Syagrus coronata fixed oil prevents rotenone-induced movement disorders and oxidative stress in Drosophila melanogaster.

One prominent aspect of Parkinson's disease (PD) is the presence of elevated levels of free radicals, including reactive oxygen species (ROS). Syagrus coronata (S. coronata), a palm tree, exhibits antioxidant activity attributed to its phytochemical composition, containing fatty acids, polyphenols, and flavonoids. The aim of this investigation was to examine the potential neuroprotective effects of S. coronata fixed oil against rotenone-induced toxicity using Drosophila melanogaster. Young Drosophila specimens (3-4 d old) were exposed to a diet supplemented with rotenone (50 µM) for 7 d with and without the inclusion of S. coronata fixed oil (0.2 mg/g diet). Data demonstrated that rotenone exposure resulted in significant locomotor impairment and increased mortality rates in flies. Further, rotenone administration reduced total thiol levels but elevated lipid peroxidation, iron (Fe) levels, and nitric oxide (NO) levels while decreasing the reduced capacity of mitochondria. Concomitant administration of S. coronata exhibited a protective effect against rotenone, as evidenced by a return to control levels of Fe, NO, and total thiols, lowered lipid peroxidation levels, reversed locomotor impairment, and enhanced % cell viability. Molecular docking of the oil lipidic components with antioxidant enzymes showed strong binding affinity to superoxide dismutase (SOD) and glutathione peroxidase (GPX1) enzymes. Overall, treatment with S. coronata fixed oil was found to prevent rotenone-induced movement disorders and oxidative stress in Drosophila melanogaster.

Dry residue of cassava on slow-growing broiler diets, with or without the addition of carbohydrases.

Dry residue of cassava was studied on the digestibility, performance, intestinal measurements, with or without inclusion of carbohydrases, of slow-growing broilers. 160 Label Rouge broiler chickens, 21-d-old, were distributed in a randomized, 2x5 factorial arrangement (male and female x 0, 10, 20, 30 and 40% residue) (metabolism trial). 1,100 male chicks were distributed in a 2x5 factorial arrangement (with/without carbohydrases x 0; 2.5; 5.0; 7.5; and 10.0% residue), with five replicates (performance trial). Increasing residue levels led to increases in energetic values. Feed intake from 1-21-d-old and 1-63-d-old decreased linearly. At 42 d-old, feed intake and weight gain levels exhibited a quadratic response, which predicted a highest value at 3.32% and 4.77%, respectively, for diets without carbohydrases. For 21- and 42-d-old chickens, the inclusion of carbohydrases reduced the weight and length of the small intestine. The energetic values of the diets were positively influenced by the residue and had similar digestibility values for both sexes. Inclusion of up to 10% of residue in slow-growing broiler diets does not impaired performance and intestinal morphology. The addition of carbohydrases reduced the viscosity of the digesta but it was not enough to improve the performance of the birds.

Performance and bone characteristics of broilers fed diets supplemented with vitamin A at different concentrations.

This work evaluated the influence of vitamin A on performance, organ weight, and bone and skin characteristics in broilers (Cobb 500) at 21 and 42 days of age. A total of 1920 chickens were distributed in a randomised design, considering six vitamin A supplementation levels (0, 6000, 16,000, 26,000, 36,000, and 46,000 IU kg-1 ), with 16 replicates and 20 chickens per experimental unit, established due to rising the range of vitamin levels observed in the literature to evaluate the effect of vitamin A on broilers. At 22 days, half of the replicates from each treatment continued receiving the initial diet, and the other eight repetitions received diets without vitamin A (0 IU kg-1 ) until 42 days. The level of vitamin A influenced feed intake (FI) and body weight gain (BWG) until 21 days for all treatments. Broilers at 21 days of age had a more significant BWG at a vitamin A supplementation level of 28,209 IU kg-1 . At 42 days, vitamin A influenced the BWG and FI of broilers at treatments that were not supplemented after 21 days. Treatments supplemented up to 42 days showed quadratic responses to vitamin A for BWG, FI, and feed conversion. The vitamin A levels influenced the relative weights of the small intestine, pancreas, gizzard, abdominal fat, Seedor index, and breaking strength at 42 days, where the adequate supplementation of vitamin A improved these characteristics in broilers. Vitamin A supplementation from 22 to 42 days old did not affect broiler performance. An increased BWG was obtained when vitamin A supplementation occurred until 42 days, with supplementation of 29,375 IU kg-1 and a lower response of feed conversion with the addition of 27,775 IU kg-1 .

