Caracterização morfológica, perfil químico, atividade biológica e conservação in situ do gênero Lychnophora Mart. (Asteraceae: Vernonieae: Lychnophorinae), Brasil

Many people who live in the cerrado regions use plant species for therapeutic purposes. However, due to intensive extraction of some species, native botanical populations are at risk of disappearing or suffering a dramatic decrease, such as, for instance, individuals of the Lychnophora genus. This has 24 species distributed into the categories vulnerable, endangered, critically endangered, and possibly extinct. These individuals are known in folk medicine as “arnica” and their leaves and flowers are commonly used as anti-inflammatory, analgesic, and healing agents. The chemical profile of the genus is characterized by the presence of sesquiterpene lactones, sesquiterpenes, diterpenes, triterpenes, flavonoids, steroids, polyacetylenes, and caryophyllene derivatives which also have lignans with analgesic activity. Studies with Lychnophora species show significant results with regard to their biological activities against Leishmania amazonensis, Staphylococcus aureus, and Tripanosoma cruzi. Therefore, this study aimed to perform a survey of the morphology, chemical composition, and biological activity, as well as the use and current conservation status of the Lychnophora genus in Brazil.

Detecção imunoistoquímica de receptores de estrógeno e progesterona no endométrio de vacas Nelore (Bos taurus indicus) durante o anestro pós-parto

Twenty-four postpartum anestrous Nelore purebred cows were used in the study. Anestrous was determined based on the reproductive history which was confirmed in each cow based on plasma progesterone concentration and by transrectal ultrasonography. Endometrial biopsies were collected. The animals were separated into two groups according to maximum follicular diameter- Group 1: follicles <6mm (n=12) and Group 2: follicles >-6mm follicles (n=12). The immunohistochemistry technique was employed to evaluate the presence of estrogen and progesterone receptors in the uterine glandular epithelium and stroma. High counts of positive nuclei and high intensity of immunostain for estrogen and progesterone receptors in the glandular epithelium and stroma were observed in the two groups. However, the immunostain intensity of progesterone receptors in the glandular epithelium was higher in Group 2 compared to Group 1. When glandular epithelium and stroma were compared within each group, the relative number of estrogen receptors in the Group 1 was higher in the glandular epithelium compared to stroma and the immunostain intensity for the progesterone receptor in Group 2 was higher in the glandular epithelium compared to stroma. The results suggest that the mechanisms that control the expression of endomerial receptors in the anestrus are similar to the ones observed during the estrus cycle.

Bioprospecção em espécies de Inga (Fabaceae Mimosoideae)

Pós-graduação em Química - IQ

Caracterização por espectrometria de massas e investigação das atividades anti-inflamatória e gastroprotetora do extrato etanólico e diterpenos clerodânicos de folhas de Casearia sylvestris Swartz

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Caracterização por espectrometria de massas e investigação das atividades anti-inflamatória e gastroprotetora do extrato etanólico e diterpenos clerodânicos de folhas de Casearia sylvestris Swartz

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Avaliação anti-inflamatória e antipeçonhenta das espécies Hancornia speciosa e Mimosa tenuiflora em modelos experimentais de inflamação e envenenamento induzidos por Bothrops jararaca e Tityus serrulatus

