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The high frequency of infectious diseases has spurred research into effective tactics to combat microorganisms that are resistant to several drugs. The overproduction of the transmembrane efflux pump protein NorA, which may export hydrophilic fluoroquinolones, is a common mechanism of resistance in S. aureus strains. This work evaluated the antimicrobial activity of the ethanolic extract from the leaves of Croton heliotropiifolius (EECH) against different bacterial and fungal strains, as well as investigating its modulating effect on the resistance to norfloxacin in a Staphylococcus aureus SA1199B overproducing the NorA efflux pump. Microdilution assays were used to assess the EECH’s antibacterial efficacy. The MIC of norfloxacin or ethidium bromide (EtBr) against the SA1199B strain was determined in the presence or absence of the EECH in order to assess the modifying influence on drug resistance. The EECH showed no activity against the Gram-positive and Gram-negative bacterial strains tested. The EECH also showed no antifungal activity against Candida albicans ATCC 10231. On the other hand, the extract reduced the MIC values for norfloxacin against SA1199B at subinhibitory concentrations. In addition, the EECH also reduced the MIC values of EtBr at subinhibitory concentrations, suggesting the occurrence of phytochemicals that inhibit efflux pumps. Molecular docking showed that retusin, a flavonoid found in the extract, could compete with norfloxacin at the orthosteric site of the NorA, indicating that it could be a potential efflux pump inhibitor. However, isolated retusin did not enhance the activity of norfloxacin or EtBr and it did not inhibit the EtBr efflux, showing that it is not a NorA inhibitor. Even though C. heliotropiifolius is a source of phytochemicals that function as adjuvants for norfloxacin, isolated retusin cannot be used in conjunction with norfloxacin to treat infections brought on by S. aureus that overproduces NorA.

Brown seaweeds of the Fucus genus represent a rich source of natural antiviral products. In this study, a Fucus ceranoides hydroalcoholic extract (FCHE) was found to inhibit 74.2 ± 1.3% of the proteolytic activity of the free SARS-CoV-2 3CL protease (3CLpro), an enzyme that plays a pivotal role in polyprotein processing during coronavirus replication and has been identified as a relevant drug discovery target for SARS- and MERS-CoVs infections. To purify and identify 3CLpro ligands with potential inhibitory activity using a one-step approach, we immobilized the enzyme onto magnetic microbeads (3CLpro-MPs), checked that the enzymatic activity was maintained after grafting, and used this bait for a ligand-fishing strategy followed by a high-resolution mass spectrometry analysis of the fished-out molecules. Proof of concept for the ligand-fishing capacity of the 3CLpro-MPs was demonstrated by doping the FCHE extract with the substrate peptide TSAVLQ-pNA, resulting in the preferential capture of this high-affinity peptide within the macroalgal complex matrix. Ligand fishing in the FCHE alone led to the purification and identification via high-resolution mass spectrometry (HRMS) of seven hepta-, octa-, and decapeptides in an eluate mix that significantly inhibited the free 3CLpro more than the starting FCHE (82.7 ± 2.2% inhibition). Molecular docking simulations of the interaction between each of the seven peptides and the 3CLpro demonstrated a high affinity for the enzyme’s proteolytic active site surpassing that of the most affine peptide ligand identified so far (a co-crystallographic peptide). Testing of the corresponding synthetic peptides demonstrated that four out of seven significantly inhibited the free 3CLpro (from 46.9 ± 6.4 to 76.8 ± 3.6% inhibition at 10 µM). This study is the first report identifying peptides from Fucus ceranoides with high inhibitory activity against the SARS-CoV-2 3CLprotease which bind with high affinity to the protease’s active site. It also confirms the effectiveness of the ligand-fishing strategy for the single-step purification of enzyme inhibitors from complex seaweed matrices.

Abstract This study assessed the inhibitory potential of the probiotics Lactobacillus (LB) exopolysaccharides (EPS) with or without extracts of Satureja calamintha on enteropathogenic Escherichia coli (EPEc) responsible for gastroenteritis. Methanolic and hydromethanolic extracts were prepared by cold maceration and subjected to phytochemical screening. The compounds of the extracts were determined with the colorimetric assays and identified using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). Antioxidant activities of the extracts were also evaluated by using 2,2-diphenyl-1-picrylhydrazil (DPPH) radical scavenging. Antibacterial effect on EPEc was evaluated by using both agar disc diffusion and microdilution methods. The in vitro test of auto-aggregation was investigated. Microbiological analysis showed that 63% of the isolated LB were producing EPS, with the amount ranging from 8.21 to 43.13 mg/L. Chemical analysis of the extracts revealed the presence of polyphenols and flavonoids, more abundant in the hydromethanolic extract, which presented the highest content with 2.11 mg EGA/g of polyphenol and 1.64 mg EC/g of flavonoids and 1.71 mg EGA/g of polyphenol and 1.15 mg EC/g of flavonoids in the methanolic extract. Hydromethanolic extracts and EPS exhibited a more important activity than did the methanolic extract against EPEc. The combined action of EPS and extracts reduced the aggregation ability of EPEc and decreased the rate of their adhesion.

The development of photoprotective products has been highly focused on natural ingredients, and exposure to ultraviolet (UV) radiation is also related to the production of reactive oxygen species (ROS), which are extremely damaging to tissues. Hymenaea martiana Hayne has flavonoids related to its pharmacological activities, but a flavonoid profile of this species has not been reported yet. In this context, this work aimed to perform high-performance liquid chromatography-mass spectrometry-electrospray ionization-ion trap (HPLC-MS-ESI-IT) to characterize the flavonoids from Hymenaea martiana bark extract and develop a cosmetic formulation with photoprotective action. Total phenolic compounds, total flavonoids, sun protection factor (SPF) and antioxidant activity of the crude extract were determined. An HPLC-ESI-IT profile of flavonoids was developed. Photoprotective gel formulations were developed with the extract of H. martiana. The highest content of phenolic compounds was found in the crude extract, followed by the ethyl acetate fraction. The total flavonoid content in the samples demonstrated that these are the major phenolic compounds. The crude extract showed significant antioxidant and photoprotective activity. A flavonoid profile was developed, and bioactive flavonoids reported in the species were identified. In the development of the formulations, it was evidenced that the addition of the crude extract to the chemical filter increased the antioxidant activity and FPS, suggesting a synergistic effect in the photoprotection. Formulation F4 was considered a promising product. These results show the cosmetic potential of Hymenaea martiana, thus justifying the development of a cosmetic formulation with photoprotective activity.

Background: Bromelia laciniosa Mart. ex Schult. & Schult.f. is a Bromeliaceae plant species from the Brazilian Caatinga, popularly used for the treatment of childhood colic, diarrhea, fever, jaundice, dandruff and hepatitis. The objective of this work was to evaluate the chemical composition and antimicrobial activity of the species B. laciniosa. Method: In this study, we evaluated the antimicrobial activity of ethanolic extract from the leaves of B. laciniosa by microdilution MIC method, and provided a comprehensive panel of B. laciniosa’s metabolite composition through mass spectrometry (MS) coupled to gas chromatography (GC–MS) and liquid chromatography (LC-MS). Results: B. laciniosa ethanolic extract inhibited Staphylococcus aureus growth at the lowest concentration tested. The GC–MS analysis revealed 45 non-polar metabolites, including campesterol, palmitic acid, oleic acid and α-tocopherol. Isolation and structural elucidation by NMR experiments supported the identification of cirsilineol (1), and the mixture of steroids β-sitosterol (2) and stigmasterol (3). The LC-MS metabolite profiling was assisted by Global Natural Product Social Molecular Networking (GNPS) and led to the putative annotation of 22 metabolites, consisting of phenylpropanoids, C- and O-glycosyl-flavonoids and fatty acids. In total, 39 chemical constituents are being described for the first time in B. laciniosa. Conclusions: The results show the diversity of secondary metabolites in the species B. laciniosa as well as antibacterial activity against S. aureus.