Effects of feeding diets with zinc-l-selenomethionine on growth performance of broilers subjected to cyclic heat stress.

Limited information exists on the use of zinc-l-selenomethionine (Zn-L-SeMet) in broiler diets and its effects on the growth performance, body temperature, mortality rates, blood profile, and gene expression, especially when animals are reared under cyclic heat stress conditions. This study aimed to investigate the impact of Zn-L-SeMet in broiler diets from 1 to 42 days of age reared under cyclic heat stress and its effects on growth performance, cloacal temperatures, mortality rate, blood parameters, and insulin-like growth factor 1 (IGF-1) and growth hormone receptor (GHR) gene expression in the breast muscle. A total of 1000 male Cobb 500® broiler chicks were randomly assigned to five treatments: 0, 0.15, 0.23, 0.47, and 1.30 mg/kg of Zn-L-SeMet. Each treatment consisted of 10 replicates with 20 birds each. No statistically significant differences in growth performance were observed from 1 to 21 days of age (P > 0.05). However, from 1 to 42 days, feed intake (FI) and feed conversion ratio (FCR) decreased linearly (P < 0.05). Cloacal temperatures showed no significant effects (P > 0.05), while overall mortality rate exhibited a quadratic response (P < 0.05), with the optimal inclusion level predicted to reduce broiler mortality at 0.71 mg/kg. Triglyceride (TRG) levels increased with 0.97 mg/kg (P < 0.05), and gama-glutamil transferase (GGT) levels decreased with the inclusion of 1.19 mg/kg (P < 0.05). No significant effects on IGF-1 and GHR gene expression were found (P > 0.05). In conclusion, the inclusion of 1.30 mg/kg of Zn-L-SeMet in diets of heat-stressed broilers improved growth performance from 1 to 42 days of age. An inclusion of 0.71 mg/kg reduced mortality rate, while 0.97 mg and 1.19 mg increased and reduced TRG and GGT levels, respectively.

Zeolite and corn with different compositions in broiler chickens feeding.

The objective of this work was to evaluate the behavior of zeolite against different types of corn in broiler chickens' diets. 1,200 male broiler chickens were assigned to 6 diets in a completely randomized design and a 2 × 3 factorial arrangement, consisting of 2 types of corn (higher or lower mycotoxin contamination) and the inclusion of zeolite (0; 5,000 and 10,000 g ton-1). In the period from d 1 to 21, there was an interaction (P = 0.0040) between types of corn and the inclusion of zeolite for feed conversion ratio (FCR). In the phase from 1 to 42 d, there was an interaction (P = 0.0322) on the serum levels of creatinine (CREA) and digestible gross energy (dGE); corn with lower mycotoxin level contamination (LMLC), caused a reduction in body weight gain (BWG) (P = 0.0046) and increase in the relative weight of abdominal fat (P = 0.0256). Inclusion rates of zeolite promoted an increase in the digestible CP (P = 0.0477) and digestible ash (P < 0.0001), as well as an increase (P < 0.0001) in hot carcass yield (P = 0.0433). The results indicate that the inclusion of zeolite, in the amounts used, did not alter the performance, serum levels, intestinal development and litter quality of the birds at 42 d of age. However, it was responsible for the improvement in the percentage of digestible nutrients (CP, GE, and MM).

Toxicological assessment of a bioactive extract from Triplaris gardneriana Wedd. seeds using alternative models.

