Caracterização e quantificação de marcadores químicos do extrato hidroetanólico das folhas de Kalanchoe brasiliensis Cambess

Kalanchoe brasiliensis Cambess (Crassulaceae), commonly known as saião , coirama branca , folha grossa , is originally from Brazil and commonly found in São Paulo to Bahia, mainly in the coastal zone. Regarding of biological activities, most preclinical studies were found in the literature, mainly about the anti-inflammatory activity of extracts obtained from leaves and / or aerial parts of K. brasiliensis. As regards the chemical constitution, it has been reported mainly the presence of flavonoids in the leaves of the species, but until this moment did not knows which are the active compounds. Although it is a species widely used in traditional medicine in Brazil, there is no monograph about the quality parameters of the plant drug. In this context, this study aims to characterize and quantify the chemical markers of hydroethanolic extract (HE) from the leaves of K. brasiliensis, which can be used in quality control of plant drug and derivatives obtained from this species. The methodology was divided into two parts: i. Phytochemical study: to fractionate, isolate and characterizate of the chemical (s) marker (s) of the HE from the leaves of K. brasiliensis; ii. To Developed validate of analytical method by High Performance Liquid Chromatography (HPLC)-diode array detector (DAD) to quantify the chemical (s) marker (s) of the EH. i. The EH 50% was prepared by turbo extraction method. It was then submitted to liquid-liquid partition, obtaining dichloromethane, n-butanol and ethyl acetate (AcOEt) fractions. The AcOEt fraction was selected to continue the fractionation process, because it has a chemical profile rich in flavonoids. The acOEt fraction was submitted to column chromatography using different systems for obtaining the compound Kb1. To identify this compound, it was submitted to UV analysis ii. For quantitative analysis, the EH was analyzed by HPLC, using different methods. After selecting the most appropriate method, which showed satisfactory resolution and symmetrical peaks, it was validated according to parameters in the RE 899/2003. As result, it was obtained from the AcOEt fraction the compound Kb1 (2.7 mg). Until this moment, the basic nucleus was characterized by UV analysis using shift reagents. The partial chemical structure of the compound Kb1 was identified as a flavonol, containing hydroxyls in 3 , 4 position (ring A), 5 and 7 free (ring B) and a replacement of the C3 hydroxyl by a sugar. As the analysis were performed in the HPLC coupled to a DAD, we observed that the UV spectrum of the major peaks of EH from K. brasiliensis shown similar UV spectrum. According to the literature, it has been reported the presence of patuletin glycosydes derivatives in the leaves of this species. Therefore, it is suggested that the compound Kb1 is glycosylated patuletin derivative. Probably the sugar (s) unit(s) are linked in the C3 in the C ring. . Regarding the development of HPLC analytical method, the system used consists of phase A: water: formic acid (99,7:0,3, v / v) and phase B: methanol: formic acid (99,7:0,3, v / v), elution gradient of 40% B - 58% B in 50 minutes, ccolumn (Hichrom ®) C18 (250x4, 0 mm, 5 μm), flow rate 0.8 mL / min, UV detection at 370 nm, temperature 25 ° C. In the analysis performed with the co-injection of thecompound Kb1 + HE of K. brasiliensis was observed that it is one of the major compounds with a retention time of 12.47 minutes and had a content of 15.3% in EH of leaves from K. brasiliensis. The method proved to be linear, precise, accurate and reproducible. According to these results, it was observed that compound Kb1 can be used as a chemical marker of EH from leaves of K. brasiliensis, to assist in quality control of drug plant and its derivatives

Caracterização térmica (TG/DTG, DTA, DSC, DSC-fotovisual) de Hormônios bioidênticos (estriol estradiol)