In this study, four Moroccan plants, Halimium antiatlanticum, Adenocarpus artemisiifolius, Pistacia lentiscus and Leonotis nepetifolia, were evaluated for their phytoconstituents and biological activities. Methanolic extracts of these plants were obtained by Soxhlet apparatus, phytochemical screening was performed, and the total phenolic and flavonoid contents were determined. Then, the antioxidant and dermocosmetic activities of the methanolic extracts were evaluated. The obtained results revealed that the leaves and/or aerial parts contained tannins, polyphenols, flavonoids, coumarins, carotenoids, terpenoids and saponins. The higher total phenolic content values were recorded on Pistacia lentiscus and Halimium antiatlanticum with 396.64 ± 30.79 and 304.96 ± 55.61 mgGAE/gDW, respectively. The antioxidant activity was measured by DPPH, ABTS and FRAP assays, and showed that Pistacia lentiscus and Halimium antiatlanticum were the most active extracts, with, respectively, IC50 values of 3.705 ± 0.445 and 5.037 ± 0.122 µg/mL for DPPH. The same results were observed for the FRAP and ABTS assays. Those extracts also showed a strong collagenase inhibitory activity at 200 µg/mL, with 78.51 ± 2.27% for Pistacia lentiscus and 73.10 ± 8.52% for Halimium antiatlanticum. Adenocarpus artemisiifolius showed the highest elastase inhibition rate, with 76.30 ± 5.29%. This study disclosed the dermocosmetic potential of Halimium antiatlanticum and Adenocarpus artemisiifolius, two Moroccan endemic plants that can be traditionally used by local populations or exploited by the cosmetic industry.

For more than 40 years, marine microorganisms have raised great interest because of their major ecological function and their numerous applications for biotechnology and pharmacology. Particularly, Archaea represent a resource of great potential for the identification of new metabolites because of their adaptation to extreme environmental conditions and their original metabolic pathways, allowing the synthesis of unique biomolecules. Studies on archaeal carotenoids are still relatively scarce and only a few works have focused on their industrial scale production and their biotechnological and pharmacological properties, while the societal demand for these bioactive pigments is growing. This article aims to provide a comprehensive review of the current knowledge on carotenoid metabolism in Archaea and the potential applications of these pigments in biotechnology and medicine. After reviewing the ecology and classification of these microorganisms, as well as their unique cellular and biochemical characteristics, this paper highlights the most recent data concerning carotenoid metabolism in Archaea, the biological properties of these pigments, and biotechnological considerations for their production at industrial scale.

In Brazil, the leather industry is an important economic segment moving around U$ 3 billions of dollars a year. However, high amounts of water are requested to transform skin animals into leather, causing high wastewater amounts to be consequently produced. A major problem is attached to the presence of chromium in the wastewater from the tanning process. Chromium is a heavy metal potentially toxic both to the environment and to the human health. In order to control the levels of chrome dumped into the environment, Brazilian agencies require the treatment of effluents by the generating source. Thus, this study aimed to develop an alternative method to the removal of chromium in wastewater from the leather industry using the Opuntia ficus-indica biomass as eco-friendly biosorbent. Crude waste samples were collected in a tannery stabilization pond for chromium quantification and further treatments. The powdered Opuntia ficus-indica was obtained from species collected in Pernambuco, Brazil, and its physical parameters and pHPCZ were characterized. Adsorptions studies and acute toxicity were also carried out. The biomass remaining after the sorption was analyzed through scanning electron microscopy and Fourier-transform infrared spectroscopy. The chromium content was above the limit allowed by the Brazilian regulatory agency. In sorption studies, biomass was able to remove 74.8% and 84.88% of Cr (III) using 2.0 g and 4.0 g of biomass, respectively. The surface of biomass is very favorable to biosorption and the chemical bindings among oxygen atoms present in the chemical components of this biomass and the heavy metal was confirmed through infrared spectrum. This study proved that Opuntia ficus-indica is effectively biosorbent to chromium, promising and with low costs for the leather industry, able to reduce its ecotoxicity as proven by chemical and biological assays.

Inflammation is a protective response of the organism against damaging agents, this process is considered beneficial, however in some situations, this response can be damage when exacerbated effect are present. This claim objective to evaluate the qualitative and quantitative chemical profile, acute toxic and anti-inflammatory effects of the hydroalcoholic extract of leaves from Tocoyena formosa (Cham. & Schlecht.) K. Schum. (HELTF). Quantitative and qualitative phytochemical analysis was performed by HPLC-DAD and colorimetric assay. The topical anti-inflammatory activity was determined in Croton oil-induced ear edema assay and systemic activity was performed in vascular permeability, paw edema induced by carrageenan and dextran. Phytochemical analysis of leaves from HELTF showed presence of tannin, flavonoid, saponins an other that confirmed by HPLC analysis. The extract did not cause significant with LD50 greater than 5000 mg/kg and did not promote significate reduction in topical inflammatory process. However, HELTF demonstrate significant reduction of paw edema induced by carrageenan and dextran. The HELTF (200 mg/kg) reduced the protein/cell migration in the intradermal carrageenan-induced inflammation. Our results demonstrated that the first time the chemical profile and describe the effective action in systemic anti-inflammatory, antiedematogenic activity and low acute toxicity. This activity presents, supporting its traditional use. However, new studies are necessary for the detection and clarification of the possible mechanism of action. Keywords: Acute toxicity, Anti-inflammatory activity, Chemical profile, Tocoyena formosa

Background: Bothropic venoms cause intense local damage, pain, edema, and myonecrosis. Morus nigra L. (Moraceae) has several uses in folk medicine and can be a promising candidate for the treatment of several inflammatory disorders. Hypothesis/Purpose: The present study aims to evaluate the anti-inflammatory and antinociceptive effects of the ethanolic extract of Morus nigra L. (Mn-EtOH) on paw lesions induced by Bothrops jararacussu snake venom (BjcuV) in mice. Methods: UV–vis absorption of BjcuV was evaluated. A phytochemical study was performed, which led to the isolation and characterization of three compounds. These compounds were identified using spectrometric methods, namely LC–MS and NMR (1D and 2D), followed by the validation of their spectra with the data available in the literature. Further, the flavonoids i.e. rutin and quercetin (chemical markers of M. nigra), Mn-EtOH or Mn-EtOH-encapsulated electrospun fibers of Eudragit L100 (FB/Mn-EtOH), and Mn-EtOH-encapsulated microparticles of Eudragit L100 (MP/Mn-EtOH) were evaluated, in paw edema test induced by BjcuV. Results: UV–vis spectra showed the presence of phospholipases A2 as component of BjcuV. The chemical examination resulted in the isolation of β-sitosterol, quercetin-3-O-glucopyranoside, and kaempferol-3-O-glucopyranoside. Mn-EtOH, FB/Mn-EtOH, MP/Mn-EtOH, rutin, and quercetin reduced the local edema induced by BjcuV. The Mn-EtOH also prevented edema provoked by serotonin and bradykinin. Moreover, it reduced paw edema and peritoneal leukocyte infiltration induced by carrageenan, and decreased the mechanical hypernociception of BjcuV. Mn-EtOH exerted anti-inflammatory and antinociceptive effects, possibly by the inhibition of leukocyte migration and the modulation of serotonin and bradykinin actions. This anti-inflammatory activity was maintained even upon incorporation of the M. nigra extract into the drug delivery systems (i.e., Mn-EtOH-encapsulated FBs and MPs of Eudragit L100). Conclusion: These results reinforce the therapeutic potential of M. nigra in the treatment of inflammatory conditions, in addition to, its role as a complementary treatment of snakebites.

