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Viscum album L., popularly known as mistletoe, is well known for its anti-cancer properties, and the pharmaceutical application of hydroalcoholic dry extracts is still limited due to its low solubility in aqueous media, and physicochemical instability. The Pluronic® F127 is an amphiphilic polymer, which permits the solubilization of lipophilic and hydrophilic compounds. In this investigation, physicochemical features of hydrogel containing V. album dry extract (VADE-loaded-hydrogel) were performed by: dynamic light scattering (DLS), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and transmission electron microscopy (TEM). VADE-loaded-hydrogel presented nanometer-size micelles with volume distribution ranging from 10.58 nm to 246.7 nm, and a polydispersity index of 0.441. The sample thermal analyses (TG and DSC) showed similar decomposition curves; however, the thermal events indicated an increase in thermal stability in relation to the presence of the extract. In addition to these interesting pharmaceutical features, IC50 values of 333.40 µg/mL and >1000 µg/mL were obtained when tumor (SCC-25) and non-tumor (L929) cells were incubated with VADE-loaded-hydrogel, respectively. The optical and ultrastructural cellular analysis confirmed the tumor selectivity since the following alterations were detected only in SCC-25 cells: disorganization of plasmatic membrane; an increase of cytoplasmatic vacuole size; alteration in the cristae mitochondrial shape; and generation of amorphous cellular material. These results emphasize the promising antitumoral potential of VADE-loaded-hydrogel as an herbal drug delivery system via in vitro assays.

RESUMO

BACKGROUND: Recent experimental results supporting the dynamization process show modification in the characteristics of solid mixtures. OBJECTIVE: The present work aims to evaluate the physicochemical properties of metallic zinc and lactose, evidencing the interactions between all chemical components presented in dynamized solid mixtures by analytical techniques. METHODS: Mixtures of zinc and lactose (1:9 w/w) were successively triturated at the same proportion according to the Brazilian Homeopathic Pharmacopoeia, receiving the designation of 10-1 - 10-6 (1dH - 6dH). All samples were submitted to the following characterization techniques: Atomic Absorption Spectrometry (AAS), Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD), Differential Scanning Calorimetry (DSC), Thermogravimetry (TG), and Raman Spectroscopy (RS). RESULTS: AAS results detected 97.0% of zinc in the raw material, and the triturated zinc lactose system (ZnMet) presented mean values similar to those expected for the physical mixtures: i.e., 9.94%, 1.23%, and 0.11% in the three first proportions (10-1, 10-2, 10-3), respectively. SEM images showed particle size reduction due to the trituration process. The XRD assays of ZnMet 10-3 and 10-6 indicated peak changes at 12.3° and 43.26°, probably associated with modifications of inter-atomic crystalline spacing. The thermal analysis results of dynamized samples suggest modifications in the chemical interaction between zinc and lactose induced by the physical forces applied. RS experiments showed variation in vibration frequencies due to the dynamization procedure, in which marked ZnMet 10-6 spectral modifications were detected at 357, 477, 1086 and 1142 cm-1, and in the wavelength range 860-920 cm-1. CONCLUSION: These results highlight the importance of applying suitable characterization methods to improve our understanding of the properties of homeopathic solid mixtures, whereas the uses of sensitive tools evidence the influence of trituration on the crystalline properties and in the enthalpy variation of dynamized samples.

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Leishmaniasis is caused by protozoan parasites belonging to the genus Leishmania and includes cutaneous, mucocutaneous and visceral clinical forms. Drugs currently available for leishmaniasis treatment present high toxicity, and development of parasite resistance. Plants constitute an important source of compounds with leishmanicidal potential. This study aimed to evaluate the anti-Leishmania amazonensis activity of the terpenoid fraction of Eugenia pruniformis leaves (TF-EpL). TF-EpL was active against the promastigote and intracellular amastigote forms of L. amazonensis with IC50(24h) value of 43.60µg/mL and 44.77µg/mL, respectively. TF-EpL altered the cell cycle of the parasite, increasing 2.32-fold the cells in the Sub-G0/G1 phase. TF-EpL also changed the ΔΨm and increased ROS and the number of annexin-V-PI positive promastigotes, which suggests incidental death. ß-sitosterol, ursolic acid, corosolic acid and asiatic acid were isolated from TF-EpL. The results showed the antileishmanial activity of E. pruniformis terpenoids and its potential for further studies as a source of new drugs for leishmaniasis.

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ABSTRACT Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.

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Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.