Bioidentical hormones are defined as compounds that have exactly the same chemical and molecular structure as hormones that are produced in the human body. It is believed that the use of hormones may be safer and more effective than the non-bioidentical hormones, because binding to receptors in the organism would be similar to the endogenous hormone. Bioidentical estrogens have been used in menopausal women, as an alternative to traditional hormone replacement therapy. Thermal data of these hormones are scarce in literature. Thermal analysis comprises a group of techniques that allows evaluating the physical-chemistry properties of a drug, while the drug is subjected to a controlled temperature programming. The thermal techniques are used in pharmaceutical studies for characterization of drugs, purity determination, polymorphism identification, compatibility and evaluation of stability. This study aims to characterize the bioidentical hormones estradiol and estriol through thermal techniques TG/DTG, DTA, DSC, DSC-photovisual. By the TG curves analysis was possible to calculated kinetic parameters for the samples. The kinetic data showed that there is good correlation in the different models used. For both estradiol and estriol, was found zero order reaction, which enabled the construction of the vapor pressure curves. Data from DTA and DSC curves of melting point and purity are the same of literature, showed relation with DSC-photovisual results. The analysis DTA curves showed the fusion event had the best linearity for both hormones. In the evaluation of possible degradation products, the analysis of the infrared shows no degradation products in the solid state

Preparação e caracterização de sistemas emulsionados contendo benznidazol

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Obtenção e caracterização de complexos de inclusão binários e ternários com praziquantel

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Extração, caracterização e atividades biológicas de proteínas da espécie cnidoscolus urens (L.) Arthur

The extraction, chemical and structural characterization of a wide variety of compounds derived from plants has been a major source of bioactive molecules. Several proteases have been isolated in the plant kingdom, with numerous pharmacological and biotechnological applications. Among the proteases isolated from plants, are the fibrinogenolytic, with relevant application in the treatment of disorders in the coagulation cascade, in addition to potential use as a tool in clinical laboratories. In this study, in addition to evaluating the effects of the protein extract of Cnidoscolus urens (L.) Arthur (Euphorbiaceae) in the coagulation cascade also investigates the presence of antimicrobial activity and characterizes the proteolytic activity detected in this extract, aiming to determine their potential pharmacological and biotechnological application. In this way, crude protein extracts obtained from the leaves of C. urens in Tris-HCl 0.05M, NaCl 0.15M, pH 7.5, were precipitated in different concentrations of acetone, and assessed for the presence of proteolytic activity in azocaseína and fibrinogen. The most active fraction (F1.0) in these tests was chosen for assessment of biological activity and biochemical characterization. The Aα chain and Bβ of fibrinogen were completely cleaved at a concentration of 0.18 μg/μL of protein fraction in 4 minutes. Fibrinogenolytic activity presented total inhibition in the presence of E-64 and partial in the presence of EDTA. The fraction demonstrated coagulant activity in plasm and reduced the APTT, demonstrating acting on the factors coagulation of the intrinsic pathway and common, not exerting effects on the PT. Fibrinolytic activity on plasma clot was detected only in SDS-PAGE in high concentrations of fraction, and there were no defibrinating. Although several proteases isolated from plants and venomous animals are classically toxic, the fraction F1.0 of C. urens not expressed hemorrhagic nor hemolytic activities. Fraction F1.0 also showed no antimicrobial activity. In proteolytic activity on the azocasein, the optimal pH was 5.0 and optimum temperature of 60ºC. The enzyme activity has been shown to be sensitive to the presence of salts tested, with inhibition for all compounds. The surfactant triton did not influence the enzyme activity, but the tween-20 and SDS inhibited the activity. In the presence of reducing agents increase in enzyme activity occurred, a typical feature of enzymes belonging to the class of cysteine proteases. Several bands with proteolytic activity were detected in zymogram, in the region of high-molecular-weight, which were inhibited by E-64. In this study, we found that C. urens presents in its constitution cysteine proteases with fibrinogenolytic and procoagulant activity, which may be isolated, with potential application in treatment of bleeding disorders, thrombolytic and clinical laboratory

Preparação e caracterização de sistemas emulsionados lipidicos contendo praziquantel