Annona vepretorum is an endemic species of the Caatinga biome, known in Northeastern Brazil as ''araticum” and/or “pinha da Caatinga”. In the present study it was evaluated the neuropharmacological potential of the essential oil obtained from the leaves of Annona vepretorum, as well as of the inclusion complexes of oil obtained with cyclodextrin. Thus, were used neuropharmacological tests already consolidated in the literature like open-field, elevated plus maze, rota-rod, tail suspension test, thiopental-induced sleep test, among others. The acute treatment of essential oil (EO) has anxiolytic, sedative, antiepileptic and antidepressant effects. The anxiolytic and anticonvulsant effects seems to be related to the GABAergic system, probably in the receptor subtypes that mediate the effects of the benzodiazepines, to generate anxiolytic activity. The sedative effect seems to be involved with other signaling pathways. The antidepressant effect of EO seems to be related to its action on serotonergic receptors. It was verified that some behavioral parameters were improved with the oil complexed with β-cyclodextrin, but this effect was not uniform for all the doses and tests used. Further studies are needed in order to use other options for drug delivery systems. Thus, the essential oil of Annona vepretorum is a promising agent with neurobiological activity and a potential target for drug discovery, since the natural products such as medicinal plants have been a source of new therapeutic proposals.

Abstract Background Spondias tuberosa is a plant that produces a fruit crop with high economic relevance at Brazilian Caatinga. Its roots and leaves are used in folk medicine. Methods Chemical composition of a hexane extract from S. tuberosa leaves was evaluated by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and 1H nuclear magnetic resonance (NMR). Antioxidant potential was investigated by DPPH and ABTS assays. Antifungal action on Candida species was evaluated determining the minimal inhibitory concentration (MIC50) and putative mechanisms were determined by flow cytometry analysis. In addition, hemolytic activity on human erythrocytes was assessed and the concentration required to promote 50% hemolysis (EC50) was determined. Results Phytochemical analysis by TLC showed the presence of flavonoids, hydrolysable tannins, saponins and terpenes. The HPLC profile of the extract suggested the presence of gallic acid (0.28 ± 0.01 g%) and hyperoside (1.27 ± 0.01 g%). The representative 1H NMR spectrum showed saturated and unsaturated fatty acids among the main components. The extract showed weak and moderate antioxidant activity in DPPH (IC50: 234.00 μg/mL) and ABTS (IC50: 123.33 μg/mL) assays, respectively. It was able to inhibit the growth of C. albicans and C. glabrata with MIC50 of 2.0 and 0.078 mg/mL, respectively. The treatment of C. glabrata cells with the extract increased levels of mitochondrial superoxide anion, caused hyperpolarization of mitochondrial membrane, and compromised the lysosomal membrane. Weak hemolytic activity (EC50: 740.8 μg/mL) was detected. Conclusion The results demonstrate the pharmacological potential of the extract as antioxidant and antifungal agent, aggregating biotechnological value to this plant and stimulating its conservation.

Pain and inflammation are unpleasant experiences that usually occur as a result of tissue damage. Despite the number of existing analgesic drugs, side effects limit their use, stimulating the search for new therapeutic agents. In this sense, five hydrazone derivatives (H1, H2, H3, H4, and H5), with general structure R1R2C = NNR3R4, were synthesized with molecular modification strategies. In this paper, we describe the ability of hydrazone derivatives to attenuate nociceptive behavior and the inflammatory response in mice. Antinociceptive activity was evaluated through acetic acid-induced writhing and formalin-induced nociception tests. In both experimental models, the hydrazone with the greatest potency (H5) significantly (p < 0.05) reduced nociceptive behavior. Additionally, methods of acute and chronic inflammation induced by different chemicals (carrageenan and histamine) were performed to evaluate the anti-inflammatory effect of H5. Moreover, molecular docking analysis revealed that H5 can block the COX-2 enzyme, reducing arachidonic acid metabolism and consequently decreasing the production of prostaglandins, which are important inflammatory mediators. H5 also changes locomotor activity. In summary, H5 exhibited relevant antinociceptive and anti-inflammatory potential and acted on several targets, making it a candidate for a new multi-target oral anti-inflammatory drug.

Morus nigra L. is a species popularly known in the Northeast of Brazil as “amora miúra”. This species is a source of flavonoids with antioxidant activity. Antioxidants play an important role in the preservation of cosmetic formulations, and they neutralize free radicals. The objective of this study was to develop a topical emulsion containing leaf extract of Morus nigra L., as well as to evaluate the stability, antioxidant and antibacterial activities of the formulations. A crude hydroalcoholic (70%) extract of M. nigra leaves (MnCE) was submitted to high-performance liquid chromatography with diode-array detection (HPLC–DAD) analysis and incorporated into an anionic base emulsion. Antioxidant activity was evaluated according to the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, and the stability of the formulation was assessed for 90 days, submitting the emulsion to storage at 4, 20, and 37 °C. Microdilution techniques evaluated the antibacterial activity and a challenge test assessed the microbiological stability. Analysis by HPLC–DAD identified the flavonoids rutin and isoquercetin in the M. nigra extract. The emulsion and plant extract presented antioxidant activity, and the stability of the emulsion was preserved in terms of pH value and viscosity—which did not show significant changes, except for the spreadability, which was affected by the temperature. The antioxidant activity did not change significantly, except for the sample under 4 °C, which showed a considerable decrease in activity. The crude hydroalcoholic extract and formulation showed antimicrobial activity and the emulsion was considered stable in terms of organoleptic, physicochemical, and microbiological properties.

The argan tree (Argania spinosa (L.) Skeels) is one of the most important floristic resources in Morocco. This Moroccan endemic tree is known for its numerous therapeutic and medicinal uses. In addition to some medicinal and cosmetic uses, argan fruit pulp and press cake are traditionally used by the Berber population for heating and feeding livestock. Molecular docking is an in silico approach that predicts the interaction between a ligand and a protein. This approach is mainly used in chemistry and pharmacology of natural products as a prediction tool with the purpose of selecting plant extracts or fractions for in vitro tests. The aim of this research is to study the evaluation of potential tyrosinase, collagenase, and elastase inhibitory activities of argan fruit press-cake and pulp extracts. Extracts were evaluated for their total phenolic content (TPC), and the major polyphenols of both press-cake and pulp extracts were submitted to molecular docking in order to determine the mechanisms of action of these compounds. Obtained results revealed that fruit pulp had the strongest dermocosmetic activities, as well as the highest TPC, with values above 55 mg gallic-acid equivalent per gram of dry matter (mgeq AG/gDM). Moreover, those results were positively correlated with the docking findings, suggesting that the pulp lead compounds have higher affinity with tyrosinase, collagenase, and elastase action sites. The results here presented are very promising and open new perspectives for the exploitation of argan-tree by-products as cosmetic agents towards the development of new anti-aging products.

Amburana cearensis is an arboreal legume of the Fabaceae family, with high phytotherapic and medicinal potential due the presence of secondary metabolites. The objective of this study was to evaluate the effect of 2,4-dichlorophenoxyacetic acid (2,4-D) and 4-amino-2,5,6- trichloro-2-pyridinecarboxylic acid (picloram) on the in vitro induction of callogenesis of A. cearensis and analyze the biochemical and phytochemical potential of these calluses. For callus induction, leaf and cotyledon segments were used as explants, which were inoculated in woody plant medium (WPM) supplemented with different concentrations of 2,4-D (0, 5, 10, 20, 40 μM) or picloram (0, 5, 10, 20, 40, 80 μM). The callus growth curve was estimated based on fresh weight, measured at 7-day intervals until 28 days after inoculation. The calluses were analyzed by biochemical tests to quantify the reducing sugars and total proteins. Phytochemical screening and high-performance liquid chromatography were performed to establish the phytochemical profile of extracts from calluses. The concentrations of 21.94 μM and 26.46 μM of 2,4-D induced the greatest formation of compact and friable calluses from the leaf and cotyledon segments, respectively. The growth curve had two distinct phases (lag and exponential) for both types of calluses evaluated. The maximum levels of reducing sugars and total proteins in the calluses from leaf and cotyledon segments were obtained on the day of inoculation and after 28 days of cultivation, respectively. The results of the phytochemical analysis identified the presence of coumarin in all the extracts evaluated, this secondary metabolite has high pharmacological potential.

