Polyphenols, Antioxidants, and Wound Healing of Lecythis pisonis Seed Coats.

To better use the Lecythis pisonis Cambess. biomass, this study investigates whether Sapucaia seed coats present wound healing properties. We analyzed the antibacterial, antioxidant, and wound healing-promoting potentials, plus cytotoxicity and stimulation of vascular endothelial growth factor-A. The chemical composition was analyzed by positive ion mode electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry. A total of 19 compounds were identified, such as proanthocyanidin A1, procyanidins A1, B2, and C1, epigallocatechin, and kaempferol (p-coumaroyl) glycoside. Potent antioxidant strength/index was verified for 2,2-diphenyl-1-picrylhydrazyl radical (IC50 = 0.99 µg/mL) and ferric reducing antioxidant power (IC50 = 1.09 µg/mL). The extract did not present cytotoxicity and promoted significant cell migration and/or proliferation of fibroblasts (p < 0.05). Vascular endothelial growth factor-A was stimulated dose-dependently at 6 µg/mL (167.13 ± 8.30 pg/mL), 12.5 µg/mL (210.3 ± 14.2 pg/mL), and 25 µg/mL (411.6 ± 29.4 pg/mL). Platelet-derived growth factor (PDGF) (0.002 µg/mL) was stimulated at 215.98 pg/mL. Staphylococcus aureus was susceptible to the extract, with a minimum inhibitory concentration of 31.25 µg/mL. The identified compounds benefit the antioxidant activity, promoting hemostasis for the wound healing process, indicating that this extract has the potential for use in dermatological cosmetics.

Toxicological effects of air settled particles from the Vitoria Metropolitan Area mediated by oxidative stress, pro-inflammatory mediators and NFΚB pathway.

Atmospheric pollution is a major environmental and public health risk due to its effect on global air quality and climate. Increase in pollutants concentrations, especially particulate matter (PM), are associated with increased respiratory diseases. The pathophysiology of respiratory diseases involves molecular and cellular mechanisms as inflammatory biomarkers and reactive oxygen species production. Thus, the present study aimed to investigate the in vitro cytotoxic and pro-inflammatory effects of particulate matter (PM) of six monitoring stations (1-6) from the Vitoria Metropolitan Area (VMA), Espirito Santo, Brazil in 2018. The PM was chemically characterized by inductively coupled plasma mass spectrometry. In vitro cytotoxic effects of PM (3.12-200.0 µg/mL) were analyzed in human lung epithelial cells (A549) and macrophage cells (RAW 264.7) by MTT assay (3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide). To investigate the pro-inflammatory effects of PM in RAW 264.7 cells, the levels of proinflammatory mediators such as nitric oxide (NO), superoxide anion (O2•-), tumor necrosis factor (TNF-α), interleukin 6 (IL-6), and the activation of nuclear factor kappa B (NF- κB) were measured. The comet assay evaluated genotoxicity. Cell cycle, oxidative stress (DCF and DHE), and apoptosis were analyzed by flow cytometry. Chemical analysis of PM revealed aluminum (Al) and Iron (Fe) as the major chemical elements in all studied monitoring stations. In addition, worrying concentrations of mercury (Hg) were detected in the PM. The in vitro results showed that PM presents a dose-dependent cytotoxic effect in macrophage and pulmonary epithelial cell lines. The PM increased the production of NO, O2•-, and pro-inflammatory cytokines TNF-α and IL-6. PM also promoted alterations in the cell cycle, increased apoptosis frequency, and DNA damage. Moreover, PM increased the expression NF-κB. In addition, a positive correlation between Al and Fe and ROS production was observed. Based on the results obtained during the study period, it was concluded that the sedimented particles from the VMA might have deleterious effects on human health, which was evidenced by the increase in oxidative stress, an increase in pro-inflammatory mediators, and genotoxic effects partially mediated by the NF-κB pathway. These results add aspects to elucidate the molecular mechanisms involved in the effects of sedimented particles in vivo and in vitro.