Accidents caused by venomous animals represents a significant and serious public health problem in certain regions of Brazil, as well as in other parts of the world by the frequency with which they occur and the mortality they cause. The use of plant extracts as an antidote for poisoning cases is an ancient practice used in many communities that have no access to antivenom. Medicinal plants represent an important source of obtaining bioactive compounds able to assist directly in the treatment of poisoning or indirectly supplementing serum therapy currently used. The aim of this study was to evaluate the effect of extracts, fractions and isolated compounds from M. tenuiflora and H. speciosa in the inflammatory process induced by carrageenan and the venom of B. jararaca and T. serrulatus. The results showed that both M. tenuiflora and H. speciosa were capable of inhibiting cell migration and cytokines levels in peritonitis induced by carrageenin and venom of T. serrulatus. In poisoning by B. jararaca model, mice treated with the plants in studies decreased the leukocyte influx into the peritoneal cavity. Finally the M. tenuiflora and H. speciosa had antiphlogistic activity, reducing edema formation and exerted inhibitory action of leukocyte migration in local inflammation induced by the venom of B. jararaca. Through of Thin Layer Chromatography (TLC) analysis was possible identified the presence of flavonoids ,saponins and/or terpenes in aqueous extract of M. tenuiflora. By High Performance Liquid Chromatography analysis, it was possible to identify the presence of rutin and chlorogenic acid in aqueous extract of H. speciosa. We conclude that the administration of extracts, fractions and isolated compounds of H. speciosa and M. tenuiflora resulted in inhibition of the inflammatory process in different experimental models. This study demonstrates for the first time the effect of M. tenuiflora and H. speciosa in inhibition of the inflammation caused by B. jararaca and T. serrulatus venom.

Avaliação do efeito do extrato hidroalcoólico das folhas de Anacardium occidentale L. em ratos submetidos à colite ulcerativa

Ulcerative colitis is a chronic disease characterized by inflammation in the intestinal mucosa, in most cases affects the colon and rectum. The therapeutic drugs are used as aminosalicylates and glucocorticosteroids, but due to the low response and the various side effects caused by them, reveals the need to search for new sources of useful compounds in the treatment of this disease.The species Anacardium occidentale popularly known as cashew, has been used for centuries in folk medicine in the healing aid of skin and mucosa lesions.Recent studies show its expressive antiulcerogenic effect, what we instigated to assess the effect of the extract of A. occidentaleleaves in rats with acute ulcerative colitis, therefore, 42 rats were used male Wistar, divided into 06 groups, and Negative Control (C) Positive Control (C +), treated with Sulfasalazine (Sz500) and treated with Extract A. occidentale at doses of 50 (Ao50), 100 (Ao100) and 200 mg / kg (Ao200).All groups were submitted to experimental colitis Ulcerative except C-, moreover, C- and C + received saline via gavage for 7 consecutive days while the other groups received their respective treatments.Euthanasia of animals took place on the 8th day in which it was collected intestinal colon sample for later analysis macroscopic, histopathological, morphometric and biochemistry, as well as complementary collection of blood and liver tissue. The extract is rich in saponins and phenolic compounds such as flavonoids (quercetin and kaempferol) and tannins.When the Sz500 groups and 100 showed significant protection to damage to lipids and proteins, among the groups subjected to experimental ulcerative colitis, the animals Ao100 group obtained the lowest score in all parameters analyzed.Treatment with 100 mg / kg of A. occidentale extract seems to have a combination of antiinflammatory, antioxidant, bactericidal and anabolic promoted by the bioactive compounds present in the extract.However, it is necessary to investigate harder treating dose of 100mg / kg to higher doses compared to elucidate more properly the best therapeutic dosage ulcerative colitis.

Prospecção química e avaliação biológica de Banisteriopsis laevifolia (Malpighiaceae)