This study evaluated the effect of Amburana cearensis extract as a preservation or culture medium for ovine ovarian tissue. Ovarian fragments were fixed in 4% buffered formaldehyde for 18 h (fresh control), stored in Minimal Essential Medium (MEM) or in A. cearensis extract (0.1; 0.2 or 0.4 mg/mL) at a temperature of 4ºC for 6, 12 or 24 h (preservation - experiment 1) or cultured for 7 days in ?-MEM+ or in A. cearensis extract without (0.1; 0.2 or 0.4 mg/mL) or with supplements (0.1+ ; 0.2+ or 0.4+ mg/ mL; experiment 2). The percentages of morphologically normal follicles and follicular activation were submitted to analysis of variance (ANOVA) and Tukey´s test. The values of TUNEL-positive cells were submitted to Chi-square test (P < 0.05). The storage of fragments for 6 h in MEM showed higher percentages of normal follicles (62%) and a lower rate of TUNEL positive cells (36.17%) compared to other treatments (normal follicles: 46%; 43% and 52%; TUNEL positive cells: 58.57%; 55.30% and 55.63% for Amb 0.1; Amb 0.2 and Amb 0.4 mg/mL, respectively). However, after 12 or 24 h, MEM (12 h: 48%; 24 h: 45%) and Amb 0.2 mg/mL (12 h: 37%; 24 h: 39%) showed similar percentages of normal follicles and TUNEL positive cells (MEM - 12 h: 43.26%; 24 h: 58%; Amb 0.2 mg/mL - 12 h: 50%; 24 h: 61%). After culture, ?-MEM+ recorded a higher percentage of normal follicles (58.25%) than A. cearensis treatments (32.8%; 25.4% and 34.2% for Amb 0.1; Amb 0.2 and Amb 0.4 mg/mL, and 22.25%; 20.0% and 36.6% for Amb 0.1+ ; Amb 0.2+ and Amb 0.4+ mg/mL, respectively) (P < 0.05). Follicular activation increased in all treatments (52.5%; 36.73%; 54.05%; 47.5% and 58.19% for ?-MEM+ ; Amb 0.1; Amb 0.1+ ; Amb 0.2+ and Amb 0.4+ mg/mL, respectively) compared to the fresh control (11.65%), except for Amb 0.2 mg/mL (23.69%) and Amb 0.4 mg/mL (28.85%) (P > 0.05). Moreover, after in vitro culture, A. cearensis at a concentration of 0.1 mg/mL maintained the percentage of TUNEL positive cells (30.0%) in a way that is similar to that observed in the fresh control (22%) (P > 0.05). In conclusion, ovine preantral follicles can be preserved at 4°C in MEM for 6 h. For longer periods of preservation (24 h), MEM and 0.2 mg/mL A. cearensis are recommended. Moreover, after in vitro culture, A. cearensis extract (0.1 mg/mL) showed higher activation and lower DNA fragmentation in ovine preantral follicles.

The aim of this study was to evaluate the chemical composition, antioxidant and antibacterial activities and cytotoxicity of fractions from Selaginella convoluta, obtained by liquid–liquid extraction using hexane (Sc-Hex), chloroform (Sc-CHCl3) and ethyl acetate (Sc-AcOEt). The phenolic and flavonoid contents were measured by the Folin-Ciocalteu and aluminium chloride methods, respectively. Antioxidant activities were evaluated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and β-carotene-linoleic acid bleaching test. The antibacterial effect was evaluated by the method of microdilution and the cytotoxicity analysis in HCT-116 (colon), OVCAR-8 (ovarian) and SF-295 (brain) cells were carried out for MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) test. The fractions were positive for the presence of anthracene derivatives, flavonoids, lignans, naphthoquinones, steroids and triterpenoids. The Sc-Hex and Sc-AcOEt showed good antioxidant activities. The fractions of S. convoluta demonstrated antibacterial activity and showed weak cytotoxicity. These activities were correlated with presence of phenolic compounds in active fractions.

Abstract: The objective of this work was to evaluate the lethal and sublethal toxicity of hexane and methanolic extracts from the leaves of Annona vepretorum (Annonaceae) on Tetranychus urticae (Acari: Tetranychidae). The methanolic extract toxicity was evaluated by Potter tower application (topical + residual effect) and by immersion of Canavalia ensiformis leaf disks in the extract solution (residual contact effect). The hexane extract toxicity was evaluated exclusively through residual contact effect. Sublethal effects of the methanolic extract were evaluated through LC50 on the females. Mite preference for feeding and oviposition was evaluated by multiple choice tests, between the control and the extract concentrations, using the hexane and methanolic extracts. Estimated LC50 for the methanolic extract was 10.96 mg mL-1 for the topic + residual effect and 22.07 mg mL-1 for the residual effect. Estimated LC50 for the hexane extract was 50.61 mg mL-1. The methanolic extract at the previously estimated CL50 interfered in the fecundity and longevity of females, differing significantly from the control treatment. In the multiple choice tests, for both extracts, mites showed a significant preference for the control, both for feeding and oviposition. Annona vepretorum has acaricide effect and constitutes a botanical source with great potential for controlling T. urticae.

This study demonstrated the effect of Morus nigra leaf extract during ovine ovarian tissue transportation on the survival and apoptosis of preantral follicles in vitro. High Performance Liquid Chromatography (HPLC) was used to determine the fingerprint chromatogram of the crude ethanolic extract. Four pairs of ovaries from four sheep were collected. The ovarian cortex was fragmented and one fragment was fixed in 10% buffered formaldehyde and processed for histological and TUNEL analysis (fresh control). The other fragments were placed in Minimal Essential Medium (MEM – control medium) or M. nigra extract (0.025; 0.05 or 0.1 mg/mL) and stored (simulating transport) at 4ºC for 6, 12 or 24 h. Preserved fragments (6 h) were also destined to histological and TUNEL analysis. HPLC analysis confirmed the presence of antioxidant compounds (rutin, isoquercetin e kaempferitrin) in the extract. There was a decrease (P < 0.05) in the percentage of morphologically normal preantral follicles after preservation in all treatments compared to the fresh control. The percentage of normal preantral follicles after preservation in M. nigra at 0.05 mg/mL for 6 h was higher (P < 0.05) than in MEM or 0.025 mg/mL M. nigra and similar (P > 0.05) to 0.1 mg/mL of the extract. Apoptosis increased (P < 0.05) after conservation for 6 h in all treatments compared to the fresh control. Moreover, TUNEL positive cells decreased (P < 0.05) after preservation in 0.05 or 0.1 mg/mL M. nigra compared to MEM or 0.025 mg/mL M. nigra. In conclusion, 0.05 mg/mL M. nigra extract can be used as a preservation medium for ovine ovarian tissue at 4°C for up to 6 h.