In vitro and in vivo anti-inflammatory activity and chemical composition of Renealmia petasites Gagnep.

The study aimed to investigate the chemical composition and the anti-inflammatory activity of the hydroethanolic rhizomes, stems, and leaf extracts of Renealmia petasites using in vitro and in vivo assays. The chemical composition of the extracts was characterized in a linear iron trap mass spectrometer. Total phenolic, flavonoid, and tannin content were determined by spectrophotometry analyses. In vitro anti-inflammatory activity was investigated in lipopolysaccharide-stimulated macrophages evaluating the influence on the production of superoxide anion (O2-), nitric oxide (NO), and the pro-inflammatory cytokines tumor necrosis factor (TNF-α) and interleukin-6 (IL-6). In vivo effects were determined using the air pouch model in which were inoculated carrageenan and thereafter treated with 50 mg/kg of the hydroethanolic extracts of R. petasites. After 4 and 24 h, the cellular influx, protein exudation, cytokines, and nitric oxide were evaluated. Eight compounds were tentatively identified in the R. petasites extracts, suggesting five diarylheptanoids, one flavonoid, and two fatty alcohols. The in vitro results showed that the extracts were capable of blocking free radicals and/or inhibiting their intracellular actions by inhibiting the production of important mediators of the inflammatory process, such as NO, O2-, TNF-α, and IL-6. In vivo, R. petasites significantly decrease the influx of leukocytes, mainly neutrophils, protein exudation, NO, TNF-α, and IL-6 concentration in the air pouch model. The results evidenced that R. petasites can be considered a promising alternative therapy for the treatment and management of osteoarthritis and other inflammatory diseases.

Effect of silver nanoparticles (AgNP's) from Duddingtonia flagrans on cyathostomins larvae (subfamily: cyathostominae).

The in vitro effect of silver nanoparticles of the Duddingtonia flagrans filtrate enriched with chitin was evaluated on infective larvae of cyathostomins (L3). After biosynthesis, an assay was carried out with two experimental groups in microtubes, for a period of 24 h: G1 (AgNP's-D. flagrans (43.4 µg/mL) + 120 L3) and G2 (distilled water + 120 L3). At the end of this period, AgNP's-D. flagrans (G1) demonstrated an effect on L3 with a 43% reduction (p < 0.01) in relation to G2. Thus, the authors suggest new designs with AgNP's-D. flagrans for the control of cyathostomins.

Stability and Cytotoxicity of a Cosmetic Cream Containing Oil from Lecythis pisonis Cambess (Sapucaia) Nuts.

Lecythis pisonis nuts are rich in tocopherols, polyphenols, and fatty acids, and hence, the quality of oil was analyzed for use in the elaboration of skin cream. Nut oil was extracted with hexane in a Soxhlet apparatus. The quality and safety of the oil were tested by using established protocols from Adolf Lutz Institute. Three concentrations, 1%, 5%, and 10%, of oil were incorporated into a formulated cream. The oil formulations were evaluated for their stability, organoleptic characteristics, pH, viscosity, spreadability, challenge test, cellular viability, and their response to microbial contamination, as recommended by the National Health Surveillance Agency (ANVISA). Quality analysis demonstrated the high quality of the obtained oil, with no traces of heavy metals and no toxic effects on ingestion. The cream containing L. pisonis nut oil is stable, has an effective preservative system, and is considered safe for use because it presented no toxicity in human cells. A stabilizer is required to maintain the pH in the range suitable for a body cream. Of the formulations tested, the cream containing 5% nut oil was the most stable and had presented the best organoleptic characteristics.

Lack of Standardization in Commercial Thickeners Used in the Management of Dysphagia.

