (ENMs) in study influenced soil function and microbes, but we found no evidence that changes were caused exclusively by a nano-size effect.

The main risk factor for chronic obstructive pulmonary disease (COPD) is cigarette smoke (CS). It can alter many immune cells functions such as phagocytosis, efferocytosis and cytokine production. Cytokines play a role in the orchestration of inflammation in COPD. The JAK/STAT pathways are among the most important signalling components of cytokines. The objective of this work was to investigate the role of the JAK/STAT pathway with regard to cytokine release and microsphere uptake capacity (to minimize the non-specific scavenging) in human monocyte-derived-macrophages (MDMs). The MDMs were stimulated by cigarette smoke extract (CSE) alone or in combination with lipopolysaccharide (LPS). CSE alone was not associated with significant changes in the cytokine, with the exception of IL-8/CXCL8 production. However, CSE disturbed cytokine production in LPS-stimulated MDMs. CSE increase CXCL-8 and CCL2 release in LPS-stimulated monocyte-derived macrophages and suppressed the production of IL-6 and CXCL1 in these cells. CSE also decreased microsphere uptake capacity by MDMs. Then, CSE + LPS-stimulated MDMs were treated with two different JAK inhibitors. AG490 (specific inhibitor of JAK2) and ruxolitinib (inhibitor of JAK1 and JAK2). JAK/STAT inhibitors, particularly ruxolitinib, attenuated in cytokine production without completely inhibiting when compared with dexamethasone. On the other hand, the cells exposed to dexamethasone are nearly unable to capture the microspheres, while both JAK inhibitors do not affect the uptake capacity. In summary, our results showed the versatility of ruxolitinib which might bring a better balance disturbance of cytokine release and uptake capacity. The information regarding the distinctive effect of JAK/STAT inhibitors may be useful in the development of novel treatments for COPD.

Microgrooved surfaces are recognized as an important strategy of tissue engineering to promote the alignment of bone cells. In this work, we have investigated the mechanical and morphological aspects of osteoblasts cells after interaction with different micro-structured polymeric surfaces. Femtosecond laser writing technique was used for the construction of circular and parallel microgrooved patterns in biocompatible polymeric surfaces based on pentaerythritol triacrylate. Additionally, we have studied the influence of the biocompatible TiO

In the present study, we examined the antinociceptive and anti-inflammatory activities of a guanylhydrazone derivative, (E)-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-guanylhydrazone hydrochloride (LQM10), in mice. The antinociceptive effect was determined by assessing behavioural responses in different pain models, while anti-inflammatory activity was examined in carrageenan-induced pleurisy. Intraperitoneal LQM10 administration reduced the acetic acid-induced nociceptive behaviour, a phenomenon which was unaltered by pretreatment with yohimbine, atropine, naloxone, or glibenclamide. In the formalin assay, LQM10 reduced nociceptive behaviour only in the second phase, indicating an inhibitory effect on inflammatory pain. LQM10 did not alter the pain latency in the hot plate assay and did not impact the locomotor activity of mice in the rotarod assay. In the carrageenan-induced pleurisy assay, LQM10 treatment inhibited critical events involved in inflammatory responses, namely, leucocyte recruitment, plasma leakage, and increased inflammatory mediators (tumour necrosis factor [TNF]-α and interleukin [IL]-1β) in the pleural exudate. Overall, these results indicate that LQM10 exhibits antinociceptive effects associated with peripheral mechanisms and anti-inflammatory activity mediated via a reduction in leucocyte migration and proinflammatory mediators, rendering this compound a promising candidate for treating pain and inflammatory process.

The identification of bacteria plays an essential role in multiple areas of research. Those areas include experimental biology, food and water industries, pathology, microbiology, and evolutionary ...