Praziquantel (PRZ) is the main drug used for treatment of schistosomiasis in Brazil. It is administered by oral rout as tablets. However, has low aqueous solubility which limits this therapeutic success dosage form and availability of liquid forms. The emulsion systems have great potential and represent an interesting strategy to increase the solubility of drugs. The aim of study was the development and characterization of lipid-emulsified liquid systems of the type oil in water (O / W), the base of soybean oil as the internal phase stabilized by surfactants pair Tween® 80 and Span® 80, for improving the phase biopharmaceutical of PRZ. After selecting the best value of Hydrophilic-Lipophilic Balance (HLB = 11), the parameters of the preparation of the formulations were optimized emulsification technique. The emulsions were successfully obtained; the liquid forms provided exhibited Newtonian behavior and an increase in solubility of PRZ higher than 20 times. The accelerated stability study demonstrated the stability of the emulsions and the effect of cosurfactants investigated. The study of the dynamics of interaction between components in the diagram showed pseudoternary phase regions to obtain O/W emulsions, whereas the study of the interaction of the components and their effect on system structure and the efficiency of incorporation of the drug led to systems with an amount of soluble drug even higher (about 1.5%), which demonstrates the potential of this new input mainly for the treatment of schistosomiasis, which resulted in the filing of patent BR 10 2013 0004 55 3

Preparação e caracterização de complexos multicomponentes contendo ciclodextrinas com metotrexato

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Caracterização dos marcadores químicos e avaliação de atividades biológicas do extrato de Spondias mombim

Spondias mombin is a fruitful species dispersed in tropical regions of America, Africa and Asia. In Brazil, the species can be found mainly in the northern and northeastern regions. Scarce chemical and pharmacological studies have been reported for S. mombin and until this moment studies about chemical markers were not developed. In this context, the aims of this study were to characterize the chemical markers from S. mombin leaves and evaluate their anti-inflammatory, antioxidant and antiproliferative potentials. The chemical profile of the hydroethanolic extract from S. mombin leaves analyzed by HPLC-DAD, through a validated method, allowed the identification and quantification of ellagic acid and chlorogenic acid. This extract showed anti-inflammatory potential in acute peritonitis model induced by carrageenan. The hydroethanolic extract from S. mombin leaves was subjected to a liquid-liquid partition with the solvents: n-hexane, dichloromethane, ethyl acetate and n-butanol. Regarding the anti-inflammatory potential of the fractions obtained they were active; however, ethyl acetate fraction at 200 mg/kg showed highlighted results. The compounds ellagic acid and chlorogenic acid also inhibited the leukocyte migration to the site of inflammation at 2.5, 5 and 10 mg/kg. The hydroethanolic extract, fractions and the chemical markers showed significant antioxidant potential when evaluated in different assays: DPPH Free-Radical Scavenging, Superoxide Radical Scavenging, Hydroxyl Radicals Scavenging and Reducing Power. Taken together our results showed that hydroethanolic extract of S. mombin leaves has ellagic acid and chlorogenic acid as bioactive markers and it demonstrated antiinflammatory and antioxidant properties besides no cytotoxicity against 3T3 cells. It enables us to suggest S. mombin as an important species to develop herbal drugs

Estrutura econômica, mercado de trabalho e evolução sócio-ocupacional no Rio Grande do Norte 2001 a 2008: reflexo de uma condição mercantil e estruturalmente periférica