The Triplaris gardneriana Wedd. seeds extract has great therapeutic potential due to numerous biological activities such as antioxidant, antibacterial and anti-inflammatory, which are associated with phenolic content. Although this herbal preparation has shown many benefits, recently their toxicity profile has begun to be explored. In this present study, the toxic effects of T. gardneriana seeds ethanolic extract (EETg) on biological systems of different taxonomical groups and levels of complexity (from cell culture to lower vertebrates) were assessed, through a variety of viability and toxicological assays. It was found that EETg did not impair the Saccharomyces cerevisiae growth at the highest tested concentration (200 µg/mL), and no toxicant evidence was observed in Aedes aegypti larvae or in Drosophila melanogaster adult stage. Contrarily, the extract reduced the viability of undifferentiated Caco-2 cells (250 µg/mL, 40% of viable cells), but did not affect differentiated ones. The embryotoxicity in Danio rerio model showed a LC50 of 7.41 mg/L (95% confidence interval, 4.78 - 11.49 mg/L). EETg did not show signs of toxicity in the majority of the models used, but lethality and malformations in zebrafish embryos occurred. Further analyses are needed to better understand the selective toxicity mechanism of EETg on zebrafish, as well as whether the toxic effects happen in higher vertebrates.

Effects of vitamin A on carcass and meat quality of broilers.

This study evaluated the level and length of time of vitamin A supplementation and its effects on carcass and cuts yield, meat quality, and myopathies in 42-day-old broilers. A total of 1,920 birds were divided into 6 groups, and each group received a different level of vitamin A: 0; 6,000; 16,000; 26,000; 36,000 and 46,000 IU/ kg. From d 1 to 21, the treatments were distributed among 16 replicates with 20 birds. From the 22nd d on, 8 repetitions remained with the initial treatment and the others received diets with no vitamin A supplementation. Twelve birds were slaughtered per treatment to evaluate carcass and cuts yield, shear force, cooking loss, water holding capacity, and the presence of substances reactive to thiobarbituric acid. The remaining birds were slaughtered and evaluated in loco for Wooden Breast (WB) and White Striping (WS). Wings weight was affected by vitamin A levels. The duration of the vitamin A supplementation process had effects on the weight of breast, legs with a dorsal portion, and meat color in the yellow intensity (b*). Incidence of WB had higher scores in birds supplemented until 42 d of age. WS showed a quadratic response and a lower response with supplementation of 29,700 IU/ kg. Even for WS, a higher occurrence of the normal score was found in birds supplemented until 21 d of age. Minimal quadratic responses were obtained for normal, moderate, and severe scores, in supplementations of 29,301; 29,959, and 29,827 IU/ kg, respectively. WB had lower occurrence rates in birds supplemented until 21 d of age. Consequently, the severe score was more frequent when supplementation was provided until 42 d of age. The level of vitamin A and the length of time during which this supplementation was provided had influence on cuts yield, meat color and the incidence of WB and WS of the 42-day-old birds.

Different enzymatic associations in diets of broiler chickens formulated with corn dried at various temperatures.

The effect of supplementation of different enzymatic associations in the feed of broiler chickens formulated with corn dried at 80°C or 110°C on growth performance and carcass yield was evaluated. In addition, the influence of the different enzymatic associations on the cecal microbiota was studied. One-day-old male broiler chicks (1,320) were distributed in a completely randomized design in a 2 × 5 factorial arrangement (6 replicates; 22 birds/replicate). The treatments were 2 corn drying temperatures (80°C and 110°C) and 5 diets. The diets consisted of a positive control (PC), a negative control (NC) with a reduction of 100 kcal/kg of apparent metabolizable energy, and 3 enzyme combinations added to the NC diet: amylase, amylase + xylanase, and amylase + xylanase + protease. The feed conversion ratio (FCR) from 1 to 7 d of chickens fed diets formulated with corn dried at 80°C was better (P = 0.045) than that of chickens fed diets dried at 110°C. Regardless of the enzymatic association, the supplementation improved body weight gain (P = 0.01) of the NC group to the same level as the PC group. The FCR of the NC was similar to that of the PC only when the 3 enzymes were included from 1 to 21 d (P = 0.001) and regardless of the enzymatic association for the period from 1 to 42 d (P = 0.007). Regarding cecal microbiota, the alpha diversity was similar among the groups (P > 0.05). The beta-diversity analysis showed that the microbiota of the birds receiving the combination of the 3 enzymes was similar to that of birds fed the PC diet (P = 0.18; R = 0.074), with a similar effect observed for the predicted metabolic functions (Linear discriminant analysis effect size). In conclusion, chickens fed diets formulated with corn dried at 80°C had better FCR during the prestarter phase. The enzymatic supplementation improved the FCR of the birds, which may partially be explained by the modulation of the cecal microbiota.