The use of plants and their products for medical treatment is a quite common procedure in Brazil, especially for treatment of diabetes. In fact, several plants can demonstrate hypoglycemic effects in vitro assays. However, the use for human treatment requires the knowledge of their toxicological properties. The aim of this study was to evaluate the effect of protein extracts of Chrysobalanus icaco collected from natural habitats and of Eugenia astringens acquired from the market in Rio de Janeiro on the viability and migration of fibroblasts. E. astringens has a similar morphology as C. icaco and it is sold as Chrysobalanus in a popular market. Being a different plant, E. astringens expresses different proteins, and its protein extract has proved to possess higher toxic properties than C. icaco does. Cytotoxicity assays indicated that, as the protein extract concentration increases, fibroblast viability decreases. Only the E. astringens extract displayed cytotoxicity at all concentrations, in addition to reduced fibroblast migration. The results obtained in this study demonstrates that it is necessary integrative policies for rational use of medicinal plants and their commercialization, since the current use of medicinal plants may be inadequate, and it is of great importance for Public Health.

International audience

Cinnamic acids and their derivatives are found in abundance in fruits, vegetables, and other food products of plant origin. The trans-cinnamic and p-coumaric acids in particular have been a subject...

Bowdichia virgilioides Kunth (Fabaceae) is a tree species used in folk medicine against inflammatory disorders, and it is still unclear whether consumption of the B. virgilioides stem bark extract has any effect on immune cells. Thus, this study aimed to evaluate the effects of B. virgilioides stem bark extract (AEBv) on the functions of the thymus and B lymphocytes. The AEBv was obtained by decoction and administrated orally once a day in male mice for 7 days. After treatment, thymi were obtained for morphology analysis, relative weight, cellularity and deposition of laminin. Thymocytes obtained from control and treated animals were submitted to adhesion and migration assays followed by immunophenotyping. Also, mesenteric lymph nodes were removed, and the lymphoid cells were obtained to measure B cell proliferation and cytokine production. Mice treated with AEBv and their controls were also immunized with sheep red blood cells (SRBC), and 8 days post immunization the sera were collected to perform antibody titration using hemagglutination assays. AEBv administration decreased thymus weight and cellularity and increased the laminin deposition without any significant effect on the expression of the laminin receptor VLA-6 in the thymus microenvironment. Additionally, thymocytes of AEBv-treated mice showed reduced adhesion and migration on laminin substrates, and the B lymphocytes showed reduced proliferation, enhanced IL-10 secretion, decreased TNF-α production, and attenuated anti-SRBC antibody production. These findings showed that AEBv intake might cause modulatory effects on the functions of thymocytes and B-lymphocytes, contributing to the treatment of immune diseases. Key words: Thymocytes, cell migration, cell adhesion, immunosuppression, B cell.

Rice is the third most important crop worldwide. Unfortunately, in most rice-producing countries, crop residues are burned, increasing emissions of greenhouse gases and toxic compounds. Incorporation of rice straw (RS) into the soil, either or not accompanied by a microbial inoculum, may offer a viable alternative. However, the effects of such treatments on soil, including the microbial community structure and function in the next crop cycle, still remain largely unknown. Here, we studied the effect of four different RS management strategies (leaving RS as mulch with or without a microbial inoculum, incorporation of RS into the soil with microbial inoculum, and RS burning) on rice growth and flowering-stage rhizosphere microbiomes. The relevant microbiomes were examined by amplicon sequencing based on the 16S rRNA and ITS1 gene regions. In comparison to the zero situation, all four treatments tended to increase the soil organic carbon content, albeit without significant differences. Furthermore, none of the treatments had major effects on either (rice) crop yield or phytopathogen incidence in the next cycle. However, leaving RS as a mulch incited a decrease in soil pH, and showed a trend of reducing yield by up to 1 ton·ha−1. Moreover, the different RS treatments affected the structures and predicted functions of the bacteriomes and fungomes in the rice rhizosphere. The mulching treatment was associated with an enhanced abundance of Acidobacteria, particularly Bryobacter spp. In contrast, the non-mulch treatments incited raised abundances of GammaProteobacteria, Bacteroidia and Campylobacteria. The rice rhizosphere fungomes, consisting mostly of Ascomycota, were less affected by the treatments, although the microbial inoculum was shown to drive the respective fungome structures.

Societal Impact Statement Colombia is a “megadiverse” country with vast natural resources. A history of recent conflict means that information is only now being collected on the natural capital of regions that were previously unexplored. Better access to data, tools, and expertise is required for evidence‐supported decisions on the conservation of these resources. The development of a bespoke cyberinfrastructure could help fulfill this need by providing access to digital resources in a collaborative cyberenvironment. We outline key priorities and develop a reference framework for building cyberinfrastructure in Colombia. This framework could be applied to other fields and countries to promote knowledge exchange, scientific innovation, and socioeconomic growth.