The aim of this thesis was to investigate the evolution of the socio-occupational status in Rio Grande do Norte from 2001 to 2008, based on the characterization of the socio-economic status of this State from the analysis of labor market norte-rio-grandense . The study, specifically, drew a comparison between the dynamics of the labor market in Rio Grande do Norte and the capital city, Natal. From this perspective, the purpose was to make a relationship between the social division of labor and its effects on the socio-spatial division, represented in the "macro scale" by the federal unit and the "micro level" for the capital; locus of economic and population concentration. The collection of data on the labor market had as a major source PNAD/IBGE, characterizing the labor market in many ways: people of working age, economically active population and employed and unemployed people, classified by age, sex, color, education, income and social protection condition. However, as for the socio-occupational division, we follow the methodology used by the research group on national television, based in IPPUR /UFRJ, called Monitoring of the Metropolis," which rallied twenty-four groups that aggregate the occupations found in the PNAD/IBGE, in eight groups of socio-occupational categories, according to the similarity between them. It was used in the socio-spatial cutting two relevant discussions, which are inter-related and were characterized as crucial points in developing the research problem: the former was related to the influence of the hegemony of merchant capital in the labor market in Rio Grande North and, the latter, it referred the socio-economic relations between the territory and the variable occupation. Lastly, the results all indicated that in Rio Grande do Norte, as a peripheral state, has suffered the devastating influence of the hegemony of capital purely commercial basis, where "wealth" of capitalism is generated through the sphere of mere movement of goods and services rather than a productive process due to the social relations of production more advanced. We have a little advanced economic structure, with a tertiary sector that has propagated under-employment or disguised unemployment. Similarly, the agricultural sector has been presented as an example of greater social degradation of working conditions in the state. The secondary sector, in turn, also was not behind this uncertainty; on the contrary, confirmed that condition, with poor levels of income, low education of the workforce and a high degree of social helplessness, even in the state capital, space full urban area, which although always appear with a favorable condition compared to Province, in practically most of the variables studied, was also reflected at the same time the author of a structurally underdeveloped condition

Utilização intracoágulo de espuma fibrinolítica - preparação, caracterização e atividade in vitro de uma espuma de estreptoquinase e proposta de uma nova abordagem terapêutica

Foam was developed as a novel vehicle for streptokinase with the purpose of increasing the contact time and area between the fibrinolytic and the target thrombus, which would lead to a greater therapeutic efficacy at lower doses, decreasing the drug s potential to cause bleeding. Fibrinolytic foams were prepared using CO2 and human albumin (at different v:v ratios), as the gas and liquid phases, respectively, and streptokinase at a low total dose (100,000 IU) was used as fibrinolytic agent conveyed in 1 mL of foam and in isotonic saline solution. The foams were characterized as foam stability and apparent viscosity. The thrombolytic effect of the streptokinase foam was determined in vitro as thrombus lysis and the results were compared to those of a fibrinolytic solution (prepared using the same dose of streptokinase) and foam without the fibrinolytic. In vitro tests were conducted using fresh clots were weighed and placed in test tubes kept at 37 ° C. All the samples were injected intrathrombus using a multiperforated catheter. The results showed that both foam stability and apparent viscosity increased with the increase in the CO2:albumin solution ratio and therefore, the ratio of 3:1 was used for the incorporation of streptokinase. The results of thrombus lysis showed that the streptokinase foam presented the highest thrombolytic activity (44.78 ± 9.97%) when compared to those of the streptokinase solution (32.07 ± 3.41%) and the foam without the drug (19.2 ± 7.19%). We conclude that fibrinolytic foam showed statistically significant results regarding the enhancement of the lytic activity of streptokinase compared to the effect of the prepared saline solution, thus it can be a promising alternative in the treatment of thrombosis. However, in vivo studies are needed in order to corroborate the results obtained in vitro

Dispersões sólidas de sinvastatina: preparação, caracterização, no estado sólido utilizando técnicas emergentes e estudo de estabilidade

This thesis aimed to assess the increase in solubility of simvastatin (SINV) with solid dispersions using techniques such as kneading (MA), co-solvent evaporation (ES), melting carrier (FC) and spray dryer (SD). Soluplus (SOL), PEG 6000 (PEG), PVP K-30 (PVP) e sodium lauryl sulphate (LSS) were used as carriers. The solid dispersions containing PEG [PEG-2(SD)], Soluplus [SOL-2(MA)] and sodium lauryl sulphate [LSS-2(ES)] were presented with a greater increase in solubility (5.02, 5.60 and 5.43 times respectively); analyses by ANOVA between the three groups did not present significant difference (p<0.05). In the phase solubility study, the calculation of the Gibbs free energy (ΔG) revealed that the spontaneity of solubilisation of SINV occurred in the order SOL>PEG >PVP 75%>LSS, always 80%. The phase diagrams of PEG and LSS presented solubilization stoichiometry of type 1:1 (type AL). The diagrams with PVP and SOL tend to 1:2 stoichiometry (type AL + AP). The stability coefficients (Ks) of the phase diagrams revealed that the most stable reactions occurred with LSS and PVP. The solid dispersions were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), particle size distribution (PSD), near-infrared spectroscopy imaging (NIR-CI) and X-ray diffraction of the powder using the Topas software (PDRX-TOPAS). The solid dispersion PEG-2(SD) presented the greatest homogeneity and the lowest degree of crystallinity (18.2%). The accelerated stability study revealed that the solid dispersions are less stable than SINV, with PEG-2(SD) being the least stable, confirmed by FTIR and DSC. The analyses by PDRX-TOPAS revealed the amorphous character of the dispersions and the mechanism of increasing solubility

