ABSTRACT
Several secondary metabolites have been isolated from Zornia brasiliensis (Leguminosae), mainly flavonoids. These compounds are known for many pharmacological actions, such as antispasmodic and antidiarrheal. Therefore, we evaluated the antidiarrheal effect of the ethanolic extract obtained from Zornia brasiliensis aerial parts (ZB-EtOHAP), as well as its underlying mechanisms. Castor-oil-induced diarrhea, fluid accumulation, and intestinal transit (normal and castor oil induced) were performed to assess the antidiarrheal, antisecretory, and antipropulsive activities of the extract. The involvement of opioid and adrenergic pathways was also investigated. ZB-EtOHAP inhibited, in a dose-dependent manner, both total defecation frequency and the number of watery stools. The extract showed no effect on fluid accumulation or normal intestinal transit. On the other hand, when the animals were pretreated with castor oil, the extract decreased the distance traveled by the marker in the small intestine. Investigation of the involvement of opioid and adrenergic systems showed that the pharmacological potency of the extract did not change in the presence of naloxone, but it was reduced in the presence of yohimbine. The data indicate that Zornia brasiliensis has an antidiarrheal effect due to inhibition of the intestinal motility through adrenergic pathway activation.
ABSTRACT
Hyptis umbrosa (syn. Mesosphaerum sidifolium) (Lamiaceae Family) has been used to treat several conditions such as gastrointestinal disorders, skin infections, nasal congestion, fever and cramps. The objective of this study was to evaluate the chemical composition, analgesic and anti-inflammatory profiles of ethanol extract from leaves of Hyptis umbrosa (EEB). HPLC-DAD was used to determine the fingerprint chromatogram of the extract. Male Swiss mice were orally pretreated with EEB (100, 200 or 400 mg/kg; 60 min before initiating algesic stimulation) and antinociceptive activity was assessed using the acetic acid-induced writhing model, formalin test and hyperalgesia induced by glutamate or capsaicin. Also, peritonitis was induced by the intrathoracic injection of carrageenan to quantify the total number of leukocytes. The presence of phenolic compounds in the extract was confirmed using HPLC-DAD. The treatment with EEB, at all doses, produced a significant analgesic effect against acetic acid-induced antinociceptive activity. In the formalin test, only the 400-mg/kg-dose of EEB had a significant effect in the first phase. However, all doses tested were able to reverse nociception in the second phase. The effect of all doses of EEB also showed a significant antinociceptive effect in the glutamate and capsaicin tests and inhibited the carrageenan-induced leukocyte migration to the peritoneal cavity. The present study suggests that the EEB possesses peripheral analgesic action and showed potential in reducing the spreading of the inflammatory processes. Also, it seems to be related with vanilloid and glutamate receptors.
ABSTRACT
Mimosa paraibana Barneby foi submetida a um estudo fitoquímico para o isolamento de seus constituintes químicos, através de métodos cromatográficos usuais, e posterior identificação estrutural, utilizando-se métodos espectroscópicos de RMN ¹H e 13C uni e bidimensionais, além de comparações com modelos da literatura. Deste estudo pioneiro, foram isolados e identificados cinco constituintes da fase clorofórmica: uma mistura dos esteróides, β-sitosterol e estigmasterol, a 15¹-hidroxi-feofitina A, a 5,7-dihidroxiflavanona, o 3,4,5-trihidroxibenzoato de etila e o ácido p-cumárico. A atividade antioxidante das fases hexânica, clorofórmica e acetato de etila foi avaliada utilizando o radical estável DPPH (1,1-difenil-2-picril-hidrazil) e os resultados comparados com o padrão ácido ascórbico. A avaliação da citotoxicidade das fases foi realizada empregando-se o ensaio de letalidade contra Artemia salina. Dos extratos avaliados, somente o hexânico mostrou baixa toxicidade.
The phytochemical study of Mimosa paraibana Barneby led to the isolation of its chemical constituents, through the usual chromatographic methods, and further structural identification, using ¹H and 13C NMR spectroscopic methods based on one and two-dimensional techniques, in addition to comparison with literature data. From this pioneering investigation with M. paraibana, five constituents were isolated and identified from the chloroform extract: a mixture of β-sitosterol and stigmasterol, 15¹-hydroxy-phaeophytin A, 5,7-dihydroxyflavanone, ethyl 3,4,5-trihydroxybenzoate and p-coumaric acid. The antioxidant activity of the hexane, chloroform and ethyl acetate extracts of M. paraibana were measured using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging assay and the results compared with standard ascorbic acid. The toxicity activity of the extracts were performed using the bioassay of Artemia salina.
ABSTRACT
O óleo essencial das folhasde Rollinia leptopetala foi obtido por hidrodestilação em aparelho de Clevenger e a sua composição química foi analisada através de CG-EM. Com essa técnica, foi possível identificar 22 constituintes em uma mistura complexa demonoterpenos (54,5 por cento) e sesquiterpenos (45,5 por cento). O principal componente encontradonas folhas foi o biciclogermacreno (22,47 por cento). O óleo essencial foi avaliado numa linhagem de Staphylococcus aureus portadora de bomba de efluxo responsável pela resistência norfloxacino. Embora o óleo essencial não tenha apresentado atividade antibacteriana relevante in vitro, ele apresentou atividade moduladora da resistência, ou seja, em combinação com o norfloxacino observou-se uma redução de 4x na concentração inibitória mínima do antibiótico, indicando inibição de bomba de efluxo.
The essential oil from the leaves of Rollinia leptopetala was obtained by hydrodistillation in Clevenger's apparatus and its chemical composition was analyzed by GC-MS. With this technique could be identified 22 constituents in a complex mixture of monoterpenes (54.5 percent) and sesquiterpenes (45.5 percent). The main component found in the leaves was the bicyclogermacrene (22.47 percent). The essential oil was assayed against a strain of Staphylococcus aureus possessing efflux mechanism of resistance to norfloxacin. Although the essential oil did not display relevant antibacterial activity in vitro, it modulated the activity of the norfloxacin, i.e. in combination with the antibiotic it was observed a fourfold reduction in the minimum inhibitory concentration for norfloxacin, indicating inhibition of efflux pump.