Carcass characteristics and meat quality of slow-growing broilers fed diets containing dry residue of cassava, with or without the addition of carbohydrases.

This study evaluated the carcass and portion yield and meat quality of slow-growing broilers fed diets with increasing levels of dry residue of cassava (DRC), with or without the addition of carbohydrases. A total of 1100 Label Rouge male broilers were distributed in a completely randomized 2 × 5 factorial design (with or without the addition of carbohydrases and five levels of DRC [0, 2.5, 5.0, 7.5, and 10.0%]), with five replicates and 22 birds per experimental unit. No interaction (P > 0.05) was observed between enzyme addition and DRC levels for the carcass yield, portion yield (back, legs, wings, breast), or abdominal fat variables. There was an interaction (P < 0.05) between the addition of enzyme and DRC on breast pH 15 min post-mortem and the a* intensity of the breast in a colorimetry test. There was a quadratic effect on b* intensity independent of adding enzymes, with the lowest intensity predicted at 8.89% DRC. Regarding feet color, increasing DRC supplementation (independent of enzyme supplementation) led to an increase and decrease in L* and b* intensity, respectively (P < 0.05). Moreover, there was a quadratic effect on a* intensity, with a lower level of intensity predicted at 6.93% DRC (P < 0.05), regardless of the inclusion of enzymes. The inclusion of up to 10% dry residue of cassava in slow-growing broiler diets does not affect carcass and portion yield or the qualitative characteristics of the meat but does reduce the color of the breast meat and feet.

Metabolic aspects of phenolic compounds from Triplaris gardneriana seeds in the management of oxidative stress.

Objective: Considering the limited number of studies that analyze the behavior of plant preparations in human body, this study aimed to characterize the phenolic compounds from Triplaris gardneriana extract (EETg) in terms of antioxidant and metabolic aspects, integrating in vitro, in silico and in vivo strategies.Methods: EETg was analyzed in relation to polyphenols release from the plant matrix under in vitro digestion, as well as the pharmacokinetic prediction of their major compounds by in silico simulation and understanding of its in vivo antioxidant effect in an alternative animal model.Results: About 35.22% of polyphenols from EETg proved to be accessible after enzymatic hydrolysis. A kinetics study showed that 40% of the total content of these phytochemicals was released from the extract accompanied by increased antioxidant capacity after 180 min of gastrointestinal simulation. A computational approach revealed that 7 out of 9 major phenolic compounds of EETg showed good pharmacokinetic parameters such as intestinal absorption and bioavailability score. In addition, the extract showed a protective effect on copper-induced oxidative stress in Drosophila melanogaster, evidenced by the restoration of basal levels of thiol and malondialdehyde contents. These biochemical observations were supported by the examination of histological features of D. melanogaster brain.Conclusion: It was demonstrated that the oral administration of EETg would provide phenolic compounds partially absorbable by the human gut and capable of providing health benefits associated with the inhibition of oxidative stress. Additionally, the results highlight the need to implement new approaches for the rational development of plant-based medicines.

Versatile chromatographic method for catechin determination in development of topical formulations containing natural extracts.

Catechin is found in several natural sources, as Eugenia dysenterica and Syzygium cumini extracts. Its antioxidant and UV-protective properties suggest a potential use in cosmetic and dermatological formulations. A simple analytical method capable of giving support to experiments performed along the development of topical formulations containing this natural substance (i.e. drug assay, skin permeation and stability studies), however, is still needed. Thus, this work aimed to develop and validate a selective HPLC method for catechin determination during the development of topical formulations. Separation was achieved using an RP-C18 column (300 × 3.9 mm; 10 µm), with a mobile phase of methanol-phosphoric acid 0.01 m (15: 85, v/v), a flow rate of 0.8 mL/min, temperature set at 40°C and UV detection at 230 nm. The method was linear in a range from 0.5 to 10.0 µg/mL (r = 0.9998), precise with an overall variation coefficient of 5.5% and accurate with catechin recovery from the skin layers >85%. Additionally, the method was sensitive (limit of detection, 0.109 µg/mL; limit of quantification, 0.342 µg/mL) and selective against plant extracts, skin matrices and formulation interferents, as well as catechin degradation products. It was also robust regarding both methodology parameters and analytical stability.