INTRODUCTION: Oral feeding safety is necessary to provide nutrition, hydration, and eating pleasure for patients with dysphagia. Commercial thickeners are prescribed for these patients to change food viscosity and may alter the proper preparation of modified food. OBJECTIVE: Analyze composition, employed terminology, preparation instructions, recommended amount and weight of provided measuring spoons, nutritional information, and viscosity of 7 commercial thickeners. METHODS: The sample comprised all thickeners from different brands available in Brazil, named A to G. Products were submitted to viscosity analysis using viscometer and the International Dysphagia Diet Standardization Initiative (IDDSI) test. Samples were prepared with mineral water (25°C) and with the amount of thickener recommended to obtain intermediate viscosity (level 2) according to the manufacturer's instructions. RESULTS: Products B, C, and E presented similar composition. Manufacturer's information about the amount and preparation procedure, time, temperature, and base liquid was incomplete. Viscosity tests revealed that thickener C was basically solid while D displayed results out of the desired viscosity level. CONCLUSIONS: The study showed differences in components and viscosity, beyond the lack of label details. There was no established correlation between viscosity classifications provided by National Dysphagia Diet and IDDSI.

In vitro anti-inflammatory activity of terpenes via suppression of superoxide and nitric oxide generation and the NF-κB signalling pathway.

BACKGROUND AND AIMS: Terpenes are considered the main components of essential oils and an important source for the identification of novel lead molecules. This study aimed to investigate the in vitro anti-inflammatory activity of L-carveol, L-carvone, and m-cimene (monoterpenes) and of valencene and guaiene (sesquiterpenes). METHODS: The influence on intracellular nitric oxide (NO) and pro- and anti-inflammatory cytokine (TNF-α, IL-1α and IL-10) production and on nuclear factor kappa B (NF-κB) activity was determined using Griess reagent, immunoenzymatic assay kits (ELISA) and chemiluminescence measurements in cell-based assays, respectively. Antioxidant activity was assayed through the protective effect against cellular oxidative damage produced by superoxide anion production (O 2 ·- ) and hydrogen peroxide on macrophages and by the quenching activity of the NO radical. RESULTS AND DISCUSSION: Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O 2 ·- production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 µM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.

Antibacterial Activity of Terpenes and Terpenoids Present in Essential Oils.

Background: The antimicrobial activity of essential oils has been reported in hundreds of studies, however, the great majority of these studies attribute the activity to the most prevalent compounds without analyzing them independently. Therefore, the aim was to investigate the antibacterial activity of 33 free terpenes commonly found in essential oils and evaluate the cellular ultrastructure to verify possible damage to the cellular membrane. Methods: Screening was performed to select substances with possible antimicrobial activity, then the minimal inhibitory concentrations, bactericidal activity and 24-h time-kill curve studies were evaluated by standard protocols. In addition, the ultrastructure of control and death bacteria were evaluated by scanning electron microscopy. Results: Only 16 of the 33 compounds had antimicrobial activity at the initial screening. Eugenol exhibited rapid bactericidal action against Salmonella enterica serovar Typhimurium (2 h). Terpineol showed excellent bactericidal activity against S. aureus strains. Carveol, citronellol and geraniol presented a rapid bactericidal effect against E. coli. Conclusions: The higher antimicrobial activity was related to the presence of hydroxyl groups (phenolic and alcohol compounds), whereas hydrocarbons resulted in less activity. The first group, such as carvacrol, l-carveol, eugenol, trans-geraniol, and thymol, showed higher activity when compared to sulfanilamide. Images obtained by scanning electron microscopy indicate that the mechanism causing the cell death of the evaluated bacteria is based on the loss of cellular membrane integrity of function. The present study brings detailed knowledge about the antimicrobial activity of the individual compounds present in essential oils, that can provide a greater understanding for the future researches.

Wound healing activity of terpinolene and α-phellandrene by attenuating inflammation and oxidative stress in vitro.