International audience; Inflammasomes are protein complexes that produce IL-1β in response to damage or pathogens. As such, inflammasomes are involved in several types of hepatic fibrosis. However, the mechanisms by which these complexes drive the liver's fibrogenic status remain unclear. We co-cultured differentiated macrophages (the THP-1 cell line or human monocyte-derived macrophages (MDMs)) with human hepatic fibroblasts (either the LX-2 cell line or primary human hepatic stellate cells (HSCs)). The inflammasome pathway was activated with lipopolysaccharide (LPS) and monosodium urate (MSU) crystals, and the HSCs' responses were analyzed. Our results show that co-culture of HSCs with THP-1 cells upregulated transcription of the genes coding for metalloproteinase (MMP)-3 and MMP-9. After inflammasome pathway activation, the HSCs' phenotype was the same in the presence of THP-1 cells or MDMs (i.e. upregulation of MMP-3, MMP-9, and the pro-inflammatory cytokine IL-1β). We found that two cytokines were involved in these changes IL-1β regulated MMP-3 and IL-1β mRNA expression, whereas TNF-α regulated MMP-9 mRNA expression. Experiments with primary cells revealed that a general inflammatory environment is responsible for the downregulation of pro-fibrotic markers. Our present results suggest that inflammasome pathway activation in macrophages leads to a pro-inflammatory environment for HSCs leading to MMP/TIMP imbalance and enhanced fibrolytic properties.

Obituary

Macrophages are key cells in the immune inflammatory response that can be differentiated into M1 and M2 phenotypes. Polarization has a critical therapeutic value, especially in diseases in which an M1/M2 imbalance plays a pathophysiological role. Raman spectroscopy has proven to be a promising bioanalytical technique for discriminating different cell types. However, to our knowledge, its application to identify the functional polarization of macrophages into M1 or M2 cells is yet to be investigated. In this work, Raman spectroscopy was applied to the analysis of macrophage polarization, and the spectral datasets were analyzed using principal component analysis (PCA). In vitro, resting J774.1 macrophages were treated with LPS/IFN-γ to induce the M1 phenotype or with IL-4 to induce the M2 phenotype. The resulting Raman spectra showed sufficient biochemical information to distinguish between M1 and M2 phenotypes when analyzed by PCA, reflecting the changes in cell markers caused by differentiation. The Raman spectra collected from LPS-stimulated M1 and M2 macrophages were more intense. The functional phenotype of M1 macrophages was confirmed by IL-6 secretion and TNF-α mRNA expression, while M2 macrophages produced IL-10 and Arg-1 mRNA, as well as by the morphological changes observed by scanning electron microscopy. Taken together, the results indicate that Raman spectroscopy combined with PCA analysis is a useful tool to identify the functional phenotypes of macrophages, providing an alternative way to distinguish between cells in distinct differentiation stages.

International audience; Inflammatory lung disease results in a high global burden of death and disability. There are no effective treatments for the most severe forms of many inflammatory lung diseases, such as chronic obstructive pulmonary disease, emphysema, corticosteroid-resistant asthma, and coronavirus disease 2019; hence, new treatment options are required. Here, we review the role of oxidative imbalance in the development of difficult-to-treat inflammatory lung diseases. The inflammation-induced overproduction of reactive oxygen species (ROS) means that endogenous antioxidants may not be sufficient to prevent oxidative damage, resulting in an oxidative imbalance in the lung. In turn, intracellular signaling events trigger the production of proinflammatory mediators that perpetuate and aggravate the inflammatory response and may lead to tissue damage. The production of high levels of ROS in inflammatory lung diseases can induce the phosphorylation of mitogen-activated protein kinases, the inactivation of phosphoinositide 3-kinase (PI3K) signaling and histone deacetylase 2, a decrease in glucocorticoid binding to its receptor, and thus resistance to glucocorticoid treatment. Hence, antioxidant treatment might be a therapeutic option for inflammatory lung diseases. Preclinical studies have shown that antioxidants (alone or combined with anti-inflammatory drugs) are effective in the treatment of inflammatory lung diseases, although the clinical evidence of efficacy is weaker. Despite the high level of evidence for the efficacy of antioxidants in the treatment of inflammatory lung diseases, the discovery and clinical investigation of safer, more efficacious compounds are now a priority.