The Banisteriopsis genus is widespread in traditional medicine. This work aims to contribute with information about the chemical composition and on the evaluation of the biological activity of the essential oil, the ethanol extract of the leaves and partitions of the Banisteriopsis laevifolia. The phytochemical screeningtest of ethanol extract and partitions of leaves indicated the presence of flavonoids, terpenoids, saponins, phenols and steroids compounds. Nitrogenous compounds, characteristic of some species of this family, were not detected. Flavonoids were the predominant metabolite, with the highest concentrations on the partitions ethyl acetate and n-butanol. The antibacterial activity, antifungal and cytotoxicity of the essetial oil, ethanol extract and partitions were assyed by microdilution broth method (MBM), where the minimum inhibitory concentrations (MIC) were calculated. The ethanol extract and partitions did not inhibit growth against to Gram positive bacteria tested, with MIC less than 400 mg L-1. For the Gram negative bacteria tested, the hexane and hydroethanol partitios were more effective against F. nucleatum bacteria (MIC 100 ug mL-1). The ethanol extract showed antifungal activity with MIC of 31.2 mg L-1. Ethyl acetate and n-butanol partitions showed MIC 187.5 mg L-1 and 93.7 mg L-1, respectively, arousing interest for isolation studies. The antioxidant activity was evaluated by the DPPH free radical method. The ethanolic extract, ethyl acetate and n-butanol partitions were active, since they showed EC50 values (4.53 ug mL-1, 4.07 and 8.39 ug mL-1, respectively), values equivalent to the BHT (7.3 mg L-1). The analysis by HPLC-MS/MS of the most active fractions (ethyl acetate and n-butanol) identified phenolic compounds (flavonols and phenolic acids) which exert recognized biological activity. The GC-MS analysis of the essential oils from leaves collected in two periods studied (dry and wet), showed a small variation in the number of compounds. The major classes identified for the oil collected in the dry period were aliphatic alcohols (23,4%), terpenoids (18.7%), sterols (10.4%) and long-chain alkanes (9.2%) compounds. Terpenoids (26.8%) were the major class for the rain season. The major compounds (3Z) -hexenol, phytol and untriacontano are present in the two seasons but in different amounts (19.4%, 9.8% and 7.5% during the dry season, and 17.0 %, 14.9% and 15.3% in the rainy season, respectively). The essential oil from rainy season was not effective against to the oral bacteria Gram positive and Gram negative tested. However, showed significant antifungal activity with MIC 1000 mg L-1 against Candidas. Thus, the promising results with respect to biological assays of ethanolic extract and partitions from B. laevifolia contributed to the chemical and biological knowledge of the species B. laevifolia.

Chemical characterization and evaluation of biological activity of Cynara cardunculus extractable compounds