This study was undertaken to investigate the in vitro wound healing effects and the anti-inflammatory and antioxidant activities of terpinolene and α-phellandrene. The in vitro stimulatory effects on the proliferation and migration of fibroblasts were assessed using the scratch assay. The anti-inflammatory activity was evaluated using cell-based assays by investigating their influence on nitric oxide (NO), superoxide anion (O2•-), tumour necrosis factor-alpha (TNF-α) and interleukin 6 (IL-6) production and using the TNF-α-induced nuclear factor kappa (NF-κB) assay. Antioxidant activity was determined by the ABTS cation radical scavenging capacity, ferric reducing/antioxidant potential (FRAP), and NO free radical scavenging assays. Terpinolene and α-phellandrene significantly increased the migration and proliferation of fibroblasts and suppressed the pro-inflammatory cytokines IL-6 and TNF-α in a dose-dependent manner. Terpinolene and α-phellandrene at a concentration of 100 µM significantly inhibited NO production (41.3 and 63.8%, respectively) in a macrophage cell-culture-based assay, and resulted in reductions in O2•- production of 82.1 ±â€¯3.5% and 70.6 ±â€¯4.3%, respectively. Moreover, these monoterpenes were verified to suppress NF-κB activity. In summary, terpinolene and α-phellandrene may contribute to broadening clinical options in the treatment of wounds by attenuating inflammation and oxidative stress in vitro.

Antioxidant, antimicrobial and cytotoxic activities of gold nanoparticles capped with quercetin.

In the present work, we report the antioxidant, antimicrobial and cytotoxic activities of quercetin-capped gold nanoparticles (AuNPsQct). The synthesis of AuNPsQct was confirmed by UV-Vis spectroscopy, FTIR and transmission electron microscopy (TEM) analyses. The FTIR spectrum showed the integrity of the quercetin molecules on the nanoparticle surface. The TEM images showed sizes less than 100 nm and a slight spherical shape. The electrostatic stability was confirmed by the zeta potential method. The antioxidant activity of quercetin, evaluated by DPPH, ABTS and nitric oxide free radical scavenging methods, was preserved in the gold nanoparticles, furthermore quercetin-capped gold nanoparticles (IR50 0.37 µg/mL) demonstrated a higher antioxidant activity than free quercetin (IR50 0.57 µg/mL) by nitric oxide free radical scavenging method. Strong antifungal activity was observed for Aspergillus fumigatus with concentrations ranging from 0.1 to 0.5 mg/mL. The nanoparticles with quercetin did not exhibit cytotoxicity to human fibroblasts (L929 cells). In conclusion, these results suggest that AuNPsQct, produced by cost-effective method, can act as a promising candidate for different medical applications.

Maltodextrin and Gum Arabic-Based Microencapsulation Methods for Anthocyanin Preservation in Juçara Palm (Euterpe edulis Martius) Fruit Pulp.

The juçara fruits (Euterpe edulis Martius), native to the Atlantic Forest, are rich in anthocyanins. To preserve the anthocyanins in juçara fruit pulp, this study aimed to evaluate the effectiveness of microencapsulation by spray drying and freeze drying with maltodextrin (dextrose equivalent 16.5 to 19.5) and gum arabic in different proportions. The obtained microparticles were characterized by quantifying the total polyphenol and anthocyanin contents, by performing differential scanning calorimetry, thermogravimetry, and infrared spectroscopy and by using scanning electron microscopy to analyze the morphology of the particles. The total amount of polyphenols in the fruit pulp was 750 ± 16.7 mg GAE/100 g of the freeze-dried sample. The total anthocyanins in the fruit pulp was 181.25 ± 5.36 (mg/100 g). The microparticles were formed by employing maltodextrin and gum arabic in a 1:1 proportion as the polymeric matrix; the mixtures of pulp and polymeric matrix were prepared in proportions of 2:3 and 2:1, preserving up to 83.69% of the anthocyanin content. Lyophilization of the 2:1 mixture resulted in an anthocyanin content of 116.89 ± 4.43 (mg/100 g), whereas lyophilization of the 2:3 mixture resulted in 151.68 ± 1.39 (mg/100 g) anthocyanin content, which did not differ from the value obtained by spray drying the 2:3 mixture (150.76 ± 5.79 (mg/100 g)). Thermal analyses showed that the microparticles obtained by freeze drying at a ratio of 2:3 presented greater resistance to degradation with increasing temperature. The incorporation of the pulp in the polymeric matrix was demonstrated by IR analyses. Microparticles obtained by freeze drying showed the formation of various-sized flakes, whereas those obtained by spray drying were spherical in shape. Microencapsulation is a possible alternative for improving the stability of the anthocyanins in this fruit.

