ABSTRACT
Bredemeyera floribunda roots are popularly used to treat snakebites in the semiarid region of Northeast Brazil, and previous studies indicate the anti-ophidian actions of triterpenoid saponins found in its roots. To assess B. floribunda root extract (BFRE) activity against the effects of Bothrops jararacussu venom (BjuV), antiphospholipasic, antiproteolytic, antihemorrhagic, antinecrotic, and anti-edematogenic activities were investigated in mice. Phytochemical analysis revealed the presence of saponins, flavonoids, and sugars, with rutin and saccharose being the major constituents of BFRE. Acute toxicity was determined and BFRE was nontoxic to mice. Phospholipase A2 and proteolytic activities induced by BjuV were inhibited in vitro by BFRE at all concentrations tested herein. BFRE (150 mg/kg) inhibited paw edema induced by BjuV (50 µg/animal), reducing total edema calculated by area under the curve, but carrageenan-induced paw edema was unchanged. Hemorrhagic and necrotizing actions of BjuV (50 µg/animal) were considerably decreased by BFRE treatment. Thus, BFRE blocked the toxic actions of B. jararacussu venom despite having no anti-inflammatory activity, which points to a direct inhibition of venom's toxins, as demonstrated in the in vitro assays. The larger amounts of rutin found in BFRE may play a role in this inhibition, since 3′,4′-OH flavonoids are known inhibitors of phospholipases A2.
Subject(s)
Animals , Male , Rats , Antivenins/pharmacology , Plant Extracts/pharmacology , Plant Roots/chemistry , Crotalid Venoms/antagonists & inhibitors , Edema/drug therapy , Hemorrhage/etiology , Antivenins/isolation & purification , Bothrops , Crotalid Venoms/toxicity , Polygalaceae/chemistry , Disease Models, Animal , Dose-Response Relationship, Drug , Edema/etiology , Hemorrhage/drug therapyABSTRACT
Ethanol extract of the leaves of Paullinia elegans Cambess., Sapindaceae, and its hexane, chloroform, ethyl acetate, and hydroethanol fractions were evaluated for their antiedematogenic and free radical scavenging activities. The ethanol extract and the hexane fraction produced statistically significant inhibition (74.4 and 76.0 percent, respectively) of the ear edema induced by croton oil in mice, observed at doses of 5 mg/ear. The ethyl acetate and hydroethanol fractions showed significant radical scavenging effect in the DPPH assay, with IC50 of 36.7 and 30.1 µg/mL, respectively. Fractionation of the extracts through chromatographic methods afforded epifriedelanol, oleanolic acid 3-O-acetyl, a mixture of stigmasterol 3-β-O-glucopyranoside and sitosterol 3-β-O-glucopyranoside, kaempferol 3,7-O-α-dirhamnopyranoside, kaempeferol-3-O-α-rhamnopyranoside and 2-O-methyl-chiro-inositol. The compounds were identified on the basis of their NMR spectral data and comparison with those of literature.
O extrato etanólico das folhas de Paullinia elegans Cambess., Sapindaceae, e as frações n-hexano, clorofórmio, acetato de etila e hidroetanólica, obtidas de seu fracionamento, foram avaliadas quanto às suas atividades anti-edematogênica e sequestradora de radicais livres. O extrato etanólico e a fração hexano produziram inibição significativa (74,4 e 76,0 por cento, respectivamente) do edema da orelha induzido pelo óleo de cróton em ratos, em doses de 5 mg/orelha. As frações acetato de etila e hidroetanólica mostraram atividade sequestradora de radicais livres no ensaio de DPPH, com IC50 de 36,7 e de 30,1 µg/mL, respectivamente. O fracionamento dos extratos pelo uso de métodos cromatográficos resultou no isolamento do epifriedelanol, ácido 3-O-acetil oleanólico, mistura do stigmasterol 3-β-O-glucopiranosídeo e sitosterol 3-β-O-glucopiranosídeo, canferol, canferol 3,7-O-α-diramnopiranosídeo, canferol 3-O-α-ramnopiranosídeo e 2-O-metil-chiro-inositol. Os compostos foram identificados com base na comparação de seus dados espectroscópicos de RMN com os da literatura.