Abstract Purpose: To realize a morphological examination of the musculoskeletal tissue, assessing the effect of a contusion method for the production in rat gastrocnemius, comparing the inflammatory responses generated by different impacts. Methods: For the analysis of a contusion method, twelve female Wistar rats were distributed into four groups. The lesion was generated by 324 g of mass that was dropped from different predetermined heights for each group (30, 45, 60 and 70 cm). Results: In the analysis of musculoskeletal tissue, the response to injury varied according to the mass of the height drop onto the muscle. Only the group that was injured from 70 cm responded with uniform and severe inflammation, whereas the groups 30, 45 and 60 cm showed inflammation in some regions of the tissue with mild and moderate infiltrates. Conclusion: The method with the 324-gram mass dropped from a 70-cm height onto the gastrocnemius muscle of rats seems to be the most suitable for the production of muscle injury in these animals after 72 hours, showing an important inflammatory infiltrate.

In this study, the phytochemical profile of extracts from the flowers of Bromelia laciniosa was characterized. The total phenolic and flavonoids contents were determined and the antioxidant and photoprotective activities were evaluated using in vitro assays. Phytochemical analysis demonstrated that the extracts were found to be positive for the presence of anthracene derivatives, anthraquinones, coumarins, flavonoids and tannins, lignans, mono and diterpenes. The ethanol extract (Bl-EtOH) presented the most significant total phenolic content (53.75 ± 1.25 mg GAE/g). The dichloromethane extract (Bl-CH2Cl2) showed the highest flavonoid content (46.06 ± 1.18 mg CE/g). The methanol extract (Bl-MeOH) was the most effective extract in the DPPH (2,2-diphenyl-1-picrylhydrazil) assay (EC50 141.90 ± 3.01 μg/mL). Bl-EtOH and Bl-MeOH showed higher sun protection factor at a concentration of 100 mg/L (3.38 ± 0.04 and 3.78 ± 0.11, respectively). Therefore, the extracts proved to be interesting for the development of new studies aiming their incorporation into photoprotective cosmetic formulations.

ABSTRACT: This study aimed to perform phytochemical analysis and to test the antimicrobial activity of the crude hydroalcoholic extract obtained from the leaves of Sphagneticola trilobata. Classes of secondary metabolites present in the extract were identified through phytochemical screening using analytical thin-layer chromatography. Antimicrobial activity was evaluated by testing cultures of Staphylococcus aureus, S. epidermidis, Staphylococcus spp., Escherichia coli, Serratia marcescens, Enterococcus faecalis, Pseudomonas aeruginosa, Salmonella Typhimurium, and Klebsiella pneumoniae isolated from human skin and those of Staphylococcus spp. isolated from dog skin using the broth microdilution method. In the phytochemical screening, classes of anthracenic derivatives and mono-, sesqui-, and diterpenes were identified. Colorimetric analysis showed total phenol and total flavonoid contents of 21.7 ± 0.009 mg of gallic acid equivalents per gram of sample and 0.23 ± 0.005 mg of catechin equivalents per gram of sample, respectively. Microbiological analysis revealed that the hydroalcoholic extract of S. trilobata exhibited antimicrobial activity against cultures of Staphylococcus spp., E. coli, S. marcescens, and E. faecalis isolated from human skin and those of Staphylococcus spp. isolated from dog skin. Thus, crude hydroalcoholic extract of leaves of S. trilobata contained flavonoids and terpenoids as secondary metabolites, which contributed to its antimicrobial activity against skin bacteria isolated from different sources.

Neoglaziovia variegata is endemic to northeastern Brazil. The drought resistant plant produces edible fruits and is used as a fibre plant by rural communities in the Caatinga region where a variety of products are made from the white, soft and flexible fibres. Extracts of N. variegata have been reported to be of low toxicity and to exhibit antinociceptive effect, photoprotective potential, antioxidant effect, gastroprotective effects and antibacterial effect against both Gram-positive and Gram-negative bacteria, however, the chemical constituents of this species are mainly unknown. The novel poly-oxygenated flavone glucoside 5,6,7,4'-tetrahydroxy-3',5'-dimethoxy-flavone 7-O-β-glucopyranoside in addition to the rare poly-oxygenated flavone 5,4'-dihydroxy-6,7,3'-trimethoxyflavone 4'-O-β-glucopyranoside and the flavonol quercetin 3-O-(6''-rhamnopyranosyl-β-glucopyranoside) have been characterised from the leaves of N. variegata. 5,6,7,4'-tetrahydroxy-3',5'-dimethoxy-flavone, which comprises the core structure of the novel compound, is a new flavonoid aglycone in nature. The structure determinations were based on extensive use of 2D NMR spectroscopic techniques and high-resolution mass spectrometry. Both substances exhibited toxicity towards MOLM-13 acute myeloid leukaemia cells.

Background Leonotis nepetifolia (Family Lamiaceae) is a medicinal plant from which the flavonoid cirsiliol with sedative, hypnotic, anti-inflammatory and cytotoxic activity has been extracted. Methods Seedlings were cultivated under different levels of shade in native or fertilized modes. The content of cirsiliol was measured monthly by high-performance liquid chromatography and the total phenolic content by the Folin-Ciocalteu method. Monitoring of growth was carried out with the weekly measurement of height until the stabilization of growth. Results The application of fertilizing and/or shading does not alter significantly the cirsiliol content. However, this content varies throughout the year, reaching the peak production in the summer, independently of the treatment applied. This same profile, with production in the summer, was also verified for phenolic compounds, reaching 58.15 ± 9.35 mg of equivalents of gallic acid per g of extract in the summer, content 1.84 times greater than the content verified in winter (31.56 ± 4.09 mg of gallic acid/g of extract). Although shading and fertilizing had no effect on cirsiliol content, the results also showed a positive influence on the height and biomass of the plant, which can causes a higher yield of extractable material. Discussion Biotic and abiotic stresses are able to increase or decrease the production of secondary metabolites, including phenolic compounds in medicinal plants and, as the stress response is peculiar to each species, cultivation studies become necessary. The present study reports by the first time the influence of shading, fertilizing and seasons in cirsiliol content in L. nepetifolia. Among analyzed variables, the seasons showed a larger influence in expression of cirsiliol and among seasons, our results showed that the summer is the ideal season for collections. In summer, the photoperiod is larger than in other seasons of the year and due to that, the plants need greater protection against the long photoperiod. For this, the plants increase the production of phenolic compounds as observed in this study. Although they do not influence the production of cirsiliol, the shading and nutrients in soil favor growth and leaf area of several plants, explaining, thus, the higher height and biomass obtained.

Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in β-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of β-cyclodextrin/Essential oil (β-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs.

The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high antioxidant action from B. tetraphylla (BT) leaf extracts. In vitro methods (DPPH and ABTS assays; determination of phenolic and flavonoid contents) were used to select products derived from B. tetraphylla with high antioxidant action. Then, the samples with the highest potentials were evaluated in a model of injury based on the inoculation of a lethal dose of heat-inactivated Escherichia coli in Tenebrio molitor larvae. Due to its higher antioxidant properties, the methanolic extract (BTME) was chosen to be fractionated using Sephadex LH-20 column-based chromatography. Two fractions from BTME (BTFC and BTFD) were the most active fractions. Pre-treatment with these fractions protected larvae of T. molitor from the stress induced by inoculation of heat-inactivated E. coli. Similarly, BTFC and BTFD increased the lifespan of larvae infected with a lethal dose of enteroaggregative E. coli 042. NMR data indicated the presence of aliphatic compounds (terpenes, fatty acids, carbohydrates) and aromatic compounds (phenolic compounds). These findings suggested that products derived from B. tetraphylla leaves are promising candidates for the development of antioxidant and anti-infective agents able to treat oxidative-related dysfunctions.

