Oral Administration of Euterpe oleracea Mart., Its Influence over Body Weight and Lymphoid Organs and Alterations in Haematological and Glycaemical Parameters.

Aims: The aims of the study were to evaluate alterations caused by the oral administration of the aqueous extract of Euterpe oleracea to non-isogenic adult male mice during 15 and 30 consecutive days through the comparison of body and spleen weights, number of splenic and medullary cells, their hemogram and glycemia indices. Study Design: Animals were divided into 8 groups (5 animals/group). Treated groups received the AEA concentration (125 mg/ml by gavage) at doses of 5, 50 and 500 mg/kg for 15 and 30 days. The control group received only the vehicle of dilution (1x PBS) in volume of 0.5 ml. After treatment the animals were sacrificed in a CO2 chamber for testing. Place and Duration of Study/Methodology: The aqueous extract of concentration of 125 mg/ml of lyophilized açaí pulp was prepared in Laboratory of General and Analytical Chemistry of Federal University of Amapá. Values of body weight, weight of liver and spleen, number of spleen and bone marrow cells, blood count and glucose of the mice were conducted on Drugs Research Laboratory between January and November of 2013. Results: The statistical analysis was done by ANOVA test two-way with significance level p<0.05 in relation to control followed by Tukey post-test. The AEA caused significant changes in body weight, about 22% in animals treated with 500mg/kg. Weight of spleen showed no significant changes, there was statistical difference in blood glucose levels between groups 5 and 500 mg/kg treated for 15 days and punctually in the 500 mg/kg group treated for 15 and 30 days. It was observed that the treatment with the AEA doses (5, 50 and 500 mg/kg) for 30 days increased the number of bone marrow cells. Regarding the number of spleen cells, treatment promoted changes, reducing the amount of cells during the 30 days of treatment, principally at the dose of 50 mg/kg. During the 15 day treatment of 500 mg/kg there was an increase in the number of spleen cells. Conclusion: The treatment of mice with aqueous extract of açaí pointed that the concentration has significant influence in: 1) glucose concentration in the blood; 2) The increased number of bone marrow cells; 3) and the number of spleen cells. Thus, comparison between groups of animals was compatible with the hypothesis that the increase in body mass is a risk factor for insulin resistance.

Study of dissolution profiles and desintegration of capsules containing the dried hydroethanolic extract of Calophyllum brasiliense

Calophyllum brasiliense Cambess, Calophyllaceae, is of great interest in folk medicine and is used in the treatment of various diseases such as diabetes. Granules containing the hydroethanolic extract from the stem bark of C. brasiliense were obtained. The polyphenol content was standardized, and the average weight, disintegration, and the dissolution profiles of the capsules were determined after encapsulation. The capsules had an average weight of 574.5±8.0 mg. In vitro tests showed that the most efficient disintegration profile was in hydrochloric acid buffer (pH 1.2), with a capsule disintegration time within 9 min. The dissolution analysis showed a better uniformity of capsule content release when the test was performed in a hydrochloric acid buffer (pH 1.2), with a maximal release rate at 15 min (giving a polyphenol content of 4.38%, which corresponds to a concentration of 0.0080 mg/mL). In distilled water, the maximal release was reached at 20 min (giving a polyphenol content of 5.41%, which is equivalent to 0.0105 mg/mL). In phosphate buffer, the maximal release of capsule contents was reached at the end of the dissolution assay (30 min), with the lowest amount of released polyphenols (3.61%, which corresponds to a concentration of 0.0070 mg/mL). The encapsulated form of the hydroethanolic extract of C. brasiliense was shown to have the necessary traits of a desirable delivery agent, and the dissolution test was an effective analysis of this material's polyphenol release profile for the specific dosage form.

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 percent, 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 percent (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 percent (p<0.01). In ear erythema induced by croton oil, OEO presented a significant inhibition (37.9 percent). In the vascular permeability test, treatment with OEO decreased the response to histamine, inhibiting vascular permeability by 54.16 percent. In carrageenan-induced peritonitis, OEO reduced the number of neutrophils migrating compared to the control group by 80.14 percent. 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 / Atividades anti-inflamatória e analgésica de extratos padronizados de Hypericum brasiliense (Willd)