Two lanthanide complexes supported on MCM48 type silica have been synthetized to introduce a new concept of multi-stimuli responsive materials for anti-counterfeiting applications. This new technology provides a simple and secure way of storing information with different levels of security from biocompatible materials. Different luminescent patterns can be revealed and suppressed by external stimuli: addition and removal of a specific reagent (chemical stimulus) followed by UV exposure to reveal the characteristic luminescence of the material and heat treatment (physical stimulus) to suppress the red luminescence of the material. The chemical stimulus occurs from the complexation of β-diketone 4,4,4-trifluoro-1-phenyl-1,3-butadione (BTFA) in the Eu(H2O)nL–SiO2 (L = chelidamic acid or trimesic acid) printed hybrid and can be made via insertion of the ligand by soaking the label using a marker pen. Physical stimuli can occur through a portable heat gun. The complexation with BTFA enhances the Eu-luminescence through the antenna effect under exposure to common UV-light. Heating (∼145 °C) for a few seconds rapidly quenches the luminescence of the label and, after some cycles of heating–cooling, BTFA sublimates and leads to complete quenching of the red luminescence. The combination of chemical and physical stimuli provides two levels of security verification and unbreakable encryption.

International audience; AIM: Hydroxycinnamic acids their derivatives have various pharmacological properties. The hydroxycinnamic acid derivatives, methyl cinnamate, trans-cinnamic, and p-coumaric acids have been the object of study in the treatment of skin wounds. However, it is unclear whether these derivatives exert a direct beneficial effect on fibroblast function. In this study, we evaluated the effects of methyl cinnamate, trans-cinnamic, and p-coumaric acids on fibroblast migration in vitro. MATERIALS AND METHODS: NIH 3T3 and L929 fibroblast cell lines were exposed to each drug at several concentrations and the effect on cell viability, cell cycle, and extracellular matrix production were assessed by MTT assay, flow cytometry, and immunofluorescence staining, respectively. The effect on cell migration was examined using scratch assay. RESULTS: The results showed that hydroxycinnamic acid derivatives not affect cell viability, but increase fibroblast migration in the in vitro scratch-wound healing assay. They also induced an increase in S and G2/M phases accompanied by a decrease in the G0/G1 phase of the cell cycle. The cell proliferation inhibitor mitomycin C abolished the effect induced by p-coumaric acid and methyl cinnamate, indicating that only the trans-cinnamic acid stimulated migration. A transwell migration assay confirmed that trans-cinnamic acid-treated fibroblasts exhibited increased migration compared with untreated cells. trans-Cinnamic acid-induced fibroblast migration was decreased by PKA inhibitor and p38-MAPK inhibitor but not by JNK inhibitor. Additionally, trans-cinnamic acid-treated fibroblasts showed an increase in the production of laminin and collagen type I. CONCLUSION: Our study showed that trans-cinnamic acid improves fibroblast migration and modulates extracellular matrix synthesis, indicating its potential for accelerating the healing process.

INTRODUCTION: Leprosy is a chronic infectious disease caused by Mycobacterium leprae.This study aimed to analyze the epidemiological, temporal, and spatial dynamics ofleprosy in a municipality in northeastern Brazil. METHODS: This is an ecological study on new leprosy cases in the population of Arapiraca (Alagoas, Northeast Region, Brazil), from 2008 to 2017. Data extracted from a national database were analyzed forepidemiological indicators, factors associated with physical disabilities, and spatialanalysis in the neighborhoods of Arapiraca. RESULTS: A total of 292 new cases of leprosy were recorded, particularly occurring among the following groups: women, the age group of 46-59 years, brown-skinned individuals, people with less than eight years of schooling, and urban residents; the new cases were also predominantly the tuberculoid form and were of the paucibacillary classification of the disease. Almost 1/3 of the people had some degree of physical disability, which was mainly associated with the group 60 years of age and older, black ethnicity, and the multibacillary clinical form of leprosy. The joinpoint regression showed a stationary temporal behavior of indicators. There was a heterogeneous spatial distribution with active transmission areas, especially in the neighborhoods Primavera, Baixão, Ouro Preto, and downtown. CONCLUSIONS: The epidemiological indicators revealed complexity in the process of leprosy development. These spatial and temporal studies are relevant to help in the planning, monitoring, and guidance of interventions in the municipality. The spatial analysis showed heterogeneous distribution in the analyzed neighborhoods.