The Mediterranean species Cynara cardunculus L. is recognized in the traditional medicine, for their hepatoprotective and choleretic effects. Biomass of C. cardunculus L. var. altilis (DC), or cultivated cardoon, may be explored not only for the production of energy and pulp fibers, but also for the extraction of bioactive compounds. The chemical characterization of extractable components, namely terpenic and phenolic compounds, may valorize the cultivated cardoon plantation, due to their antioxidant, antitumoral and antimicrobial activities. In this study, the chemical composition of lipophilic and phenolic fractions of C. cardunculus L. var. altilis (DC), cultivated in the south of Portugal (Baixo Alentejo region) was characterized in detail, intending the integral valorization of its biomass. The biological activity of cultivated cardoon extracts was evaluated in terms of antioxidant, human tumor cell antiproliferative and antibacterial effects. Gas chromatography-mass spectrometry (GC-MS) was used for the chemical analysis of lipophilic compounds. Sixty-five lipophilic compounds were identified, from which 1 sesquiterpene lactone and 4 pentacyclic triterpenes were described, for the first time, as cultivated cardoon components, such as: deacylcynaropicrin, acetates of β- and α-amyrin, lupenyl acetate and ψ-taraxasteryl acetate. Sesquiterpene lactones were the major family of lipophilic components of leaves (≈94.5 g/kg), mostly represented by cynaropicrin (≈87.4 g/kg). Pentacyclic triterpenes were also detected, in considerably high contents, in the remaining parts of cultivated cardoon, especially in the florets (≈27.5 g/kg). Taraxasteryl acetate was the main pentacyclic triterpene (≈8.9 g/kg in florets). High pressure liquid chromatography-mass spectrometry (HPLC-MS) was utilized for the chemical analysis of phenolic compounds. Among the identified 28 phenolic compounds, eriodictyol hexoside was reported for the first time as C. cardunculus L. component, and 6 as cultivated cardoon components, namely 1,4-di-O-caffeoylquinic acid, naringenin 7-O-glucoside, naringenin rutinoside, naringenin, luteolin acetylhexoside and apigenin acetylhexoside. The highest content of the identified phenolic compounds was observed in the florets (≈12.6 g/kg). Stalks outer part contained the highest hydroxycinnamic acids abundance (≈10.3 g/kg), and florets presented the highest flavonoids content (≈10.3 g/kg). The antioxidant activity of phenolic fraction was examined through 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay. Stalks outer part, and receptacles and bracts extracts demonstrated the highest antioxidant effect on DPPH (IC50 of 34.35 μg/mL and 35.25 μg/mL, respectively). (cont.) abstract (cont.) The DPPH scavenging effect was linearly correlated with the total contents of hydroxycinnamic acids (r = -0.990). The in vitro antiproliferative activity of cultivated cardoon lipophilic and phenolic extracts was evaluated on a human tumor cells line of triple-negative breast cancer (MDA-MB-231), one of the most refractory human cancers to conventional therapeutics. After 48 h of exposition, leaves lipophilic extract showed higher inhibitory effect (IC50 = 10.39 μg/mL) than florets lipophilic extract (IC50 = 315.22 μg/mL), upon MDA-MB-231 cellular viability. Pure compound of cynaropicrin, representative of the main compound identified in leaves lipophilic extract, also prevented the cell proliferation of MDA-MB-231 (IC50 = 17.86 μM). MDA-MB-231 cells were much more resistant to the 48 h- treatment with phenolic extracts of stalks outer part (IC50 = 3341.20 μg/mL) and florets (IC50 > 4500 μg/mL), and also with the pure compound of 1,5-di-O-caffeoylquinic acid (IC50 = 1741.69 μM). MDA-MB-231 cells were exposed, for 48 h, to the respective IC50 concentrations of leaves lipophilic extract and pure compound of cynaropicrin, in order to understand their ability in modelling cellular responses, and consequently important potentially signaling pathways for the cellular viability decrease. Leaves lipophilic extract increased the caspase-3 enzymatic activity, contrarily to pure compound of cynaropicrin. Additionally, leaves lipophilic extract and pure compound of cynaropicrin caused G2 cell cycle arrest, possibly by upregulating the p21Waf1/Cip1 and the accumulation of phospho-Tyr15-CDK1 and cyclin B1. The inhibitory effects of leaves lipophilic extract and cynaropicrin pure compound, against the MDA-MB-231 cell proliferation, may also be related to the downregulation of phospho-Ser473-Akt. The antibacterial activity of cultivated cardoon lipophilic and phenolic extracts was assessed, for the first time, on two multidrug-resistant bacteria, such as the Gram-negative Pseudomonas aeruginosa PAO1 and the Gram-positive methicillin-resistant Staphylococcus aureus (MRSA), two of the main bacteria responsible for health care-associated infections. Accordingly, the minimum inhibitory concentrations (MIC) were determined. Lipophilic and phenolic extracts of florets did not have antibacterial activity on P. aeruginosa PAO1 and MRSA (MIC > 2048 μg/mL). Leaves lipophilic extract did not prevent the P. aeruginosa PAO1 growth, but pure compound of cynaropicrin was slightly active (MIC = 2048 μg/mL). Leaves lipophilic extract and pure compound of cynaropicrin blocked MRSA growth (MIC of 1024 and 256 μg/mL, respectively). The scientific knowledge revealed in this thesis, either by the chemical viewpoint, or by the biological viewpoint, contributes for the valorization of C. cardunculus L. var. altilis (DC) biomass. Cultivated cardoon has potential to be exploited as source of bioactive compounds, in conciliation with other valorization pathways, and Portuguese traditional cheeses manufacturing.

