Achyrocline satureioides (Lam.) D.C. is a herb native to South America, and its inflorescences are popularly employed to treat inflammatory diseases. Here, the effects of the in vivo actions of the hydroalcoholic extract obtained from inflorescences of A. satureioides on neutrophil trafficking into inflamed tissue were investigated. Male Wistar rats were orally treated with A. satureioides extract, and inflammation was induced one hour later by lipopolysaccharide injection into the subcutaneous tissue. The number of leukocytes and the amount of chemotactic mediators were quantified in the inflammatory exudate, and adhesion molecule and toll-like receptor 4 (TLR-4) expressions and phorbol-myristate-acetate- (PMA-) stimulated oxidative burst were quantified in circulating neutrophils. Leukocyte-endothelial interactions were quantified in the mesentery tissue. Enzymes and tissue morphology of the liver and kidney were evaluated. Treatment with A. satureioides extract reduced neutrophil influx and secretion of leukotriene B4 and CINC-1 in the exudates, the number of rolling and adhered leukocytes in the mesentery postcapillary venules, neutrophil L-selectin, β2-integrin and TLR-4 expression, and oxidative burst, but did not cause an alteration in the morphology and activities of liver and kidney. Together, the data show that A. satureioides extract inhibits neutrophil functions related to the innate response and does not cause systemic toxicity.
The aim of the study was to analyze the constituents of the dichloromethane fraction obtained from A. moluccana and also to evaluate the anti-inflammatory and antinociceptive properties of α,β-amyrenone isolated from A. moluccana in mice. The dichloromethane fraction was evaluated by gas chromatography and submitted to purification. The mixture of α,β-amyrenone was isolated and then evaluated using the carrageenan-induced paw-oedema or pleurisy and CFA-induced arthritis models in mice. Five triterpenes, α,β-amyrenone, glutinol, and α,β-amyrin were isolated from dichloromethane fraction of A. moluccana leaf extract. The mixture of α,β-amyrenone, dosed orally, was able to reduce mechanical hypersensitivity and paw-oedema induced by carrageenan, interfering with neutrophil migration. Similar results were observed in the carrageenan-induced pleurisy model. Repeated administration of the compounds was also effective in reducing the mechanical sensitization and oedema developed in the arthritis model induced by CFA. In conclusion, the results demonstrate that α,β-amyrenone interferes in both acute and chronic inflammatory processes. We can infer that these effects involve, at least in part, a reduction in the neutrophil migration. Therefore, it seems reasonable to suggest that α,β-amyrenone could represent a new therapeutic tool for the management of painful and inflammatory diseases, especially those presenting a chronic profile.
This work describes the seasonal variation of curcumenol (1) and dihydrocurdione (2), two active terpenoids from different parts (roots, mother rhizome and rugous rhizome) of Curcuma zedoaria grown in Brazil. The analysis was carried out by high resolution gas chromatography, using external standards for determination. The results showed that both terpenoids are present in all the parts studied. However, C. zedoaria exhibited about three times more terpenoids in the mother rhizome in autumn than in other parts and seasons studied. The antinociceptive activity of the dichloromethane extracts from different parts and collected in different seasons was studied using the acetic acid-induced abdominal constriction model in mice. The extracts obtained from mother rhizome collected in autumn and winter at doses of 10 mg/kg body weight, i.p., caused considerable antinociceptive activity inhibiting 91.1 and 93.4% of the abdominal constrictions, respectively, whereas compounds 1 and 2 caused inhibitions of 64.0 and 46.0%, respectively. These results confirm that both compounds contribute to explain the antinociceptive effect of the plant but suggest that other compounds are also acting as analgesics
A simple and efficient microwave-assisted extraction process has been developed in order to extract plumieride from Allamanda cathartica flowers. The extracts have been obtained through microwave-assisted extraction (MAE) process with ethanol and ethyl acetate at different time, power and temperatures. Static maceration at room temperature with ethanol and ethyl acetate was obtained in order to compare the efficiency of extraction. HPLC method was validated to quantify plumieride in the extracts. The analyzed parameters: linearity (R 2 = 0.999), precision (CV 3.3%), recovery (98%), specificity (97%), limit of detection (1 µg mL -1), and limit of quantification (2 µg mL -1 ) were satisfactory. The yield of plumieride reached 43% in the extracts under the optimal MAE conditions (10 min, 300W). Plumieride recoveries by conventional extraction method were 12% with ethanol and 22% with ethyl acetate. Time and power parameters on plumieride extraction yield was determined by applying a factorial design and surface plots. Ethanol was the best extractor solvent and it was possible to obtain high contents (52 mg g -1 of dry flowers) at optimized conditions. It can be concluded that MAE process has actual advantages over the conventional extraction method in terms of shorter time and higher efficiency to recover plumieride from A. cathartica flowers.