As atividades antiinflamatória e antinociceptiva do extrato padronizado de Hypericum brasiliense (HBSE) (Guttiferae) foi avaliada em modelos animais. Ratos Wistar machos foram tratados com extrato de H. brasiliense (50, 250 e 500 mg/kg, v.o.) em solução 3 por cento Tween 80 0,9 por cento NaCl. O tratamento com HBSE (500 mg/kg) mostrou inibição significativa sobre o edema induzido por carragenina comparado ao grupo controle. Nessa dose, o edema foi reduzido em 31,25 por cento na terceira hora (pico do edema) após o tratamento, mas na dose de 50 mg/kg, o edema apresentou redução de 53,13 por cento (p < 0,05). Ainda com a dose de 50 mg/kg, a diminuição do edema induzido por dextrana foi similar ao controle positivo, ciproeptadina. Houve diminuição na formação do tecido granulomatoso (6,6 por cento) comparável ao grupo controle. O HBSE também inibiu o número de contorções abdominais em 46,4 por cento, estatisticamente igual ao controle positivo, tratado com indometacina (42,9 por cento). Na dose de 250 mg/kg, houve inibição do número de contorções em 70,7 por cento quando comparado ao grupo controle (p < 0,001). No teste da placa-quente, foi verificado aumento no tempo de latência com a dose de 50 mg/kg. Os resultados demonstram que o HBSE possui atividade antiinflamatória sobre processos agudos, principalmente quando sua gênese está relacionada à síntese dos derivados do ácido araquidônico, e seu efeito analgésico provavelmente envolve ação sobre o Sistema Nervoso Central.

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 percent Tween 80 0.9 percent 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 percent in the third hour after treatment (edema peak), but the dose of 50 mg/kg has inhibited the edema by 53.13 percent (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 percent) 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 percent) was comparable to that produced by indomethacin (42.9 percent). A dose of 250 mg/kg inhibited these constrictions by 70.66 percent 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.

Comparative anti-inflammatory and antinociceptive effects of terpenoids and an aqueous extract obtained from Croton cajucara Benth

The 19-nor-clerodane trans-crotonin (CTN) and the triterpene acetyl aleuritolic acid (AAA), isolated from the stem bark of Croton cajucara Benth (Euphorbiaceae), a traditional medicinal plant from Amazon region of Brazil, as well as the aqueous extract (AE) from its stem bark, were submitted to pharmacological screening for anti-inflammatory and antinociceptive activities in animal models. The oral administration of AAA (50 mg/kg), CTN (50 mg/kg) or AE (300 mg/kg) inhibited the acetic acid-induced writhing in mice. The AE, CTN and AAA had shown significant inhibition of carrageenin-induced edema in rats, in all time intervals measured after the injection of the stimulus, with the greatest inhibition at the first hour for AAA (47.7 percent) and the second hour for CTN (54.4 percent). They have also exhibited significant inhibition in the dextran-induced edema 90 minutes after the stimulus: 31.9 percent for CTN and 28.5 percent for AAA. In the histamine-induced edema, the inhibition showed by CTN and AAA were 43.2 percent and 40.5 percent, respectively, 90 minutes after the injection of stimulus. This study extends and supports the popular medicine and folkloric uses of Croton cajucara in the Amazon region of Brazil.

O 19-nor-clerodano trans-crotonina (CTN) e o triterpeno ácido acetil aleuritólico (AAA), isolados das cascas do caule de Croton cajucara Benth (Euphorbiaceae), uma planta tradicional da Região Amazônica do Brasil, bem como o extrato aquoso (EA) das cascas do caule deste Croton, foram submetidos a experimentos farmacológicos utilizando animais, para avaliação das atividades anti-inflamatória e antinociceptiva. A administração oral de AAA (50 mg/kg), CTN (50 mg/kg) ou AE (300 mg/kg) inibiram as contorções em ratos, induzidas por ácido acético. Os terpenóides AAA e CTN, bem como o extrato polar EA, inibiram significativamente o edema de pata em ratos, induzido por carragenina. As inibições foram observadas em todos os intervalos de medições, tendo sido evidenciado melhores inibições para os terpenóides AAA (47,7 por cento, após a primeira hora) e CTN (54,4 por cento, após a segunda hora). Evidenciou-se ainda, após 90 minutos do estímulo, significante inibição no edema induzido por dextrana (31,9 por cento para CTN e 28,5 por cento para AAA) e por histamina (43,2 por cento para CTN e 40,5 por cento para AAA). Estes resultados confirmam o uso popular de Croton cajucara na região Amazônica do Brasil, no combate a inflamações.