ABSTRACT
O presente estudo investigou as atividades antinociceptiva e antiedematogênica do extrato etanólico das folhas de J. princeps através dos testes de contorções abdominais, formalina, placa quente e edema de pata induzido por carragenina. O extrato etanólico reduziu (p < 0,05) as contorções abdominais (100 mg/kg = 55,75±1,29 e 200 mg/kg = 47,75±1,35) quando comparado ao grupo controle (67,25±1,51). Ambas as fases do teste de formalina foram inibidas (p < 0,05): 1ª fase (50 mg/kg = 79,50±1,12; 100 mg/kg = 69,37±1,03 e 200 mg/kg = 56,75±1,95) e 2ª fase (50 mg/kg = 86,50±1,22; 100 mg/kg = 69,62±1,66 e 200 mg/kg = 49,37±1,50). Após 90 min de tratamento, o limiar nociceptivo dos animais quando avaliados no modelo de placa quente foi aumentado de forma significativa com o extrato nas doses de 100 mg/kg (8,12±0,48) e 200 mg/kg (10,25±0,45) quando comparados com o grupo controle (6,62±0,46). Após 3 h de aplicação da carragenina, a dose de 200 mg/kg (0,43±0,02) reduziu o edema de pata em relação ao grupo controle (0,55±0,04). Este efeito também foi observado nas doses de 100 mg/kg (0,52±0,04) e 200 mg/kg (0,45±0,02) após 4 h de experimento (controle = 0,63±0,03). Estes resultados sugerem que J. princeps pode constituir uma fonte de substâncias ativas com atividades antinociceptiva e antiedematogênica.
The antinociceptive and anti-edematogenic activities of ethanol extract of Joannesia princeps leaves were investigated in male rats. The responses tested were acetic acid writhing, paw licking induced by formalin, hot plate and carrageenan-induced paw edema. The ethanol extract reduced (p<0.05) the abdominal contortions (100 mg/kg = 55.75±1.29 and 200 mg/kg = 47.75±1.35) in comparison with the control group (67.25±1.51). Both phases of paw lick were inhibited (p < 0.05): 1st phase (50 mg/kg = 79.50±1.12; 100 mg/kg = 69.37±1.03; 200 mg/kg = 56.75±1.95; controls 84.37±1.91) and 2nd phase (50 mg/kg = 86.50±1.22; 100 mg/kg = 69.62±1.66; 200 mg/kg = 49.37±1.50; controls 91.87±1.31). After 90 min of treatment, the reaction time on the hot plate increased at the doses 100 mg/kg (8.12±0.48) and 200 mg/kg (10.25±0.45), compared to the control group (6.62±0.46). After 3 h of application of carrageenan, a dose of 200 mg/kg (0.43±0.02) inhibited the paw edema, compared to the control group (0.55 ± 0.04). This effect was also observed at doses of 100 mg/kg (0.52±0.04) and 200 mg/kg (0.45±0.02) after 4 h of the experiment (control = 0.63 ± 0.03). These results suggest that the Brazilian arara-nut tree, J. princeps, could constitute a source of active substances with antinociceptive and anti-edematogenic activities and, after further tests, may help to validate the use of this plant in popular medicine.
Subject(s)
Animals , Male , Rats , Analgesics , Euphorbiaceae , Phytotherapy , Mice , Plants, MedicinalABSTRACT
We tested the capacity of leaf (Urera baccifera, Loasa speciosa, Urtica leptuphylla, Chaptalia nutans, and Satureja viminea) and root (Uncaria tomentosa) extracts to inhibit edema induced by Bothrops asper snake venom. Edema-forming activity was studied plethysmographically in the rat hind paw model. Groups of rats were injected intraperitoneally with various doses of each extract and, one hour later, venom was injected subcutaneously in the right hind paw. Edema was assessed at various time intervals. The edematogenic activity was inhibited in those animals that received an injection U. tomentosa, C. nutans or L. speciosa extract. The extract of U. baccifera showed a slight inhibition of the venom effect. Extract from S. viminea and, to a lesser extent that of U. leptuphylla, induced a pro-inflammatory effect, increasing the edema at doses of 250 mg/kg at one and two hours.
Se investigó la capacidad de los extractos de las hojas de Urera baccifera, Loasa speciosa, Urtica leptuphylla, Chaptalia nutans, Satureja viminea y de la raíz de Uncaria tomentosa para inhibir el edema inducido por el veneno de Bothrops asper por métodos pletismométricos. Los grupos de ratas fueron inyectados intraperitonealmente con varias dosis de cada extracto y una hora mas tarde se inyectó veneno por vía subcutánea en la pata trasera derecha de la rata. Se evaluó el edema en distintos intervalos de tiempo. Los resultados muestran que la actividad edematogénica fue inhibida en los animales que recibieron los extractos de raíz de U. tomentosa, hojas de C. nutans y L. speciosa. Los extractos de hojas de U. baccifera mostraron leve inhibición del efecto del veneno. El extracto de hojas de S. viminea y en menor grado el de U. leptuphylla indujeron un efecto pro inflamatorio.