Involvement of GABAergic pathway in the sedative activity of apigenin, the main flavonoid from Passiflora quadrangularis pericarp

Abstract In the current study we showed that oral administration of an aqueous extract of Passiflora quadrangularis L., Passifloraceae, pericarp results in a significant prolongation of the sleep duration in mice evaluated in the ethyl ether-induced hypnosis test which indicates sedative effects. Apigenin, the main flavonoid of the extract, induced a similar sedative response when applied alone, at a dose equivalent to that found in the extract, suggesting that apigenin is mediating the sedative effects of P. quadrangularis extract. In addition, the sedative effect of apigenin was blocked by pretreatment with the benzodiazepine antagonist flumazenil (1 mg/kg), suggesting an interaction of apigenin with gamma-aminobutyric acid type A (GABAA) receptors. However, apigenin at concentrations 0.1–50 µM failed to enhance GABA-induced currents through GABAA receptors (α1β2γ2S) expressed in Xenopus oocytes. Nevertheless, based on our results, we suggest that the in vivo sedative effect of the P. quadrangularis extract and its main flavonoid apigenin maybe be due to an enhancement of the GABAergic system.

Anti-inflammatory and opioid-like activities in methanol extract of Mikania lindleyana, sucuriju

Mikania lindleyana DC., Asteraceae (sucuriju), grows in the Amazon region, where is frequently used to treat pain, inflammatory diseases and scarring. This study was carried out to investigate phytochemical profile accompanied by in vivo antinociceptive and anti-inflammatory screening of n-hexane (HE), dichloromethane (DME) and methanol (ME) extracts obtained from the aerial parts of the plant. The oral administration of ME (0.1, 0.3, 1 g/kg) caused a dose-related reduction (16.2, 42.1 e 70.2 percent) of acetic acid-induced abdominal writhing while HE and DME (1 g/kg, p.o.) were ineffective. In the hot plate test, ME (300 mg/kg, p.o.) increased the latency of heat stimulus between 30 and 120 min and inhibited the first (45 percent) and second (60 percent) phases of nociception in the formalin test. The antinociception induced by ME or positive control fentanyl (150 µg/kg, s.c.) in hot plate and formalin tests was prevented by naloxone (3 mg/kg, s.c.). When submitted to the carrageenan-induced peritonitis test, ME (0.5, 1.0, 2.0 g/kg, p.o.) impaired leukocyte migration into the peritoneal cavity by 46.8, 59.4 and 64.8 percent respectively, while positive control dexamethasone (2 mg/kg, s.c.), inhibited leukocyte migration by 71.1 percent. These results indicate that the antinociception obtained after oral administration of methanol extract of M. lindleyana involves anti-inflammatory mechanisms accompanied with opioid-like activity which could explain the use of the specie for pain and inflammatory diseases.

Evaluation of the central activity of the ethanolic extract of Acosmium subelegans (Mohlenbr) in mice

The ethanolic extract (EE) of Acosmium subelegans (Mohlenbr) Yakovl (perobinha-do-campo) was tested to behavioral paradigms in mice to investigate its putative central depressant effect. Oral pretreatment with the EE significantly reduced in a dose-dependent way the locomotor activity and increased by 30-55 percent the barbiturate sleep duration relatively to control values. At the highest dose (1,0 g.kg-1) it decreased the extension time/flexion time ratio of the maximal electroshockinduced convulsions, enhanced the latency to the pentylenetetrazol-induced convulsions and diminished by 26 percent the number of seizures, indicating an anticonvulsant action. No changes were observed in the motor coordination, the core temperature, climbing behavior, catalepsy and the plus-maze performance. The preliminary results indicate that the EE of A. subelegans induce a CNS depressant effect, more specifically an anticonvulsant effect that deserve a thorough investigation.

Influência da diabete experimental na atividade exploratória de ratos no labirinto em cruz elevado / Influence of experimental diabetes in the exploratory activity of rats in high cross labirinth

Indivíduos portadores de diabetes mellitus apresentam um elevado nível de ansiedade. Há também relatos a respeito de alterações de sua função cognitiva, porém esses sáo conflitantes. Neste estudo, investigamos se a indução de diabete experimental por estreptozotocina promove alterações de performance no teste do labirinto em cruz elevado (elevated plus-maze), empregado para avaliação da ansiedade e dos processos de aprendizagem e momória em animais de laboratório....

Evaluation of antinociceptive effect of Petiveria alliacea (guiné) in animals

Petiveria alliacea (Phytolaccaceae) is a bush widely distributed in South America including Brazil, where it is popularly known as "guiné", pipi", "tipi" or "erva-de-tipi". Brazilian folk medicine attributes to the hot water infusion of its roots or leaves the following pharmacologicalproperties: antipyretic, antispasmodic, abortifacient, antirrheumatic, diuretic, analgesic and sedative. The present study has evaluated the alleged effects of P. alliacea on central nervous system (CNS), particularly, the sedative and analgesic properties of root crude aqueous extract of this plant in mice and rats. This extract showed an antinociceptive effect in acetic acid - acetylcholine - and hypertonic saline - induced abdominal constrictions, but not in hot-plate and tail flick tests P. alliacea did not produce any CNS depressor effect. Thus its antinociceptive action in animals can be responsible by its poplar use as an analgesic.