In Vitro and In Vivo Anti-inflammatory Effects of Struthanthus vulgaris.

Struthanthus vulgaris is probably the most common medicinal mistletoe plant in Brazil, and has been used in folk medicine as an anti-inflammatory agent and for cleaning skin wounds. Our proposal was to evaluate the anti-inflammatory activity of S. vulgaris ethanol leaf extract and provide further insights of how this biological action could be explained using in vitro and in vivo assays. In vitro anti-inflammatory activity was preliminarily investigated in lipopolysaccharide/interferon gamma-stimulated macrophages based on their ability to inhibit nitric oxide production and tumor necrosis factor-alpha. In vivo anti-inflammatory activity of S. vulgaris ethanol leaf extract was investigated in the mice carrageenan-induced inflammation air pouch model. The air pouches were inoculated with carrageenan and then treated with 50 and 100 mg/kg of S. vulgaris ethanol leaf extract or 1 mg/kg of dexamethasone. Effects on the immune cell infiltrates, pro- and anti-inflammatory mediators such as tumor necrosis factor-alpha, interleukin 1, interleukin 10, and nitric oxide, were evaluated. The chemical composition of S. vulgaris ethanol leaf extract was characterized by LC-MS/MS. In vitro S. vulgaris ethanol leaf extract significantly decreased the production of nitric oxide and tumor necrosis factor-alpha in macrophages and did not reveal any cytotoxicity. In vivo, S. vulgaris ethanol leaf extract significantly suppressed the influx of leukocytes, mainly neutrophils, protein exudation, nitric oxide, tumor necrosis factor-alpha, and interleukin 1 concentrations in the carrageenan-induced inflammation air pouch. In conclusion, S. vulgaris ethanol leaf extract exhibited prominent anti-inflammatory effects, thereby endorsing its usefulness as a medicinal therapy against inflammatory diseases, and suggesting that S. vulgaris ethanol leaf extract may be a source for the discovery of novel anti-inflammatory agents.

Cardiovascular Activity of the Chemical Constituents of Essential Oils.

Cardiovascular diseases are a leading cause of death in developed and developing countries and decrease the quality of life, which has enormous social and economic consequences for the population. Recent studies on essential oils have attracted attention and encouraged continued research of this group of natural products because of their effects on the cardiovascular system. The pharmacological data indicate a therapeutic potential for essential oils for use in the treatment of cardiovascular diseases. Therefore, this review reports the current studies of essential oils chemical constituents with cardiovascular activity, including a description of their mechanisms of action.

Potential anti-inflammatory, antioxidant and antimicrobial activities of Sambucus australis.

CONTEXT: Sambucus australis Cham. & Schltdl. (Adoxaceae) is used in Brazilian folk medicine to treat inflammatory disorders. OBJECTIVE: To evaluate the in vitro anti-inflammatory, antioxidant and antimicrobial properties of S. australis. MATERIALS AND METHODS: The anti-inflammatory activity of ethanol extracts of the leaf and bark of S. australis (1-100 µg/mL) were studied in lipopolysaccharide/interferon γ stimulated murine macrophages RAW 264.7 cells (24 h incubation) by investigating the release of nitric oxide (NO) and tumour necrosis factor-alpha (TNF-α) and in the TNF-α-induced nuclear factor kappa (NF-κB) assay. Minimum inhibitory concentration (MIC) was determined by the microdilution test (24 h incubation). Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and the NO scavenging assays. Chemical composition was assessed by LC-MS/MS. RESULTS: Antioxidant activities in the DPPH (IC50 43.5 and 66.2 µg/mL), FRAP (IC50 312.6 and 568.3 µg/mL) and NO radical scavenging assays (IC50 285.0 and 972.6 µg/mL) were observed in the leaf and bark ethanol extracts, respectively. Solely the leaf extract showed significant inhibition of NO and TNF-α production in RAW264.7 cells at concentrations of 2 and 100 µg/mL, respectively, and suppression of TNF-α inhibition of NF-κB by 12.8 and 20.4% at concentrations of 50 and 100 µg/mL, respectively. The extract also exhibited antibacterial activity against Salmonella typhimurium (MIC 250 µg/mL) and Klebsiella pneumoniae (MIC 250 µg/mL). LC-MS/MS revealed the presence of chlorogenic acid and rutin as major compounds. DISCUSSION AND CONCLUSION: The results indicate that the ethanol leaf extract of S. australis exhibit prominent anti-inflammatory effects.