International audience; Uvaol is a natural pentacyclic triterpene that is widely found in olives and virgin olive oil, exerting various pharmacological properties. However, information remains limited about how it affects fibroblasts and endothelial cells in events associated with wound healing. Here, we report the effect of uvaol in the in vitro and in vivo healing process. We show the positive effects of uvaol on migration of fibroblasts and endothelial cells in the scratch assay. Protein synthesis of fibronectin and laminin (but not collagen type I) was improved in uvaol-treated fibroblasts. In comparison, tube formation by endothelial cells was enhanced after uvaol treatment. Mechanistically, the effects of uvaol on cell migration involved the PKA and p38-MAPK signaling pathway in endothelial cells but not in fibroblasts. Thus, the uvaol-induced migratory response was dependent on the PKA pathway. Finally, topical treatment with uvaol caused wounds to close faster than in the control treatment using experimental cutaneous wounds model in mice. In conclusion, uvaol positively affects the behavior of fibroblasts and endothelial cells, potentially promoting cutaneous healing.

Cinnamic acids and their derivatives are found in abundance in fruits, vegetables, and other food products of plant origin. The

Cyclo-Gly-Pro (CGP) attenuates nociception, however its effects on salivary glands remain unclear. In this study, we investigated the acute effects of CGP on salivary flow and composition, and on the submandibular gland composition, compared with morphine. Besides, we characterized the effects of naloxone (a non-selective opioid receptor antagonist) on CGP- and morphine-induced salivary and glandular alterations in mice. After that, in silico analyses were performed to predict the interaction between CGP and opioid receptors. Morphine and CGP significantly reduced salivary flow and total protein concentration of saliva and naloxone restored them to the physiological levels. Morphine and CGP also reduced several infrared vibrational modes (Amide I, 1687-1594cm-1; Amide II, 1594-1494cm-1; CH2/CH3, 1488-1433cm-1; C = O, 1432-1365cm-1; PO2 asymmetric, 1290-1185cm-1; PO2 symmetric, 1135-999cm-1) and naloxone reverted these alterations. The in silico docking analysis demonstrated the interaction of polar contacts between the CGP and opioid receptor Cys219 residue. Altogether, we showed that salivary hypofunction and glandular changes elicited by CGP may occur through opioid receptor suggesting that the blockage of opioid receptors in superior cervical and submandibular ganglions may be a possible strategy to restore salivary secretion while maintaining antinociceptive action due its effects on the central nervous system.

In this paper, we first summarise the 2020 International Conference of EMBnet (The Global Bioinformatics Network) on “Bioinformatics Approaches to Precision Research”, held on 23th-24th September 2020, and then briefly introduce the main topics and contributions presented at the Conference and published in this supplement issue. The Conference’s main aim was to share the knowledge and scientific achievements of EMBnet members to prompt the cross-fertilisation of ideas and collaborations. The title reflects the type of contributions presented (20 in total), covering a wide range of cutting-edge research topics for which advanced bioinformatics methods and precision approaches are essential, and training in Bioinformatics. As for many other organisations, 2020 was the first year that the EMBnet Annual General Meeting was not in presence but ran on a virtual meeting platform because of the pandemic’s travel restrictions to moves. If this situation represented a limitation to our social activities, it allowed us to offer the possibility to attend the Conference to a larger number of researchers (i.e., 190 from 38 different countries). Among all registered people, 148 were following the conference presentations on both days. Under the authors’ permission, presentations were recorded and are available at the EMBnet Conference 2020 playlist on YouTube (https://youtube.com/playlist?list=PLVP2771lOozCHAOgVXBdqPW3oclEmzNIA), whereas the programme is available at the EMBnet Conference 2020 Google Drive folder (https://drive.google.com/file/d/1wWqp_I5vf-1GUlKmbCUq45EDQ9LfbrpC/view)

A multifunctional smart supramolecular platform based on a lanthanide-organic hydrogel is presented. This platform, which provides unique biocompatibility and tunable optical properties, is synthesized by a simple, fast, and reproducible eco-friendly microwave-assisted route. Photoluminescent properties enable the production of coated light-emitting diodes (LED), unique luminescent barcodes dependent on the excitation wavelength and thin-films for use in tamper seals. Moreover, piroxicam entrapped in hydrogel acts as a transdermal drug release device efficient in inhibiting edemas as compared to a commercial reference.