Anadenanthera colubrina var cebil (Griseb.) Altschul is a medicinal plant found throughout the Brazilian semi-arid area. This work performed a bioguided purification of active substances present in ethyl acetate extract from A. colubrina leaves. The anti-Staphylococcus aureus and antioxidant actions were used as markers of bioactivity. The extract was subjected to flash chromatography resulting in five fractions (F1, F2, F3, F4, and F5). The fractions F2 and F4 presented the highest antimicrobial action, with a dose able to inhibit 50% of bacteria growth (IN50) of 19.53 μg/mL for S. aureus UFPEDA 02; whereas F4 showed higher inhibitory action towards DPPH radical (2,2-diphenyl-1-picryl-hydrazyl-hydrate) [dose able to inhibit 50% of the radical (IC50) = 133 ± 9 μg/mL]. F2 and F4 were then subjected to preparative high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR), resulting in the identification of p-hydroxybenzoic acid and hyperoside as the major compounds in F2 and F4, respectively. Hyperoside and p-hydroxybenzoic acid presented IN50 values of 250 μg/mL and 500 μg/mL against S. aureus UFPEDA 02, respectively. However, the hyperoside had an IN50 of 62.5 μg/mL against S. aureus UFPEDA 705, a clinical isolate with multidrug resistant phenotype. Among the purified compounds, the proanthocyanidins obtained from F2 exhibited the higher antioxidant potentials. Taken together, these results highlight the potential of A. colubrina leaves as an alternative source of biomolecules of interest for the pharmaceutical, food, and cosmetic industries.

Pain and inflammation are complex clinical conditions that are present in a wide variety of disorders. Most drugs used to treat pain and inflammation have potential side effects, which makes it necessary to search for new sources of bioactive molecules. In this paper, we describe the ability of LASSBio-1586, an N-acylhydrazone derivative, to attenuate nociceptive behavior and the inflammatory response in mice. Antinociceptive activity was evaluated through acetic acid-induced writhing and formalin-induced nociception tests. In these experimental models, LASSBio-1586 significantly (p

Neoglaziovia variegata is a Bromeliaceae plant species widely found in Brazil with several pharmacological properties, including photoprotective activity. Although herbal-based active ingredients have been applied in cosmetic products, especially for skin treatment, its application in sunscreen formulations remains unexplored. The aim of this work is to evaluate the photoprotective effect of cosmetic formulations containing hydroalcoholic extract of N. variegata (Nv-HA). Initially, the phenolic and flavonoid total content of Nv-HA were determined. The photoprotective activity of Nv-HA was subsequently assessed using a spectrophotometric method. Nv-HA was incorporated in O/W emulsions in the presence or absence of synthetic filters and their photoprotective efficacy was evaluated by spectrophotometric SPF determination. Finally, the stability study of the formulations was performed through the freezing/defrosting method. Nv-HA showed significant phenolic and flavonoids content (61.66±5.14 mg GAE/g and 90.27±5.03 mg CE/g, resp.). Nv-HA showed SPF values of 5.43±0.07 and 11.73±0.04 for the concentrations of 0.5 and 1.0% (v/v), respectively. It was verified that Nv-HA potentiated the photoprotective effect of formulations containing only synthetic filters. Furthermore, the formulations have remained stable at the end of the preliminary stability study. According to the results, it was concluded that Nv-HA can be used as a chemical filter in cosmetic formulations.

Schinopsis brasiliensis Engl. is a native plant of Caatinga which has high concentrations of compounds capable of absorbing ultraviolet light, suggesting its potential application for the development of sunscreen preparations. After its identification and collection, this vegetable drug was submitted to a physicochemical analysis through the preparation of ethanolic extract. The phytochemical screening and analysis of extracts were carried out by high-performance liquid chromatography (HPLC) evaluation. The antioxidant activity of the extract was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and β-carotene bleaching test. Inhibitory hemolytic activity and morphological deformation of erythrocytes induced by H2O2 were also demonstrated and the antimicrobial activity was analyzed by the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) method. For the in vitro determination of the sun protection factor (SPF), the spectrophotometric method was used. From the analyses carried out with this species, this plant showed significant results for the antioxidant and antimicrobial activities, as well as sunscreen action. Important flavonoids were identified. These data are an important step for the development of new photoprotective cosmetic with Caatinga species, revealing importance and representing another incentive for the preservation of the species involved and analyzed in the study.

Reproductive tract infections are the main causes of losses from the low reproductive efficiency of sheep. Gram negative bacilli belonging to the normal flora of the genital region can trigger diseases. The pathogenicity of these agents is expressed when females are with weakened immune system, either by food or stress management. Flaws in and concern about antibiotic residues in animal production have prompted research regarding alternatives for the treatment of diseases. The herbal medicine hás been considered in this context is the subject of numerous studies. This study aimed to evaluate the antibacterial potential of ethanol extracts of plants belonging to the flora of the Northeast against gram negative bacilli isolated from cervical-vaginal mucosa of sheep. Six plants were selected from Caatinga biome: Encholirium spectabile, Bromelia laciniosa, Neoglaziovia variegata, Amburana cearensis Hymenaea martiana and Selaginella convoluta. The plant material was processed to obtain the crude extract. This was tested by microdilution plate and determining the minimum bactericidal concentration, the second document of Clinical and Laboratory Standards Institute (CLSI) and the extracts diluted in water and alcohol. We used 43 gram negative isolates, as follows: 14 E. coli, 10 Enterobacter spp., 10 Acinetobacter spp. 9 and Klebsiella spp. In the aqueous dilution Klebsiella spp. showed response only to species B. laciniosa, S. convoluta and H. martiana. All tested extracts showed antibacterial activity against Acinetobacter spp and no activity against E. coli and Enterobacter spp. Among the extracts diluted in water H. martiana showed the highest antibacterial activity. In all dilution alcoholic extracts showed inhibitory activity against all bacterial genera, but no statistical difference between them.

Annona vepretorum Mart. é uma espécie endêmica do bioma Caatinga, conhecida no Nordeste do Brasil como "araticum". Neste trabalho, o conteúdo de fenóis totais foi determinado pelo método de Folin-Ciocalteu. O teor de flavonoides totais também foi medido. A atividade antioxidante dos extratos foi analisada pelos métodos do sequestro do radical DPPH e inibição da auto-oxidação do β-caroteno, e comparada com o ácido ascórbico, BHA e BHT, utilizados como compostos de referência. A análise de citotoxidade foi realizada frente a linhagens de células HCT-116, OVCAR-8 e SF-295. O efeito antibacteriano foi avaliado pelo método de microdiluição. O conteúdo de fenóis totais do extrato etanólico (Av-EtOH) foi de 76,60 ± 5,57 mg de equivalente de ácido gálico/g. O conteúdo de flavonoides foi de 194,50 ± 11,72 mg de equivalente de catequina/g para o extrato hexânico. O extrato EtOH exibiu boa atividade antioxidante (IC50 = 98,87 ± 11,24 mg/mL) no método do DPPH. Os extratos mostraram atividade citotóxica e antibacteriana contra a maior parte das células e microrganismos testados. Pesquisas adicionais serão realizadas para o isolamento e a identificação dos principais constituintes fenólicos dos extratos.

O objetivo deste trabalho foi quantificar os teores de fenóis e flavonoides totais, bem como avaliar as atividades antioxidante e antimicrobiana de extratos obtidos dos talos e folhas de atemoia (A. cherimola Mill. x A. squamosa L.), que pertence à família Annonaceae. A atividade antioxidante foi avaliada pelos métodos de sequestro dos radicais 2,2-difenil-1-picrilhidrazil (DPPH) e 2,2'-azinobis-3-etilbenzotiazolina-6-ácido sulfônico (ABTS), bem como pelo método da cooxidação do β-caroteno/ácido linoleico. A avaliação da atividade antimicrobiana dos extratos foi analisada contra 10 cepas de bactérias. Os resultados da atividade antioxidante dos extratos mostraram que o extrato etanólico dos talos (EEt) foi o antioxidante mais efetivo (IC50 = 10,44 ± 1,25 µg/mL) no método do sequestro do DPPH, bem como no sequestro do radical ABTS (24,81 ± 0,49%). O extrato hexânico das folhas apresentou o melhor percentual de atividade antioxidante no ensaio do β-caroteno/ácido linoleico (41,12 ± 4,35%). Os extratos etanólico dos talos e metanólico das folhas mostraram-se ativos contra cepas de Bacillus cereus, Klebsiella pneumoniae, Staphylococcus aureus resistente à meticilina (MRSA), Staphylococcus aureus e Staphylococcus epidermidis.

