Constituintes químicos das folhas de Riedeliella graciliflora Harms (Leguminosae)

A new salicylic acid derivative, pentacosanyl salicylate, was isolated from the leaves of the plant toxic to cattle, Riedeliella graciliflora, in addition to a digalactosyldiacylglycerol (DGDG), 1,2-di-O-α-linolenoyl-3-O-α-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl-glycerol, kaempferol-3-O-β-D-glucopyranoside, kaempferol-3-O-α-L-rhamnopyranoside, quercetin-3-O-α-L-rhamnopyranoside, rutin, (+)-catechin and the dimer (+)-catechin-(4β-8)-catechin, glutinol, squalene, β-sitosterol, stigmasterol, phytol, β-carotene, α-tocopherol and ficaprenol-12. Their structures were determined using spectral techniques (MS, IR, and NMR-1D and 2D) and based on literature data

Pregnanos e outros constituintes das raízes de Macrosiphonia petraea (A. St.-Hil.) Kuntze (Apocynaceae)

Macrosiphonia petraea (A. St.-Hil.) Kuntze is a plant popularly known as "velame". Its root infusion is used in the folk medicine of Mato Grosso do Sul, Brazil, for the treatment of inflammatory diseases. Phytochemical investigation of the roots of this species led to the identification of 17 compounds belonging to four different classes: two pregnanes, 12β-hydroxypregna-4,6,16-triene-3,20-dione, neridienone A, and 12β-hydroxypregna-4,6-diene-3,20-dione, cybisterol, one hydroxylated fatty acid, 5-hydroxy-octadeca-6(E)-8(Z)dienoic acid, two lignoids, pinoresinol and 8a-hydroxypinoresinol, ten pentacyclic triterpenoids, and two steroids

Novos constituintes químicos das cascas do caule de Tabebuia heptaphylla

A new triterpene, 3beta,6beta,21beta-trihydroxyolean-12-ene and a new iridoid, 8alpha-methyl-8beta-hydroxy-6beta-(3',4'-dimethoxy)benzoyloxy-1 alpha,3alpha-dimethoxy-octahydro-cyclopenta[c]pyran were isolated from the trunk bark of a specimen of Tabebuia heptaphylla (Bignoniaceae) collected in the "Pantanal" of Mato Grosso do Sul, Brazil. Twelve known compounds were also obtained in this work, comprising four iridoids, 6-O-p-hydroxybenzoylajugol, 6-O-p-methoxybenzoylajugol, 6-O-3",4"-dimethoxybenzoylajugol, 8alpha-methyl-8beta-hydroxy-6beta-(4'-hydroxy)benzoyloxy-1alpha,3 alpha-dimethoxy-octahydro-cyclopenta[c]pyran, a cyclopentene dialdehyde, 2-formyl-5-(3',4'-dimethoxybenzoyloxy)-3-methyl-2-cyclopentene-1-acetaldehyde, a phenylethanoid glycoside, verbascoside and three benzoic acid derivatives, p-hydroxybenzoic, p-methoxybenzoic and 3,4-dimethoxybenzoic acids, in addition to squalene, sitostenone and sitosterol. The antioxidant properties of the isolated compounds were also evaluated in this work

Antitrypanosomal butanolides from Aiouea trinervis

In a search for new antitrypanosomal agents in the Brazilian flora, the ethanol extract of the xylopodium from Aiouea trinervis (Lauraceae) exhibited in vitro activity against the epimastigote forms of Trypanosoma cruzi, the etiological agent of Chagas disease. Bioassay-guided chromatographic fractionation of the ethanol extract afforded three butanolides, isoobtusilactone A (1), epilitsenolide C2 (2), and epilitsenolide C1 (3). Butanolides 1 and 3 were more active against T. cruzi epimastigotes than the reference drug benznidazole (by 8.9-fold and 3.2-fold, respectively), while 2 proved inactive. Compounds 1 and 3 showed low cytotoxicity in mammalian Vero cells (CC50> 156 μmol L-1) and high selectivity index (SI) values for epimastigotes (SI = 56.8 and 28.6, respectively), and 1 was more selective than benznidazole (SI = 46.5). Butanolide 1 at 24 μmol L-1 also led to cell cycle alterations in epimastigote forms, and inhibited the growth of amastigote cells in more than 70 %. In silico ADMET properties of 1 were also analyzed and predicted favorable drug-like characteristics. This butanolide also complied with Lipinski’s rule of five and was not predicted as interference compound (PAINS). This is the first report on the isolation of these bioactive butanolides under the guidance of in vitro trypanocidal activity against T. cruzi