Caracterização do nicho alimentar do polvo octopus insularis (cephalopoda: octopodidae): da população ao indivíduo

Octopus insularis, target species in this study, is the dominant benthic octopus of the North and Northeast Brazil. Studies on behavior and ecology of the species have been conducted primarily on oceanic islands, with little information on the continental populations. In this study, two regions of the coast of RN, Rio do Fogo and Pirangi, were chosen for the characterization of the niche by O. insularis populations. The dietary niche, habitat and distribution of O. insularis of oceanic islands and the mainland, were compared. In addition, individual characteristics of feeding behavior in a population at Atol das Rocas was studied, taking into account the size of individuals, the proximity of the dens and characteristics of their "personality". The diet of the Rio do Fogo population was composed mainly of bivalve molluscs (82%), unlike Pirangi population that has a diet consisting mainly of crustaceans Decapoda (68%), similar to that described for the populations of the islands. Consequently, the feeding niches of the island populations were more similar, with greater overlap, but the niche breadth of the continent was larger. The habitats of occurrence on the coast includes reefs, rocks, gravel and an environment called Restinga, a plateau composed of biogenic gravel, sand, sponges and algae, showed a high density of animals. Similarly to that found in the islands, O. insularis in the continent, had a clumped distribution, and a bathymetric segregation between small and large individuals. The differences in diet composition among populations were explained by differences in habitat and coverage of the substrate, which may be directly influencing the diversity and prey availability in these environments. The individual analyzes of the population at Atol das Rocas, showed no relationship between the degree of individual specialization and the different personalities, or the distance between dens. The results suggest that the foraging strategy with greater availability of prey in the environment has an influence on diet octopuses over preferences or personalities

Caracterização ecofisiológica de sementes de espécies lenhosas da Caatinga

Dormancy is an inherent property of the seeds that define the environmental conditions in which they are able to germinate and their presence is an adaptive trait common in species inhabiting semiarid regions. Moreover, the ability of seedling establishment in these environments has been related to the size, strength and chemical characteristics of the seeds. This study investigated patterns of dormancy and germination speed in tree species of the Caatinga, exploring how the seed size influence the processes of germination, seedling size and biomass allocation. In addition, we aim to investigate the chemical characteristics of the reserves, to verify a possible relationship between nutritional content and the process of seed germination. Therefore, seeds were collected from ten species of woody Caatinga for tests of breaking dormancy, germination and biochemical characterization. Overall, the results show that the scarification treatments mechanical and chemical, and thermal shock influenced the percentage and speed of germination in 50 % of the species, suggesting that they have some level of physical dormancy in the seeds. Biochemical characterization showed the existence of large amounts of carbohydrates in the seeds of all species, low proportion of protein and low amounts of neutral lipids. Using linear regression, we demonstrated the existence of a significant relationship between seed size and the ratio of root/shoot where the largest seeds invested a greater amount of resources for shoot growth. The relationship between germination speed and non-reducing sugar content was also significant, so these compounds is related to the maintenance of physiological seed quality. These results confirm some relationships discussed in the literature for cultivated species, but can be applied to the species native to the Caatinga

Vitrine das letras: o discurso jornalístico e a modernidade pedagógica em Sergipe/Brasil e Portugal - (1910-1920)