Selaginella convoluta é uma espécie conhecida no Nordeste do Brasil como “jericó”, e bastante utilizada na medicina popular para tratamento de doenças. Este estudo teve como objetivo determinar o teor de compostos fenólicos e avaliar a atividade antioxidante in vitro do extrato etanólico e das frações obtidas por partição de S. convoluta. O conteúdo de fenóis totais foi determinado pelo método de Folin-Ciocalteu. O teor de flavonoides totais também foi avaliado. A atividade antioxidante dos extratos foi avaliada usando o método do sequestro do radical DPPH e inibição da auto-oxidação do sistema β-caroteno-ácido linoleico e comparada com os compostos de referência ácido ascórbico, BHA, BHT, quercetina e pirogalol. O conteúdo fenólico total foi de 209,90 ± 19,84 e 61,13 ± 2,50 mg equivalente de ácido gálico/g para os extratos AcOEt e EEB, respectivamente. O conteúdo de flavonoides totais foi de 155,70 ± 6,21 e 62,13 ± 4,10 para os dois extratos, respectivamente. Os extratos AcOEt e EEB apresentaram boas atividades antioxidantes. BHA foi o antioxidante mais efetivo, com um valor de IC50 de 1,62 ± 0,69 µg/mL. Os resultados obtidos mostram que S. convoluta pode ser uma boa fonte de compostos fenólicos antioxidantes. Estudos posteriores serão realizados para se chegar ao isolamento e identificação dos principais constituintes fenólicos dos extratos.

Borneol is a bicyclic monoterpenoid alcohol commonly used in traditional Chinese and Indian medicine. It is extracted from the essential oil of various medicinal plants. It has antibacterial, analgesic, and anti-inflammatory action proven in studies that used oral and intraperitoneal applications of this monoterpene in mice. The current study was designed to develop a topical gel formulation containing the monoterpene borneol using carbopol as gel base and to evaluate its stability. The prepared formulation was subjected to physical characterization and physical-chemistry assessment. The gel was prepared from carbopol and 5% of borneol. The prepared gel was subjected to pharmacotechnical tests such as its pH, viscosity, conductivity, spreadability, centrifugation, and accelerated stability with freezing-thaw cycle. The borneol was successfully incorporated into the carbopol formulation. Borneol gel (BG5) showed good stability after eight months of its development and after 12 days in the freeze-thaw cycle, not showing statistical difference in pH value, conductivity, and viscosity before and after test. Furthermore, the formulation showed a good spreadability. Therefore, it was concluded that the formulation could be very promising alternative for the topical or transdermal treatment of skin diseases.

Phytochemical investigation of Anaxagorea dolichocarpa Sprague & Sandwith led to isolation of three azaphenanthrene alkaloids: eupolauramine, sampangine and imbiline 1. Their chemical structures were established on the basis of spectroscopic data from IR, HR-ESI-MS, NMR (including 2D experiments) and comparison with the literature. Sampangine and imbiline 1 are being described in the Anaxagorea genus for the first time. Eupolauramine and sampangine show concentration-dependent antitumoral activity in leukemic cells K562 with IC50 of 18.97 and 10.95 µg/mL, respectively.

Ximenia americana L. (Olacaceae) is used in ethnomedicine as cicatrizant and for the treatment of gastric disorders. This study identified the chemical constituents of the aqueous extract of X. americana (XaAE) and evaluated its antiulcerogenic activity. After lyophilization, XaAE was analyzed by liquid chromatography-mass spectrometry (LC-MS) and its antiulcerogenic effect was evaluated in acute gastric lesions induced by ethanol, acidified ethanol, and indomethacin. Antisecretory action, mucus production and the participation of sulfhydryl groups (–SH) and nitric oxide (NO) were also investigated. The chromatographic analysis identified procyanidins B and C and catechin/epicatechin as major compounds. Oral administration of XaAE (100, 200 and 400 mg/kg) inhibited the gastric lesions induced by ethanol (76.1%, 77.5% and 100%, respectively), acidified ethanol (44.9%, 80.6% and 94.9%, respectively) and indomethacin (56.4%, 52.7% and 64.9%, respectively). XaAE reduced gastric contents and acidity (51.4% and 67.7%, respectively) but did not alter the production of gastric mucus. The reduction of the -SH and NO groups promoted by N-ethylmaleimide (NEM) and Nω-nitro-l-arginine-methyl-ester (L-NAME) respectively, reduced the gastroprotective effect of XaAE. In conclusion, XaAE has gastroprotective activity mediated in part by -SH, NO and antisecretory activity. This antiulcer action was initially correlated to its major constituents, procyanidins B and C and catechin/epicatechin.

The phytochemical investigation of Xylopia langsdorffiana led to the isolation of corytenchine, xylopinine, discretamine, xylopine, ent-atisan-16α-hydroxy-18-oic acid, 13² (S) hydroxy-17³-ethoxyphaephorbide and quercetin-3-α-rhamnoside. Their structures were assigned based on spectroscopic analyses, including two-dimensional NMR techniques. Antioxidant activities of discretamine were measured using the 1,2-diphenyl- 2-picryl-hydrazyl (DPPH) free radical scavenging assay.

O extrato etanólico bruto das folhas de M. nigra (Mn-EtOH) foi avaliado quanto à atividade antinociceptiva em modelos experimentais em camundongos. Foram usados os métodos de contorções abdominais induzidas pelo ácido acético, teste da formalina e placa quente. No teste de contorções abdominais induzidas pelo ácido acético, Mn-EtOH (100, 200 e 400 mg/kg, i.p.) reduziu o número de contorções em 38,82, 97,65 e 100%, respectivamente. O extrato também produziu uma significativa inibição de ambas as fases do teste da formalina, sendo que o efeito foi mais significativo na segunda fase (dor inflamatória). O extrato diminuiu em 42,19, 56,96 e 40,50%, respectivamente, o tempo de lambida da pata na primeira fase do teste de formalina, assim como 84,04, 77,20 e 61,07%, respectivamente, na segunda fase. Além disso, não apresentou efeito no teste da placa quente. Os dados obtidos sugerem que o extrato tem efeito antinociceptivo, provavelmente mediado através de mecanismos periféricos. Novos estudos estão sendo realizados para caracterizar o mecanismo responsável por esse efeito.Palavras-chave: Morus nigra. Moraceae. Atividade antinociceptiva. Dor. ABSTRACTAntinociceptive activity of ethanolic extract of the leaves of Morus nigra L. (Moraceae)The crude ethanolic extract of the leaves of M. nigra (Mn-EtOH) was evaluated for antinociceptive activity in mice using models of nociception. The evaluation of antinociceptive activity was carried out by the acetic acid-induced writhing, formalin and hot plate tests. In the acetic acid-induced writhing test, the Mn-EtOH (100, 200 and 400 mg/kg, i.p.) reduced the number of writhing by 38.82, 97.65 and 100%, respectively. The extract also produced a significant inhibition of both phases of the formalin test, and the effect was more significant in the second phase (inflammatory pain). The extract decreased by 42.19, 56.96 and 40.50%, respectively, the paw licking time in the first phase of the formalin test, as well as 84.04, 77.20 and 61.07%, respectively, in the second phase of this test. Also, no effect on the hot plate test was observed. The data suggest that the extract has antinociceptive activity, probably mediated via peripheral mechanisms. Pharmacological studies are continuing in order to characterize the mechanism responsible for this effect.Keywords: Morus nigra. Moraceae. Antinociceptive activity. Pain.