Supplementation of pig diets in the growth and termination phases with different calcium sources.

The aim of this study was to evaluate the effect of supplementation of pig diets in the growth and termination phases with different calcium sources. In experiment I, 36 whole males were distributed in randomized blocks in six groups, with six replications. A basal diet was formulated to meet the animals' nutritional requirements except for calcium (0.09%), and the sources evaluated (calcitic limestone, monodicalcium phosphate, calcinated bone flour, and oyster flour) replaced the basal diet to provide 0.59% of total calcium. To determine the endogenous calcium, a diet containing low calcium (0.019%) was given simultaneously to another group of animals. Feces and urine were collected for determination the coefficients of apparent and true digestibility. In experiment II, 160 piglets were distributed in randomized blocks in four treatments, with five replications and four animals per experimental unit. Carcass and performance parameters, calcium concentration in bone and serum, and bone parameters were evaluated. The data were submitted to analysis of variance and factorial. The calcium source did not influence the digestibility coefficients determined by total collection (P > 0.05). The digestibility of Ca from oyster flour estimated by collection with an indicator was higher than that from the other sources (P < 0.05). Calcium sources did not interfere in the evaluated parameters (P > 0.05). The sources studied in this work can be used to supplement growing pigs' diets.

Solid lipid nanoparticles improve octyl gallate antimetastatic activity and ameliorate its renal and hepatic toxic effects.

Metastasis is the main cause of cancer-related death and requires the development of effective treatments with reduced toxicity and effective anticancer activity. Gallic acid derivatives have shown significant biological properties including antitumoral activity as shown in a previous study with octyl gallate (G8) in vitro. Thus, the aim of this work was to evaluate the antimetastatic effect of free and solid lipid nanoparticle-loaded G8 in mice in a lung metastasis model. Animals inoculated with melanoma cells presented metastasis in lungs, which was significantly inhibited by treatment with G8 and solid lipid nanoparticle-loaded G8, named G8-NVM. However, G8-treated mice showed an increase in several toxicological parameters, which were almost completely circumvented by G8-NVM treatment. This study supports the need for pharmacological studies on new potential medicinal plants to treat cancer and can provide new perspectives on using nanotechnology to improve biological activities while decreasing the chemotherapy toxicological effects of anticancer drugs.

Identification of Predominant Phytochemical Compounds and Cytotoxic Activity of Wild Olive Leaves (Olea europaea L. ssp. sylvestris) Harvested in South Portugal.

This study has been aimed at providing a qualitative and quantitative evaluation of selected phytochemicals such as phenolic acids, flavonoids, oleuropein, fatty acids profile, and volatile oil compounds, present in wild olive leaves harvested in Portugal, as well as at determining their antioxidant and cytotoxic potential against human melanoma HTB-140 and WM793, prostate cancer DU-145 and PC-3, hepatocellular carcinoma Hep G2 cell lines, as well as normal human skin fibroblasts BJ and prostate epithelial cells PNT2. Gallic, protocatechuic, p-hydroxybenzoic, vanillic acids, apigenin 7-O-glucoside, luteolin 7-O-glucoside, and rutin were identified in olive leaves. The amount of oleuropein was equal to 22.64 g/kg dry weight. (E)-Anethole (32.35%), fenchone (11.89%), and (Z)-3-nonen-1-ol (8%) were found to be the main constituents of the oil volatile fraction, whereas palmitic, oleic, and alpha-linolenic acid were determined to be dominating fatty acids. Olive leaves methanol extract was observed to exerted a significant, selective cytotoxic effect on DU-145 and PC-3 cell lines. Except the essential oil composition, evaluated wild olive leaves, with regard to their quantitative and qualitative composition, do not substantially differ from the leaves of other cultivars grown for industrial purposes and they reveal considerable antioxidant and cytotoxic properties. Thus, the wild species may prove to be suitable for use in traditional medicine as cancer chemoprevention.