Atividade genotóxica de extratos etanólicos de plantas do gênero Ocotea

Ocotea are commonly used by population as a medicine, however there are few research is on the genotoxic activity of extracts and compounds obtained from plants of this genus. The present study examined the genotoxic potential (mutagenic and recombinogenic) of ethanol extracts obtained from the leaves of Ocotea acutifolia, Ocotea lancifolia and Ocotea minarum from in Mato Grosso do Sul state. Genotoxic activity of the plants was investigated by the Somatic mutation and Recombination Test (SMART) in wing cells of Drosophila melanogaster. Extracts of O. lancifolia and O. minarum showed no genotoxic activity, at the concentrations used. Otherside, the extract of O. acutifolia showed higher genotoxic potential and induced high frequencies of mitotic recombination. This difference in activity seems to be related to the presence of different classes of secondary metabolites and their concentrations in each extract. The pronounced genotoxic potential presented by O. acutifolia showed that, despite the frequent use of plants of the genus Ocotea pharmacological studies of these and other plant species are essential in order to characterize the possible adverse effects.Plantas do gênero Ocotea são comumente utilizadas pela população como medicamento, porém são escassas as pesquisas sobre a atividade genotóxica de extratos e compostos químicos obtidos de plantas desse gênero. No presente trabalho foi avaliado o potencial genotóxico (mutagênico e recombinogênico) de extratos etanólicos obtidos das folhas de Ocotea acutifolia, Ocotea lancifolia e Ocotea minarum, que ocorrem no estado de Mato Grosso do Sul. A atividade genotóxica destas plantas foi investigada por meio do SMART (Somatic Mutation And Recombination Test) em células de asas de Drosophila melanogaster. Nas concentrações testadas os extratos de O. lancifolia e O. minarum não apresentaram atividade genotóxica, por outro lado o extrato de O. acutifolia demonstrou elevado potencial genotóxico e induziu altas frequencias de recombinação mitótica. Esta diferença de atividade parece estar relacionada à concentração e as distintas classes de metabólitos secundários encontradas em cada extrato. O pronunciado potencial genotóxico apresentado por O. acutifolia demonstra que, apesar do uso freqüente de plantas do gênero Ocotea, são imprescindíveis estudos farmacológicos destas e outras espécies de plantas, a fim de caracterizar os possíveis efeitos adversos

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Rationale, study design, and analysis plan of the Alveolar Recruitment for ARDS Trial (ART): Study protocol for a randomized controlled trial

Background: Acute respiratory distress syndrome (ARDS) is associated with high in-hospital mortality. Alveolar recruitment followed by ventilation at optimal titrated PEEP may reduce ventilator-induced lung injury and improve oxygenation in patients with ARDS, but the effects on mortality and other clinical outcomes remain unknown. This article reports the rationale, study design, and analysis plan of the Alveolar Recruitment for ARDS Trial (ART). Methods/Design: ART is a pragmatic, multicenter, randomized (concealed), controlled trial, which aims to determine if maximum stepwise alveolar recruitment associated with PEEP titration is able to increase 28-day survival in patients with ARDS compared to conventional treatment (ARDSNet strategy). We will enroll adult patients with ARDS of less than 72 h duration. The intervention group will receive an alveolar recruitment maneuver, with stepwise increases of PEEP achieving 45 cmH(2)O and peak pressure of 60 cmH2O, followed by ventilation with optimal PEEP titrated according to the static compliance of the respiratory system. In the control group, mechanical ventilation will follow a conventional protocol (ARDSNet). In both groups, we will use controlled volume mode with low tidal volumes (4 to 6 mL/kg of predicted body weight) and targeting plateau pressure <= 30 cmH2O. The primary outcome is 28-day survival, and the secondary outcomes are: length of ICU stay; length of hospital stay; pneumothorax requiring chest tube during first 7 days; barotrauma during first 7 days; mechanical ventilation-free days from days 1 to 28; ICU, in-hospital, and 6-month survival. ART is an event-guided trial planned to last until 520 events (deaths within 28 days) are observed. These events allow detection of a hazard ratio of 0.75, with 90% power and two-tailed type I error of 5%. All analysis will follow the intention-to-treat principle. Discussion: If the ART strategy with maximum recruitment and PEEP titration improves 28-day survival, this will represent a notable advance to the care of ARDS patients. Conversely, if the ART strategy is similar or inferior to the current evidence-based strategy (ARDSNet), this should also change current practice as many institutions routinely employ recruitment maneuvers and set PEEP levels according to some titration method.Hospital do Coracao (HCor) as part of the Program 'Hospitais de Excelencia a Servico do SUS (PROADI-SUS)'Brazilian Ministry of Healt