Gastroprotective activity of the resin from Virola oleifera.

CONTEXT: The resin from the trunk wood of Virola oleifera (Schott) A. C. Smith (Myristicaceae) is used in folk medicine to hasten wound repair and to treat pain and inflammatory conditions, and our previous report indicated the anti-oxidative properties in other oxidative stress model. OBJECTIVE: To investigate the protective effects of resin from V. oleifera in two experimental models of gastric ulcer oxidative-stress dependent. MATERIALS AND METHODS: Plant material was collected and the resin was subjected to partitioning with organic solvents. The buthanol fraction was subjected to chromatographic and spectrometric methods for isolation and structural elucidation. The resin was quantified for polyphenols and flavonoids by colorimetric methods. Furthermore, the antioxidant activity of resin was determined by three different methods. The ulcers were induced acutely in Swiss male mice with ethanol/HCl and indomethacin using single-doses of 10 and 100 mg/kg. The gastroprotection of the experimental groups was comparable to reference control lansoprazole (3 mg/kg). RESULTS: The high content of polyphenols (∼82%) and the presence of epicatechin and eriodictyol were determined. The LD50 was estimated at 2500 mg/kg. At minimum (10 mg/kg) and maximum (100 mg/kg) dosage of resin, both in ethanol/HCl as indomethacin ulcer induction models demonstrate reduction of lesions (minimum: ∼97% and ∼66%; maximum: ∼95% and ∼59%). DISCUSSION: The gastroprotection might be related to tannins, phenolic acids and flavonoids present in the resin by antioxidant properties. CONCLUSIONS: The results indicate that this resin has gastroprotective activity probably associated with the presence of phenolic antioxidant substances.

Effects of ß-caryophyllene and Murraya paniculata essential oil in the murine hepatoma cells and in the bacteria and fungi 24-h time-kill curve studies.

CONTEXT: Orange Jessamine [Murraya paniculata L. (Rutaceae)] has been used worldwide in folk medicine as an anti-inflammatory, antibiotic and analgesic. OBJECTIVE: The objective of this study is to investigate the in vitro antioxidant, cytotoxic, antibacterial and antifungal activity and the time-kill curve studies of orange jessamine essential oil and ß-caryophyllene, as well as the chemical composition of the essential oil. MATERIAL AND METHODS: The cytotoxic activity of M. paniculata and ß-caryophyllene (7.8-500 µg/mL) was evaluated using the MTT assay on normal fibroblasts and hepatoma cells. The minimal inhibitory concentration and time-kill curves (24 h) were evaluated against those of Staphylococcus aureus, Escherichia coli, Salmonella typhimurium, Enterococcus faecallis, Aspergillus (niger, fumigates and parasiticum) and F. solani by the broth microdilution method. The antioxidant activity was measured by the DPPH and ABTS assays. Chemical composition was evaluated by GC/MS analyses. RESULTS: GC/MS analyses identified 13 compounds, with ß-caryophyllene as the major compound. The oil exhibited moderate antibacterial activity (MIC <1.0 mg/mL) and strong antifungal activity. Time-kill curve studies showed that either the essential oil or ß-caryophyllene presented rapid bacterial killing (4 h for S. aureus) and fungicidal effect (2-4 h for F. solani); however, both displayed weak free radical scavenger capacity. The cytotoxic activity exhibited a prominent selective effect against hepatoma cancer cells (IC50 value =63.7 µg/mL) compared with normal fibroblasts (IC50 value =195.0 µg/mL), whereas the ß-caryophyllene showed low cytotoxicity. DISCUSSION AND CONCLUSION: The experimental data suggest that the activities of M. paniculata essential oil are due to the synergistic action among its components.

