Anti-inflammatory and antinociceptive activities of Euterpe oleracea Mart., Arecaceae, oil

The oil of the fruits of Euterpe oleracea Mart., Arecaceae (OEO), was evaluated in models of inflammation and hyperalgesia in vivo to study its effects on these conditions. The experimental models contained the writhing test in mice, rat paw edema, granuloma test in rats, vascular permeability in rats, cell migration to the peritoneal cavity in rats and ear erythema induced by croton oil in mice. Doses of 500, 1000 and 1500 mg/kg of OEO were administered orally. The observed number of writhes was inhibited by 33.67, 45.88 and 55.58%, respectively. OEO produced a dose-dependent effect, with linear correlation coefficient R=0.99 (y=0.0219x+23.133), and the median effective dose found was 1226.8 mg/kg. The oral administration of 1226.8 mg/kg of OEO inhibited carrageenan-induced edema by 29.18% (p<0.05) when compared to the control group. The daily administration of OEO for six days inhibited the formation of granulomatous tissue by 36.66% (p<0.01). In ear erythema induced by croton oil, OEO presented a significant inhibition (37.9%). In the vascular permeability test, treatment with OEO decreased the response to histamine, inhibiting vascular permeability by 54.16%. In carrageenan-induced peritonitis, OEO reduced the number of neutrophils migrating compared to the control group by 80.14%. These results suggested that OEO has anti-inflammatory and antinociceptive activities, probably of peripheral origin and linked to prostaglandin biosynthesis inhibition

Anti-inflammatory and analgesic activities of Hypericum brasiliense (Willd) standardized extract

The anti-inflammatory and antinociceptive activities of the standardized leaves extract (HBSE) of Hypericum brasiliense (Guttiferae) were evaluated in animal models. Male Wistar rats were treated with H. brasiliense extract (50, 250 and 500 mg/kg, p.o.) in 3% Tween 80 0.9% saline solution. The treatment of the edema induced by carrageenin with HBSE (500 mg/kg) showed significant inhibition when compared to the control group. At this dose, the edema decreased by 31.25% in the third hour after treatment (edema peak), but the dose of 50 mg/kg has inhibited the edema by 53.13% (p < 0.05). At the dose of 50 mg/kg, the decrease of the edema induced by dextran was similar to that caused by cyproheptadine. The decrease of the formation of granulomatous tissue (6.6%) was comparable to the control group. The HBSE inhibited the abdominal constrictions induced by acetic acid. At a dose of 50 mg/kg, the inhibition of the abdominal constrictions (46.4%) was comparable to that produced by indomethacin (42.9%). A dose of 250 mg/kg inhibited these constrictions by 70.66% when compared to control (p < 0.001). In the hot-plate test, an increase in the latency time was observed at a 50 mg/kg dose. These data suggest that HBSE has anti-inflammatory activity on acute process, developed principally by arachdonic acid derivates and analgesic effect due to its probable involvement in the Central Nervous System

Avaliação toxicológica do óleo essencial de Piper aduncum L.

Este trabalho teve como objetivo a avaliação da toxidade aguda e subaguda do óleo essencial de Piper aduncum pela determinação da DL50 em camundongos e a análise dos parâmetros bioquímicos e hematológicos em ratos. A planta é utilizada na medicina popular da região amazônica em diversas doenças e no seu óleo essencial o constituinte majoritário é o fenilpropanóide dilapiol, com propriedades inseticida, fungicida, bactericida, larvicida e moluscicida. A DL50 foi de 2,400 ± 191,7 mg/kg. O óleo essencial não alterou de maneira significativa os parâmetros hematológicos e bioquímicos em relação ao controle no tratamento subagudo, exceto a redução da creatinina. O valor da DL50 e os resultados observados nos parâmetros hematológicos e bioquímicos sugerem que o óleo essencial apresenta toxidade baixa

A Combined Study Using Ligand-Based Design, Synthesis, and Pharmacological Evaluation of Analogues of the Acetaminophen Ortho-Regioisomer with Potent Analgesic Activity

A ligand-based drug design study was performed to acetaminophen regioisomers as analgesic candidates employing quantum chemical calculations at the DFT/B3LYP level of theory and the 6-31G* basis set. To do so, many molecular descriptors were used such as highest occupied molecular orbital, ionization potential, HO bond dissociation energies, and spin densities, which might be related to quench reactivity of the tyrosyl radical to give N-acetyl-p-benzosemiquinone-imine through an initial electron withdrawing or hydrogen atom abstraction. Based on this in silico work, the most promising molecule, orthobenzamol, was synthesized and tested. The results expected from the theoretical prediction were confirmed in vivo using mouse models of nociception such as writhing, paw licking, and hot plate tests. All biological results suggested an antinociceptive activity mediated by opioid receptors. Furthermore, at 90 and 120 min, this new compound had an effect that was comparable to morphine, the standard drug for this test. Finally, the pharmacophore model is discussed according to the electronic properties derived from quantum chemistry calculations.CAPESCNPqFAPESPAPARDUFPAPARD-UFP