Atividade antioxidante e antiproliferativa de extratos de folhas de Plukenetia volubilis L. (EUPHORBIACEAE)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Efecto antiinflamatorio de extractos metanólicos de plantas de Azuay y Loja (Ecuador) a través del modelo de peces cebra

Los peces cebra son utilizados como modelo biológico para screening primario de extractos de plantas con potencial bioactividad, aprovechando sus similitudes: genética, fisiológica y respuesta farmacológica con los mamíferos. En el estudio se empleó este modelo para valorar la actividad antiinflamatoria de 36 extractos metanólicos de plantas medicinales utilizadas en las provincias de Azuay y Loja (Ecuador). Parte del material vegetal fue recolectado con el aporte de una hierbatera de etnia Saraguro. Los extractos fueron preparados por percolación y su toxicidad fue evaluada en peces cebra en concentraciones variables de 400 a 3,125 μg/ml, determinándose la máxima concentración tolerada para cada uno de ´estos. La actividad antiinflamatoria se evaluó a través del ensayo de migración leucocitaria inducida por lipopolisacárido de Sallmonella typhi. Los extractos de: Cestrum aff. peruvianum, Galinsoga parviflora, Galium sp., Oenothera tetraptera, Peperomia aff. galioides , Passiflora ampullaceae y Ambrosia arborescens, correspondientes al 18,92% de los analizados, mostraron un potencial antiinflamatorio comparable con indometacina y dexametasona; siendo el extracto metanólico de Cestrum aff. peruvianum el más relevante a 50 g/ml. El análisis fitoquímico básico de los extractos se realizó por cromatografía de capa fina, evidenciándose la presencia de saponinas y terpenoidoes como compuestos principales en la mayoría de los extractos.

Diseño de un vector no viral basado en nanopartículas lipídicas para el tratamiento de la hepatitis C mediante ARN de interferencia

199 p.

Segunda opinião formativa: como deve ser feito o manejo do uso de corticoide em casos de febre chikungunya?

Os corticosteroides são contraindicados na fase aguda da febre Chikungunya e a medicação padrão para uso oral é a prednisona. Nas fases subaguda e crônica, o uso de corticóides está indicado apenas para os casos com dor articular não responsiva a AINE (Anti-Inflamatórios Não Esteroidais) e analgésicos, em pacientes com dor moderada a intensa, poliarticular e debilitante. Para os casos onde haja evidência de processo inflamatório articular, com dor associada a edema, pode ser iniciado corticosteroide na forma oral.

Odontogeriatria: interações medicamentosas

Este estudo se propôs a identificar os fármacos prescritos na Odontologia geradores de riscos de interações medicamentosas com drogas que estão sendo empregadas para o controle de doenças sistêmicas comuns na senilidade. Foi realizada uma pesquisa bibliográfica na Literatura Latino-Americana e do Caribe em Ciências da Saúde - LILACs, Scientific Electronic Library Online - SCIELO e nos manuais do Ministério da Saúde e da Secretaria Estadual de Saúde associado à identificação das principais drogas usadas em tratamento de doenças comumente associadas à senilidade como a diabetes mellitus, a hipertensão arterial, a depressão, a artrite reumatóide e outras patologias. Várias drogas para controle de doenças sistêmicas predispõem o paciente a risco de interações medicamentosas. Como resultado da pesquisa constatou-se que o uso de antiinflamatórios não esteroidais (AINES) está relacionado à atenuação dos efeitos anti-hipertensivos inibidores de enzima conversora de angiotensina, betabloqueadores e diuréticos; potencialização dos efeitos adversos do Lítio, do efeito antiagregante plaquetário dos anticoagulantes e dos efeitos tóxicos do antimetabólico Metotrexato. O analgésico dipirona quando interage com cloropromazina, antipsicótico, causa aumento das reações adversas. Os antimicrobianos prescritos pelo odontólogo aumentam as concentrações sanguíneas por déficit na excreção renal do Lítio, digoxina, ansiolíticos (midazolan e triazolan), teofilina, anticoagulantes orais e Metotrexato. Novas drogas com novos espectros de ação são comercializadas a cada ano, criando sempre a necessidade de familiarização do profissional com a literatura clínica atual permitindo prevenir respostas iatrogênicas associadas com o uso de várias drogas ao mesmo tempo. Conclui-se que os profissionais odontólogos devem ter o conhecimento dos padrões do uso dos medicamentos e das prescrições para os idosos, visto que este conhecimento constitui uma medida importantíssima para se evitar interações medicamentosas na terapêutica farmacológica proposta.