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As alterações na visão que ocorrem no recém-nascido pré-termo se dão pela imaturidade do sistema nervoso central, sendo que a visão permite a ação motora, através da experimentação. O principal objetivo da pesquisa foi promover uma melhor acuidade visual em recém-nascidos pré-termos (RNPT). Trata-se de um ensaio clínico realizado na Unidade de Terapia Intensiva Neonatal do Conjunto Hospitalar do Mandaqui. A estimulação foi realizada inicialmente com uma lanterna e cartões. O estímulo foi aplicado numa distância inicial de 20 cm, assim, foi verificada a resposta visual ou uma resposta motora. Para análise dos dados foram utilizados os critérios de média e cálculos de probabilidade. A população estudada foi composta de 4 RNPTs, com idade gestacional média de 29 semanas, peso ao nascer de 1010g, sendo 2 (50%) do sexo masculino. Em relação às doenças, 4 (100%) apresentavam síndrome do desconforto respiratório, 2 (50%) displasia broncopulmonar, 1 (25%) broncopneumonia, 3 (75%) apnéia da prematuridade, 2 (50%) hipertensão intra-craniana e 1 (25%) atelectasia, tempo médio de ventilação mecânica 52,75 dias e oxigenioterapia 17,66 dias. Com os dados iniciais pode ser relatado que ao decorrer de três dias de estimulação visual ocorreu uma melhora na movimentação, lateralização e fixação do objeto, influenciando o desenvolvimento infantil e ressaltando a importância do aumento da amostra para continuação do estudo.

The alterations in vision which occurred in the premature newborn has the origin of the immaturity of the central nervous system, the vision allows the motor action, through the experimentation. The main objective of the research was to promote a better visual acuity in premature newborn. This is about a clinical trial executed in theNeonatal Intensive Therapy Unity in Conjunto Hospitalar Mandaqui. The stimulation was done initially with lantern and cards. The stimulus was applied with initial distance of 20 cm, then, it was verified a visual or a motor response. For this data analysis, it was used the average criteria and probability calculations. The population analyzed was compound of 4 premature newborn, with gestational age around 29 weeks, birth weight of 1010g, with 2 (50%) of the sex male. Regarding to the illness, 4 (100%) had respiratory distress syndrome, 2 (50%) bronchopulmonary dysplasia, 1 (25%) broncopneumonia, 3 (75%) apnea of prematurity, 2 (50%) hipertensão intra-craniana and 1 (25%) atelectasias, around 52,75 days using the mechanical ventilation and around 17,66 days using oxygentherapy. With the initial information it can be related that during three days of the visual stimulation, it has occurred an evolution in the movement, lateralization and fixation of the object, influencing the infant development and emphasizing the importance of the sample’s increase to continuation of the study.

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Bioassays against fifth-instar nymphae of Rhodnius prolixus were conducted with essential oil of Pilocarpus spicatus extracted by hydrodistillation. The main results may be summarized as follows: (i) high levels of toxicity and paralysis together with discrete moulting inhibition were caused by topical application of either 0.5 µL or 1.0 µL per insect of the crude essential oil; (ii) partial fagoinhibition, high moulting inhibition, prolonged intermoulting period and high number of paralyzed insects, but no toxicity were observed after oral treatment using either 5 µL or 10 µL of Pilocarpus spilcatus essential oil per mL of ingested blood meal. The importance of these results in relation to the relevant biological events in R. prolixus is herein discussed.

Bioensaios contra ninfas de 5º estádio de Rhodnius prolixus foram conduzidos utilizando-se óleo essencial de Pilocarpus spicatus extraído por hidrodestilação. Os principais resultados podem ser resumidos como se segue: (i) altos níveis de toxicidade e paralisia associados à discreta inibição da muda foram induzidos pela aplicação tópica de 0,5 µL ou 1,0 µL do óleo essencial por inseto; (ii) fagoinibição parcial, altos níveis de inibição da muda, período intermuda prolongado e alto número de insetos paralisados mas ausência de toxicidade foram observados após tratamento oral com 5,0 µL ou 10 µL de óleo essencial de P. spicatus por mL de sangue ingerido. A importância destes resultados em relação a eventos biológicos relevantes em R. prolixus é aqui discutida.

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This work shows the potentiality of As as internal standard to compensate errors from sampling of sparkling drinking water samples in the determination of selenium by graphite furnace atomic absorption spectrometry. The mixture Pd(NO(3))(2)/Mg(NO(3))(2) was used as chemical modifier. All samples and reference solutions were automatically spiked with 500mugl(-1) As and 0.2% (v/v) HNO(3) by the autosampler, eliminating the need for manual dilutions. For 10mul dispensed sample into the graphite tube, a good correlation (r=0.9996) was obtained between the ratio of analyte absorbance by the internal standard absorbance and the analyte concentrations. The relative standard deviations (R.S.D.) of measurements varied from 0.05 to 2% and from 1.9 to 5% (n=12) with and without internal standardization, respectively. The limit of detection (LD) based on integrated absorbance was 3.0mugl(-1) Se. Recoveries in the 94-109% range for Se spiked samples were obtained. Internal standardization (IS) improved the repeatability of measurements and increased the lifetime of the graphite tube in ca. 15%.