Relationship between male hormonal status, Bezold-Jarisch reflex function, and ACE activity (cardiac and plasmatic).

The negative relationship between androgens and the Bezold-Jarisch reflex (BJR) has been demonstrated, but no studies evaluated the physiological influence of testosterone on this reflex. We evaluated the influence of male rat castration on the BJR, cardiac morphometric parameters, and the plasmatic and the cardiac angiotensin converting enzyme (ACE) activity. After castration (CAS), the rats were divided into 24 and 72 h (CAS24H, CAS72H), and 7 and 21 days (CAS7D, CAS21D) groups. The BJR was studied by administering increasing doses of phenylbiguanide (PBG; 1.5-24 µg/kg) at different times after castration. Castration results in the following: (i) reduction in testosterone levels (SHAM: 238.7 ± 15.1; CAS24H: 9.0 ± 0.5; CAS72H: 6.7 ± 0.4; CAS7D: 5.2 ± 0.2; and CAS21D: 2.2 ± 0.3 ng/dL; p < 0.05); (ii) no changes in 17ß-estradiol; (iii) a reduced BJR sensitivity (PBG 6 µg/kg; SHAM: 77 ± 7; CAS24H: 63 ± 10; CAS72H: 55 ± 6; CAS7D: 54 ± 4; and CAS21D: 35 ± 2%; p < 0.01); (iv) a decrease in cardiac (SHAM: 107 ± 6; CAS24H: 92 ± 2; CAS72H: 82 ± 3; CAS7D: 54 ± 3; and CAS21D: 43 ± 4%; p < 0.05) and plasmatic (SHAM: 135 ± 8; CAS24H: 102 ± 5; CAS72H: 99 ± 3; CAS7D: 89 ± 4; and CAS21D: 56 ± 6%; p < 0.05) ACE activity. No changes were observed in cardiac morphometry and hemodynamic parameters. Therefore, castration leads to decrease in testosterone levels as early as 24 h, reduction in ACE activity and loss of BJR sensitivity 7 days after castration. The loss of BJR sensitivity was not related to cardiac morphometric changes and cardiovascular hemodynamics.

Antioxidant, antimicrobial and wound healing properties of Struthanthus vulgaris.

CONTEXT: Struthanthus vulgaris (Vell.) Mart. (Loranthaceae) has been widely used in traditional medicine in Brazil to bathe wounds. OBJECTIVE: The objective of this study is to investigate the in vitro wound healing effects, together with the antioxidant and antimicrobial activities of S. vulgaris leaf and branch extracts. MATERIAL AND METHODS: Ethanol leaf and branch extracts of S. vulgaris were investigated at 1-100 µg/ml concentrations in the scratch assay after 14 h. Antioxidant activity was investigated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay, and the antibacterial activity was tested at concentrations up to 1000 µg/ml against Gram-positive and Gram-negative bacteria by the microdilution test after 24 h. The total phenolic and flavonoid contents were determined by colorimetric methods. RESULTS: Struthanthus vulgaris leaf and branch extracts at 100 µg/ml concentration stimulated migration and proliferation of fibroblasts and enhanced cell numbers by 56.2% and 18.6%, respectively. Antioxidant activity exhibited IC50 values of 24.3 and 18.9 µg/ml for the leaf and branch extracts, respectively. The ethanol leaf extract showed antimicrobial activity against the Gram-positive Staphylococcus mutans and Staphylococcus aureus bacteria, exhibiting minimum inhibitory concentration values of 125 and 500 µg/ml, respectively. An appreciable total phenolic content in the leaves (813.6 ± 2.7 mg/g) and branches (462.8 ± 9.6 mg/g), and relatively low concentration of flavonoids in the leaves (13.3 ± 4.3 mg/g) and branches (1.9 ± 0.2 mg/g), was detected. DISCUSSION AND CONCLUSION: The antioxidant and antibacterial activities, together with the strong ability to stimulate proliferation and migration of fibroblasts, provide some support for the traditional use of S. vulgaris.