Os flavonóides são uma classe de compostos fenólicos que ocorrem naturalmente, presentes em plantas vasculares, especialmente em frutas e vegetais. São considerados componentesessenciais na dieta humana, uma vez que eles são as mais comuns e mais ativas substâncias antioxidantes em nossa comida. Este trabalho apresenta as principais classes de flavonóides e faz um resumo de suas atividades biológicas mais importantes.

O presente estudo teve como objetivo realizar um screening fitoquímico com a casca do caule de Diplotropis ferruginea procurando sistematizar ou rastrear os principais grupos de constituintes químicos que compõem o extrato vegetal, além de avaliar a atividade moluscicida dos extratos frente ao molusco Biomphalaria glabrata. O extrato etanólico bruto foi obtido através de maceração exaustiva com etanol a 95% e concentrado em rota evaporador. Para realização do screening fitoquímico foi utilizada a metodologia preconizada por Matos 1997, enquanto que para avaliação da atividade moluscicida utilizou-se metodologia adotada pela Organização Mundial de Saúde, 1995. No “screening” fitoquímico foram detectadas a presença de flavonóides, taninos, esteróides e terpenóides, e o extrato hexânico, na concentração de 100 g/ml, apresentou atividade moluscicida.

Este trabalho descreve alguns dos resultados de pesquisas realizadas pelos autores no Laboratório de Tecnologia Farmacêutica (LTF/UFPB) nas áreas de química e farmacologia de produtos naturais. Os resultados foram obtidos após a seleção de algumas plantas medicinais do Nordeste do Brasil, especialmente aquelas com indicações da medicina popular. Foram isolados vários constituintes químicos destas plantas, que exibiram diferentes atividades biológicas em modelos experimentais.

Extensive regional droughts are already a major problem on all inhabited continents and severe regional droughts are expected to become an increasing and extended problem in the future. Consequently, extended use of available drought resistant food plants should be encouraged. Bromelia laciniosa, Neoglaziovia variegata and Encholirium spectabile are excellent candidates in that respect because they are established drought resistant edible plants from the semi-arid Caatinga region. From a food safety perspective, increased utilization of these plants would necessitate detailed knowledge about their chemical constituents. However, their chemical compositions have previously not been determined. For the first time, the non-polar constituents of B. laciniosa, N. variegata and E. spectabile have been identified. This is the first thorough report on natural products from N. variegata, E. spectabile, and B. laciniosa. Altogether, 20 non-polar natural products were characterized. The identifications were based on hyphenated gas chromatography-high resolution mass spectrometry (GC-HRMS) and supported by 1D and 2D Nuclear Magnetic Resonance (NMR) plant metabolomics.

Medicinal plants have been widely used in the treatment of chronic pain. In this study, we describe the antinociceptive effect of the essential oil from Croton conduplicatus (the EO 25, 50, and 100 mg/kg, i.p.), a medicinal plant native to Brazil. Antinociceptive activity was investigated by measuring the nociception induced by acetic acid, formalin, hot plate and carrageenan. A docking study was performed with the major constituents of the EO (E-caryophyllene, caryophyllene oxide, and camphor). The EO reduced nociceptive behavior at all doses tested in the acetic acid-induced nociception test (p < 0.05). The same was observed in both phases (neurogenic and inflammatory) of the formalin test. When the hot-plate test was conducted, the EO (50 mg/kg) extended the latency time after 60 min of treatment. The EO also reduced leukocyte migration at all doses, suggesting that its antinociceptive effect involves both central and peripheral mechanisms. Pretreatment with glibenclamide and atropine reversed the antinociceptive effect of the EO on the formalin test, suggesting the involvement of KATP channels and muscarinic receptors. The docking study revealed a satisfactory interaction profile between the major components of the EO and the different muscarinic receptor subtypes (M2, M3, and M4). These results corroborate the medicinal use of C. conduplicatus in folk medicine.

Borneol, a bicyclic monoterpene, has been evaluated for antinociceptive and anti-inflammatory activities. Antinociceptive and anti-inflammatory activities were studied by measuring nociception by acetic acid, formalin, hot plate, and grip strength tests, while inflammation was prompted by carrageenan-induced peritonitis. The rotarod test was used to evaluate motor coordination. Borneol produced a significant (P

The ethanol extract from the fruits of Duguetia chrysocarpa was evaluated for its antinociceptive activity in chemical and thermal models of nociception in mice. The intraperitoneal administration of the ethanol extract (100, 200, and 400 mg/kg body weight) showed a dose-dependent inhibition of acetic-acid-induced abdominal writhes. The extract also produced a significant inhibition of both phases of the formalin test in all doses tested and increased the reaction time in hot-plate test at dose of 200 mg/kg. The data obtained suggest that the antinociceptive effect of the extract may be mediated via both peripheral and central mechanisms. The phytochemical investigation yielded the isolation of the benzenoid derivative 3-methoxy-4-ethoxy benzoic acid which is being reported for the first time in this genus.

ABSTRACT: This experiment was carried out to study the bioacaricidal activity of Amburana cearensis against engorged females of Rhipicephalus ( Boophilus ) microplus . The crude ethanolic extract from the leaves of A. cearensis was submitted to partition with organic solvents (hexane, chloroform and ethyl acetate) in order of increasing polarity; and evaluated using three treatments at concentrations of 5, 10 and 25mg ml-1. To evaluate the acaricidal activity, engorged females were submitted to the adult immersion test. Parameters analyzed were the weight of females; weight of egg mass; percentage of hatch; reproductive efficiency; expected rate of reproduction; and efficacy. For each extract and concentrating fraction, tests were performed in triplicate. Among all fractions, the hexane (2.5%) achieved the best results in all parameters analyzed: 52.7% of inhibition of oviposition; 39% of hatching rate; 3,271 index of reproductive efficiency; and 67.0% effectiveness. The extract obtained gradual dose response with increasing concentration; and could be used as an aid in the control of R. ( B. ) microplus therapy.

Abstract Background: D-limonene (DL) is a monoterpene and is the major component in the essential oil of citrus fruit. It presents antihyperglycemic and vasodilatation activities. Objectives: This study evaluated the cardiovascular effects and potential antiarrhythmic of DL in rats. Methods: Hemodynamic and electrocardiographic (ECG) parameters were measured in male Wistar rats, which under anesthesia had been cannulated in the abdominal aorta and lower vena cava and had electrodes subcutaneously implanted. In the in vitro approach, the heart was removed and perfused using the Langendorff technique. The significance level adopted was 5% (p < 0.05). Results: DL, in doses of 10, 20, and 40 mg/kg (i.v), produced intense and persistent bradycardia associated with hypotension. Bradycardia with prolonged QTc was observed in the ECG in vivo recording. In the in vivo model of arrhythmia induced by Bay K8644, DL (10 mg/kg) decreased the arrhythmia score from 15.33 ± 3.52 to 4.0 ± 2.64 u.a (p < 0.05, n = 4). In isolated perfused hearts, DL (10-3 M) promoted significant reductions in heart rate (from 228.6 ± 8.5 ms to 196.0 ± 9.3 bpm; p < 0.05) and left ventricular development pressure (from 25.2 ± 3.4 to 5.9 ± 1.8 mmHg; n = 5, p < 0.05). Conclusions: DL produces bradycardia and antiarrhythmic activity in rat heart.