The supramolecular nano-aggregate CUR–CB[7] (CUR = curcumin and CB[7] = cucurbit[7]uril) was efficiently prepared by mixing CUR and CB[7] at a molar ratio of 1 : 1 in ethanol at room temperature. The supramolecular aggregate formation was evidenced by mainly FTIR, 1H NMR, DOSY and spectroscopy experiments. The supramolecular arrangement promotes the increase in the solubility and stability of CUR without affecting the biological properties of the A549 cells. The luminescence properties of CUR and CUR–CB[7] show anti-Kasha's rule fluorescence, and their remarkable NIR emission enables this material to be used as a luminescent probe and marker for in vivo tracking and structural integrity monitoring of the supramolecular complex.

This study evaluated for the first time the antibacterial activity, cell viability and migration ability on 3T3 murine fibroblast cells of extracts and isolated compounds [lupeol (1), hexamethylcoruleoellagic acid (2) and a mixture of 1 and betulinaldehyde (3)] of Myrciaria ferruginea. In antibacterial assays extracts were susceptible only against S. aureus (MIC 500 μg/mL) and S. epidermidis (MIC ranging from 7.8 to 500 μg/mL) and compounds 1-3have shown no significant activity. In trials for c ell viability, with exception of MeOH-H 2O fraction from leaves (viable cells > 90%), both the crude extract and other fractions showed inhibition of cell growth (viable cells ≤ 80% at 15.625 and 31.25 μg/mL); while the samples from stems, with the exception of CHCl 3 fraction that showed strong cytotoxic effect at the lowest concentration tested (15.625 μg/mL), the other fractions were not cytotoxic. Compounds (1-3) inhibited cell viability in dose dependent manner (15.625 to 500 μg/mL). Mixture containing 1 and 3 showed inhibitions only in concentrations greater than 62.5 μg/mL while compound 2 decreased from the lowest concentration tested. In scratch wound assay, these compoundsnot increased the population of fibroblasts at concentrations less than 62.5 μg/mL.

Context: Propolis has promising biological activities. Propolis samples from the Northeast of Bahia, Brazil – sample A from Ribeira do Pombal and B, from Tucano – were investigated, with new information regarding their biological activities. Objective: This paper describes the chemical profile, antioxidant, anti-glycation and cytotoxic activities of these propolis samples. Material and methods: Ethanol extracts of these propolis samples (EEP) and their fractions were analyzed to determine total phenolic content (TPC); antioxidant capacity through DPPH•, FRAP and lipid peroxidation; anti-glycation activity, by an in vitro glucose (10 mg/mL) bovine serum albumine (1 mg/mL) assay, during 7 d; cytotoxic activity on cancer (SF295, HCT-116, OVCAR-8, MDA-MB435, MX-1, MCF7, HL60, JURKAT, MOLT-4, K562, PC3, DU145) and normal cell lines (V79) at 0.04–25 μg/mL concentrations, for 72 h. The determination of primary phenols by ultra high-pressure liquid chromatography coupled to tandem mass spectrometry (UHPLC-MS/MS) and volatile organic compounds content by gas chromatography-mass spectrometry (GC-MS) were also performed. Results: The EEP polar fractions exhibited up to 90% protection against lipid peroxidation. The IC50 value for anti-glycation activity of EEP was between 16.5 and 19.2 μg/mL, close to aminoguanidine (IC50 = 7.7 μg/mL). The use of UHPLC-MS/MS and GC-MS allowed the identification of 12 bioactive phenols in the EEP and 24 volatile compounds, all already reported. Conclusions: The samples present good antioxidant/anti-glycation/cytotoxic activities and a plethora of biologically active compounds. These results suggest a potential role of propolis in targeting ageing and diseases associated with oxidative and carbonylic stress, aggregating value to them.