Antibacterial, antioxidant and anti-proliferative properties and zinc content of five south Portugal herbs.

CONTEXT: Crataegus monogyna L. (Rosaceae) (CM), Equisetum telmateia L. (Equisataceae) (ET), Geranium purpureum Vil. (Geraniaceae) (GP), Mentha suaveolens Ehrh. (Lamiaceae) (MS), and Lavandula stoechas L. spp. luisieri (Lamiaceae) (LS) are all medicinal. OBJECTIVE: To evaluate the antioxidant, antiproliferative and antimicrobial activities of plant extracts and quantify individual phenolics and zinc. MATERIAL AND METHODS: Aerial part extracts were prepared with water (W), ethanol (E) and an 80% mixture (80EW). Antioxidant activity was measured with TAA, FRAP and RP methods. Phenolics were quantified with a HPLC. Zinc was quantified using voltammetry. Antibacterial activity (after 48 h) was tested using Enterococcus faecalis, Bacillus cereus, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Listeria monocytogenes. Antiproliferative activity (after 24 h) was tested using HEP G2 cells and fibroblasts. RESULTS: Solvents influenced results; the best were E and 80EW. GP had the highest antioxidant activity (TAA and FRAP of 536.90 mg AAE/g dw and 783.48 mg TE/g dw, respectively). CM had the highest zinc concentration (37.21 mg/kg) and phenolic variety, with neochlorogenic acid as the most abundant (92.91 mg/100 g dw). LS was rich in rosmarinic acid (301.71 mg/100 g dw). GP and LS inhibited the most microorganisms: B. cereus, E. coli and S. aureus. GP also inhibited E. faecalis. CM had the lowest MIC: 5830 µg/mL. The antibacterial activity is explained by the phenolics present. LS and CM showed the most significant anti-proliferative activity, which is explained by their zinc content. CONCLUSION: The most promising plants for further studies are CM, LS and GP.

O judô no programa governamental bolsa-atleta: a distribuição espacial dos bolsistas (2011-2013) / Judo in the "Bolsa-Atleta" governmental program: the spatial distribution of the beneficiaries (2011-2013) / El judo en el programa gubernamental "Bolsa-Atleta": la distribución espacial de los becarios (2011-2013)

O presente artigo tem por objetivo identificar como se deu a distribuição espacial dos atletas do Judô dentro do Programa Bolsa-Atleta entre os anos de 2011-2013. Para tanto, foram utilizados os dados fornecidos pelo Ministério do Esporte, que disponibilizou informações sobre os atletas contemplados com o benefício durante o recorte temporal do estudo, e também do sistema da Confederação Brasileira de Judô. Mediante a análise realizada, podemos concluir que os atletas tendem a se manter nas regiões mais desenvolvidas do país, estando concentrados nas regiões Sul e Sudeste, seguidas pelo Nordeste, Centro-Oeste e, por último, a região Norte.

This paper aims to identify how was the spatial distribution of Judo athletes within the "Bolsa-Atleta" Program between the years 2011-2013. To achieve the goal, we used the data given by the Ministry of Sport, which provided information on athletes awarded with the benefit during the time frame of the study, and also those data obtained through the Brazilian Judo Confederation system. Through the analysis, we can conclude that athletes tend to remain in the most developed regions of the country, being concentrated in the South and Southeast, followed by the Northeast, Midwest and finally, the Northern region.

El presente artículo tiene por objetivo identificar cómo era la distribución espacial de los deportistas del Judo dentro del Programa "Bolsa-Atleta" entre los años 2011-2013. Para lograr el objetivo, fueron utilizados los datos proporcionados por el Ministerio del Deporte, que proveyó informaciones sobre los deportistas que tuvieron el beneficio durante el recorte temporal del estudio, así como aquellos datos obtenidos a través del sistema de la Confederación Brasileña de Judo. Tras el análisis realizado, podemos concluir que los deportistas tienden a permanecer en las regiones más desarrolladas del país, concentrándose en las regiones Sur y Sudeste, seguidas por Nordeste, Centro-Oeste y, finalmente, la región Norte.

Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.

Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 2(2) full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant - soybean lecithin or sorbitan monooleate and type of co-surfactants - polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin. In order to evaluate the stability of the systems, the antileishmanial assay was performed against Leishmania amazonensis 24 hours and 60 days after the preparation of the nanoemulsions. The formulation composed of soybean lecithin and polysorbate 20 presented suitable physicochemical characteristics (droplet size 171.9 nm; polydispersity index 0.14; zeta potential -39.43 mV; pH 5.16; and viscosity 2.00 cP), drug content (91.09%) and the highest retention in dermis (3.03 µg·g(-1)) - the main response of interest - confirmed by confocal microscopy. This formulation also presented better stability of leishmanicidal activity in vitro against L. amazonensis amastigote forms (half maximal inhibitory concentration value 0.32±0.05 µM), which confirmed the potential of the nanoemulsion soybean lecithin and polysorbate 20 for CL treatment.

A Clinical Trial with Brazilian Arnica (Solidago chilensis Meyen) Glycolic Extract in the Treatment of Tendonitis of Flexor and Extensor Tendons of Wrist and Hand.

One of the Brazilian arnicas, Solidago chilensis Meyen, is a species of the Asteraceae family. This plant is known by this common name because it shares remarkably similar organoleptic properties with the genus Arnica L., also within the family Asteraceae. We examined the effectiveness of the S. chilensis fluid extract used externally for treating tendinitis of flexor and extensor tendons of wrist and hand in placebo-controlled double-blind clinical pharmacological studies. This study was approved by the Ethical Committee for Scientific Research in Human Beings at University Vila Velha-UVV. Two daily skin applications on the arm skin of a gel cream containing a 5% glycolic plant extract were administered to eight volunteers for 21 days. Among the volunteers, one of their arms was used as the placebo group, and the other one was used as a test group. Statistical data analyses demonstrated a significant reduction in the perception of pain in the arms in the test group, when it was compared to those receiving only the placebo.

Induction of apoptosis and cell cycle arrest in L-1210 murine lymphoblastic leukaemia cells by (2E)-3-(2-naphthyl)-1-(3'-methoxy-4'-hydroxy-phenyl)-2-propen-1-one.

OBJECTIVES: New compounds with biological targets and less cytotoxicity to normal cells are necessary for cancer therapy. In this work ten synthetic chalcones derived from 2-naphtaldehyde were evaluated for their cytotoxic effect in murine acute lymphoblastic leukemia cells L-1210. METHODS: A series of ten chalcones derived from 2-naphtaldehyde and corresponding acetophenones were prepared by aldolic condensation, using methanol as solvent under basic conditions, at room temperature for 24 h. The cell viability was determined by MTT colorimeter method. The cell cycle phase analysis was carried out by flow cytometry after propidium iodide staining. The apoptosis induction was assessed by exposure to phosphatidylserine (ANNEXIN V-FITC). Cytometric analysis was performed to evaluate the expression of p53, Bcl-2 and Bax protein. The caspase-3 expression was studied by immunoblotting analysis. KEY FINDINGS: A preliminary screening of a series of ten chalcones derived from 2-naphtaldehyde showed that chalcone 8, (2E)-3-(2-naphtyl)-1-(3'-methoxy-4'-hydroxy-phenyl)-2-propen-1-one, had the highest cytotoxic effect (IC50 of 54 microM), but not in normal human lymphocytes. To better understand the cytotoxic mechanism of chalcone 8, its effect on cell cycle and apoptosis was assessed. Our results showed that chalcone 8 caused cell cycle arrest in the G2/M phase and a significant increase in the proportion of cells in the subG0/G1 phase. Our results also demonstrated that chalcone 8 promoted a modification in Bax:Bcl-2 ratio and increased p53 expression and caspase-3 activation. CONCLUSIONS: The studied chalcone 8 has cytotoxic effect against L-1210 lymphoblastic leukaemic cells, and this effect is associated with increase of p-53 and Bax expression.