Cardiopulmonary reflex, cardiac cytokines, and nandrolone decanoate: response to resistance training in rats.

This study evaluated the effects of nandrolone associated with resistance training (RT) on cardiac cytokines, angiotensin-converting enzyme activity (ACEA), and the sensitivity of the Bezold-Jarisch reflex (BJR). Male Wistar rats were divided into 3 groups: CONT (received vehicle, no training); EXERC (RT: after one week of water adaptation, rats were exercised by jumping into water twice a week for 4 weeks), and ND+EXERC (received nandrolone decanoate 10 mg/kg, twice/week, i.m, associated with RT). The BJR was analysed by measuring bradycardic and hypotensive responses elicited by serotonin administration. Myocyte hypertrophy and matrix collagen deposition were determined by morphometric analysis of H&E and picrosirius red-stained samples, respectively. TNF-α and ACEA were also studied. RT promoted physiological myocyte hyrpertrophy but did not cause changes in the other parameters. The association of ND with RT increased myocyte hypertrophy, deposition of matrix type I collagen, TNF-α and ACEA; decreased IL-10, and impairment in the BJR were observed in ND+EXERC compared with CONT and EXERC. ND is associated with alterations in cardiac structure and function as a result of the development of pathological cardiac hypertrophy (cardiac cytokine imbalance, elevation of ACEA) and cardiac injury, even when combined with resistance training.

Antihypertensive effect of Carica papaya via a reduction in ACE activity and improved baroreflex.

The aims of this study were to evaluate the antihypertensive effects of the standardised methanolic extract of Carica papaya, its angiotensin converting enzyme inhibitory effects in vivo, its effect on the baroreflex and serum angiotensin converting enzyme activity, and its chemical composition. The chemical composition of the methanolic extract of C. papaya was evaluated by liquid chromatography-mass/mass and mass/mass spectrometry. The angiotensin converting enzyme inhibitory effect was evaluated in vivo by Ang I administration. The antihypertensive assay was performed in spontaneously hypertensive rats and Wistar rats that were treated with enalapril (10 mg/kg), the methanolic extract of C. papaya (100 mg/kg; twice a day), or vehicle for 30 days. The baroreflex was evaluated through the use of sodium nitroprusside and phenylephrine. Angiotensin converting enzyme activity was measured by ELISA, and cardiac hypertrophy was evaluated by morphometric analysis. The methanolic extract of C. papaya was standardised in ferulic acid (203.41 ± 0.02 µg/g), caffeic acid (172.60 ± 0.02 µg/g), gallic acid (145.70 ± 0.02 µg/g), and quercetin (47.11 ± 0.03 µg/g). The flavonoids quercetin, rutin, nicotiflorin, clitorin, and manghaslin were identified in a fraction of the extract. The methanolic extract of C. papaya elicited angiotensin converting enzyme inhibitory activity. The antihypertensive effects elicited by the methanolic extract of C. papaya were similar to those of enalapril, and the baroreflex sensitivity was normalised in treated spontaneously hypertensive rats. Plasma angiotensin converting enzyme activity and cardiac hypertrophy were also reduced to levels comparable to the enalapril-treated group. These results may be associated with the chemical composition of the methanolic extract of C. papaya, and are the first step into the development of a new phytotherapic product which could be used in the treatment of hypertension.