Dans cette étude, j'ai eu comme objectif d'établir les connexions et/ou les non-connexions dans les discours journalistiques sur la modernité pédagogique, dans les journaux O Correio de Aracaju (Le Courrier d'Aracaju, Sergipe, Brésil) et O Século (Le Siècle, Portugal), dans la période 1910-1920. J'ai tout particulièrement cherché le dit dans les journaux, dans le sens foucaldien du terme, en continu dialogue avec d'autres auteurs, dans une perspective interdisciplinaire. J'ai tenté de répondre à mon interrogation initiale : quelles sont les connexions et non connexions que l'on pourrait établir entre l'École Moderne du Portugal et celle de Sergipe, au Brésil, en prenant comme source d'analyse les discours journalistiques dans des journaux des deux pays ? Á partir de ce questionnement, à travers un abordage historico-comparatif interculturel, j'ai soutenu la THÈSE que les discours journalistiques du Século et du Correio de Aracaju, bien qu'ils relèvent de genres journalistiques différents quant au niveau de développement de la presse, ont traduit une perception et une assimilation de la modernité pédagogique articulées à une même epistémè. Ainsi, ces discours ont émergé comme objets métis, dont la création s'est faite dans des interlocutions, échanges, impositions et débats dans un processus continu de communication interculturelle. La nature messianique de ces discours, dans le système d'idées républicain, traduisait le sens de la modernité pédagogique prétendue et diffusée par les textes qui exprimaient l'aspiration de rupture et de progrès, tant au Portugal que dans l'état brésilien de Sergipe. Il a également été possible de faire des approximations/comparaisons entre la dispute (article d'opinion), dans le Correio de Aracaju et l'enquête (interview et reportage), dans O Século et de souligner ainsi les connexions et/ou non-connexions présentes sur le thème de la modernité pédagogique dans les discours journalistiques

Ser professor de português: o que dizem os discursos reguladores, os alunos e os professores no contexto da formação inicial (UMINHO/Portugal e UFRN/Brasil)

The constitution of being a teacher of Portuguese occurs in a dynamic process involving various factors, such as the requirements of regulatory documents, the context of teacher formation, and the configuration of current society, per se. This study is aimed at reflecting on the initial formation of teachers of Portuguese and on official documents that face this formation, raising the following questions: (1) what does it mean to be a Portuguese teacher? (2) what is the vision of the subjects (teachers and students) involved with the formation of teaching the Portuguese Language? (3) how do these individuals deal with official documents? and (4) how do these subjects discourses relate? To understand the context of the formative processes and the knowledge inherent in them, first we take the studies of Garcia (1999) and Tardif (2002) as a theoretical framework, and to understand and interpret the utterances of the interviewees, we were grounded in the writing of Bakhtin (2003), for whom the object of the Humanities, the sciences of man, is the text, since man is, by nature, an expressive being. We situate this study in the framework of qualitative research. It is a multiple case study that focuses on two contexts: formation of teachers of Portuguese at the University of Minho, Portugal, and the Federal University of Rio Grande do Norte, Brazil. The data that make up the research corpus come from documents elaborated by the Ministries of Education of Portugal and Brazil and were adopted by the two teacher formation institutions cited, from individual interviews involving eight trainer teachers (four from each university), and from two group-interviews (one in each institution), done with students in training. Our analysis is divided into three stages: first, document analysis; second, analysis of the discourse of the teachers in both contexts studied; and, third, analysis of the speech of the students in training. It is noteworthy that our purpose in this research was not to come out with a definition like being a teacher of Portuguese is X, but we are interested, above all, in discussing the issues surrounding initial formation, seeking different points of view, and hearing voices coming from different social positions for better understanding our object of study. Our analysis reveals that the initial formation of teachers of Portuguese, both in Portugal and Brazil, occurs in a complex way, under the influence of various factors, including: (a) difficulties in having the individuals involved adapt to the demands of regulatory agencies; (b) students and teachers adequacy to the organizational model of the post-secondary institution; (c) teachers difficulties to deal with the learning problems of students who have limited schooling basis and come from distinct socioeconomic realities; (d) a search for the establishment of methodologies for teaching and learning the Portuguese Language more adequate to reality; and (e) a search for a definition of professional knowledge needed for the teaching practice