Chromatography Iridoids K562 and Nalm6 cells Plumericin A B S T R A C T The aim of this research was to evaluate the fractions obtained from the leaf, stem and roots of Allamanda schottii, Pohl, Apocynaceae, responsible for the cytotoxicity, using several cell lines. Cytotoxicity was correlated with the season the part of the plant, and the major compounds were assessed. The ethanol extracts of leaves, stems and roots obtained at different seasons were evaluated in the human erythromyeloblastoid leukemia cell line (K562). Subsequently the ethanol extracts and dichloromethane fractions collected in winter were evaluated in mouse fibroblast cell line (Mus musculus) (L929), cervix adenocarcinoma (HeLa), human pre-B leukemia (Nalm6), as well as K562 cell line. The compounds plumericin, plumieride and ursolic acid isolated from ethanol extracts of the stems were evaluated in the same cell lines, as well as on breast adenocarcinoma cell line (MCF-7), and Mus musculus skin melanoma cell line (B16F10). The chromatographic profiles of the dichloromethane fractions were obtained by high performance liquid chromatography. The results revealed that the season during which A. schottii was collected, and the part of the plant analyzed, influence the cytotoxicity on the K562 cells tested. On the other hand the dichloromethane fractions, mainly from the stems and roots, are responsible for the cytoxicity on the cells tested. These results may be associated with the seasonal variation of plumericin in these parts of the plant. This information is in accordance with the HPLC analysis. The resultsclearly show the potential for the phytotherapeutic use of this species, and suggest that the cytotoxic activity observed may be due to the presence of plumericin, or to minor com-pounds not yet identified. The seasonal influence on the production of secondary metabolites was verified.
*A quem a correspondência deve ser enviada ResumoOs fermentadores tipo air lift oferecem vantagens tais como: eficiente homogeneização dos componentes, baixo cisalhamento e economia de energia, pois o meio é agitado pelo processo de aeração, sem necessidade de agitação mecânica. O objetivo deste trabalho foi analisar a cinética de crescimento de Saccharomyces boulardii neste fermentador, com aeração de 1 e 1,5 vvm (volume de ar por volume de meio, por minuto), comparada com o crescimento em frascos agitados em shaker, visando a futura aplicação deste fermentador, em escala industrial. Os resultados indicaram que houve uma diminuição do pH com o consumo da glicose do meio, a qual foi totalmente consumida até o final da fase exponencial, de 5 e 6 horas para o shaker e o air lift, respectivamente. Após este período houve uma alteração na velocidade de crescimento de S. boulardii, em ambos os equipamentos, indicando uma possível mudança na fonte de carbono utilizada, uma vez que toda a glicose foi consumida após estes períodos. Os valores de velocidades específicas de crescimento foram semelhantes para o shaker e air-lift com 1,0 vvm, porém inferiores ao air-lift com 1,5 vvm, indicando que neste último reator há possibilidades de se conseguir uma velocidade de produção celular maior, dependendo apenas da eficiência de oxigenação oferecida. Palavras-chave: S. boulardii; fermentação; air lift; shaker. AbstractThis work aimed to analyze the kinetics of S. boulardii growth in an air lift fermentor under two aeration conditions: 1 and 1.5 air vvm (air volume per volume of culture medium per minute), in comparison with growth in shaken flasks, with a view to the future application of this fermenter on an industrial scale. Air lift fermentors offer advantages such as efficient homogenization of the components, low shear stress, and energy savings because the medium is stirred by aeration and does not require mechanical stirring. The pH of the medium decreased with the glucose uptake during the exponential phase, probably due to the formation of secondary metabolites. The entire process showed a similar specific growth rate during the exponential phase (up to 5 hours in the case of the shaker and 6 hours in that of the air-lift fermentor), indicating a possible change in the carbon source, since all the glucose was depleted after the aforementioned periods. After 6 hours, the growth rates in the shaker and the fermentor were similar under 1.0 vvm, but lower than in the fermentor under 1.5 vvm, suggesting that the fermentor may reach a higher cell production rate depending only on the oxygenation efficiency.
Epidendrum mosenii is a Brazilian medicinal plant, traditionally used to treat infective and dolorous processes. The present article reports a comparative study of the chemical and pharmacological aspects of different parts and seasons of this plant. The results demonstrate that 24-methylenecycloartanol (1), one of the main active principles present in this plant, is located practically in all the parts and during all seasons, but it is much more concentrated in the stems when collected in spring and summer. The pharmacological results indicate that dichloromethane extracts collected in spring and summer were the most active when evaluated against the writhing test in mice, being several times more potent than some reference drugs used as comparison. Together, the results strongly suggest that the antinociceptive effect of E. mosenii is related, at least in part, to the presence of compound 1, and this finding could be useful for quality control of phytopreparations based on this plant.
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