Ethnopharmacology relevance Poncianella pyramidalis (Leguminosae) is a Caatinga plant used in folk medicine because of its pharmacological properties, which include anti-inflammatory action. However, chemical compounds responsible for this effect have not yet been identified. Aim of the study This study aimed to evaluate the antioxidant, antinociceptive and anti-inflammatory effects of the ethyl acetate fraction from the inner bark of P. pyramidalis. Material and methods Total phenol content (TP) was estimated using the Folin-Ciocalteu reagent, while in vitro antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay. Chemical identification was done using LC-PDA/MS and LC-ESI/MS/MS. In vivo antinociceptive and anti-inflammatory properties were investigated using formalin, mechanical hypernociception and carrageenan-induced pleurisy assays in mice. Results TP was 525.08 ± 17.49 μg mg−1 gallic acid equivalent. The ethyl acetate fraction (EAF) inhibited 87.76% of the DPPH radical with an EC50 of 22.94 μg mL−1 and Antioxidant Activity Index of 1.74. LC-PDA/MS and LC-ESI/MS/MS identified 15 compounds that are mostly derived from gallic and ellagic acids. Regarding in vivo antinociceptive and anti-inflammatory activity, EAF (100 mg kg-1) significantly reduced the nociceptive response in the second phase of the formalin assay by 50% (p Conclusion These results demonstrate EAF from the inner bark of P. pyramidalis has strong in vitro antioxidant effect as well as in vivo antinociceptive and anti-inflammatory activities, which may be attributed to the bark being rich in phenolic compounds derived from gallic acid.

Selaginella convoluta (Arn.) Spring is a species popularly known as “jericó”, and used in folk medicine as analgesic and anti-inflammatory. This study aimed to investigate in mice the antinociceptive and anti-inflammatory activities of the hexane (Sc-Hex) and chloroform (Sc-CHCl3) fractions (100, 200 and 400 mg/kg) obtained by partition of crude ethanol extract from S. convoluta. The preliminary phytochemical analysis of the fractions was performed. Antinociceptive activity was evaluated by writhing, formalin and hot-plate tests. Anti-inflammatory activity was evaluated using carrageenan-induced pleurisy. The rota-rod test was used to evaluate motor coordination. Preliminary phytochemical screening showed that the Sc-Hex and the Sc-CHCl3 were positive for the presence of flavonoids, anthracene derivatives, quinones, triterpenes and steroids. Inhibition of writhing was observed for fractions tested. The Sc-Hex at all doses tested was effective in reducing the nociceptive behavior produced by formalin only in the second phase. However, the Sc-CHCl3 decreased the paw licking time in the first and second phases. In the hot plate no significant effect was observed for any fraction. In the rota-rod test, treated mice did not demonstrate any significant motor performance changes. In the carrageenan-induced pleurisy, Sc-CHCl3 (200 mg/kg) reduced cell migration to the pleural cavity. These results reveal the antinociceptive properties of S. convoluta , which support, in part, its traditional use, since the fractions did not presented significant activity in the inflammatory response profile. We further verify that this antinociceptive effect could be by activation of nociceptive peripheral pathway. Resumo Selaginella convoluta é uma espécie popularmente conhecida como “jericó”, e usada na medicina popular como analgésica e anti-inflamatória. Este estudo teve como objetivo investigar em camundongos as atividades antinociceptiva e anti-inflamatória das frações hexânica (Sc-Hex) e clorofórmica (Sc-CHCl3) (100, 200 e 400 mg/kg) obtidas por partição do extrato etanólico bruto de S. convoluta . A análise fitoquímica preliminar das frações foi realizada. A atividade antinociceptiva foi avaliada pelos testes de contorções abdominais, formalina e placa quente. A atividade anti-inflamatória foi avaliada usando pleurisia induzida por carragenina. O teste do rota-rod foi utilizado para avaliar a coordenação motora. A triagem fitoquímica preliminar mostrou que Sc-Hex e Sc-CHCl3 apresentaram reação positiva para a presença de flavonoides, derivados antracênicos, quinonas, triterpenos e esteroides. A inibição das contorções foi observada para as frações testadas. Sc-Hex em todas as doses testadas foi efetivo na redução do comportamento nociceptivo produzido pela formalina somente na segunda fase. No entanto, Sc-CHCl3 diminuiu o tempo de lambida da pata na primeira e segunda fases. Na placa quente, nenhum efeito significativo foi observado para qualquer fração. No teste do rota-rod os camundongos tratados não demonstraram mudanças significativas na coordenação motora. Na pleurisia induzida por carragenina, Sc-CHCl3 (200 mg/kg) reduziu a migração celular para a cavidade pleural. Estes resultados revelam a propriedade antinociceptiva de S. convoluta, justificando, em parte, seu uso tradicional, uma vez que os extratos não apresentaram atividade significativa no perfil de resposta inflamatória. Verificamos ainda que esse efeito antinociceptivo mostrou-se ligado à ativação da via periférica nociceptiva.

Corticosteroids are widely used as effective treatments for the control of chronic inflammatory diseases. However, because their long-term administration carries serious consequences, there is a need to investigate alternative therapies to reduce or even replace their use. In this regard, phenolic compounds have been presented as an alternative for the treatment of inflammatory diseases. p-Coumaric acid, a natural phenolic compound found throughout nature, exhibits antioxidative and anti-inflammatory properties. Herein, using a combination of Raman spectroscopy with principal component analysis and hierarchical cluster analysis, the inflammatory process induced by cigarette smoke extract (CSE) in epithelial cells treated with either a corticosteroid or p-coumaric acid was monitored in vitro. Our findings showed that p-coumaric acid had a significant anti-inflammatory effect in CSE-activated epithelial cells, and thus may be a useful alternative to corticosteroids for the treatment of airway inflammation in chronic obstructive pulmonary disease. In addition, multivariate analysis of the cell spectral data indicated that the mechanisms of action of the two drugs occur through different routes.

Underutilized parts of some abundant crops can be valuable and the search for additional uses, mainly in healthy and for social purposes are very attractive. This is the case of Cocos nucifera Linn., an important source of phenolic compounds and a native plant of tropical countries, widely distributed in the Northeast and North of Brazil. The objectives of this study were to determine the phenolic chemical composition, the photoprotection capacity, represented by sun protector factor (SPF), of the ethanol extract of coconut (Cocos nucifera) husk fiber of the yellow dwarf variety (EEYD) against UVB rays and after its incorporation into sunscreen formulations. Antiglycation activity [represented by bovine serum albumin (BSA) – glucose/fructose, Collagen – glucose/fructose and BSA-Methylglyoxal (MG) assays], using aminoguanidine (AG) as a positive control, and cytotoxic effects toward macrophages, were also evaluated. The identification of non-toxic antiglycation agents holds great promise in the development of alternative therapies for diseases, such as diabetes and their complications and is not often, reported in the literature. The determination of the SPF of the EEYD together with its sunscreen formulations was performed by in vitro method. A total of seven phenolic compounds, quercetin, catechin, epicatechin, vanillic, caffeic, 4-hydroxybenzoic and chlorogenic acids were identified by high performance liquid chromatography (HPLC)-UV/Vis and ultra high performance liquid chromatography - tandem mass spectrometer UHPLC-MS/MS. The present extract (EEYD) presented photoprotective activity with SPF values equivalent to the standards, benzophenone-3 and quercetin. The formulations prepared in different concentrations of the extract (5–20 % w/w) showed maximum SPF values of 15.94. The extract presented promising antiglycation activity, higher than the positive control, the pure compound aminoguanidine (AG), except for BSA/MG, with values for BSA/glucose/fructose of 9.61 μg/mL (vs.AG 18.30 μg/mL); for collagen/glucose/fructose of 4.50 μg/mL (vs.AG 82.87 μg/mL) and 34.76 μg/mL (vs.AG,13.19 μg/mL). The present ethanol extract does not decrease macrophage viability and presents a plethora of biologically active compounds. The combined results have shown the possibility of using non-toxic EEYD, as an active ingredient in sunscreen formulations and in the nutrition/medicinal areas, giving extra value to an environmental-unfriendly residue, with strong prospects for success.