RESUMO
The leaves of the Cashew plant (Anacardium occidentale L.) are used by the folk medicine in South America and West Africa. This plant is rich in flavonoids, which are polyphenolic compounds widespread in plants, and that have diverse physiological effects. In a sub-acute toxicity assay it was found that an ethanolic extract of Cashew leaves elicited lymphopenia in rats. The extract was also found to be cytotoxic and to induce apoptosis in Jurkat (acute lymphoblastic leukemia) cells. The crude ethanolic extract was fractionated and resolved by HPLC. One of the four fractions obtained led to the isolation of the biflavonoid agasthisflavone. [(3)H]-thymidine incorporation assays and flow cytometry analysis showed that the isolated compound displayed a high anti-proliferative effect in Jurkat cells with an IC(50) of 2.4 µg/ml (4.45 µM). The effect of agathisflavone on the acute promyelocytic leukemia cell line HL60, Burkitt lymphoma Raji cells and Hep-2 laryngeal carcinoma cells was also tested. The two latter ones were only mildly affected by agathisflavone. It is also shown that agathisflavone induces apoptosis in Jurkat cells and it this proposed that this is the likely mechanism of agathisflavone specific cytotoxicity.
Assuntos
Anacardium/química , Biflavonoides/farmacologia , Proliferação de Células/efeitos dos fármacos , Linfócitos/efeitos dos fármacos , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Animais , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Flavonoides/farmacologia , Citometria de Fluxo , Células HL-60 , Humanos , Células Jurkat , Masculino , Folhas de Planta/química , Ratos , Ratos WistarRESUMO
The antiulcerogenic effect of a hydroethanolic extract of Anacardium occidentale L. leaves was investigated. The extract inhibited gastric lesions induced by HCl/ethanol in female rats. A dose-response effect study showed that the ED50 was 150 mg/kgb.w. Extract doses higher than 100 mg/kgb.w. were more effective than 30 mg/kg of lansoprazol in inhibiting gastric lesions. A methanolic fraction (257.12 mg/kg) which reduced gastric lesion at 88.20% is likely to contain the active principle of the antiulcer effect. No signs of acute toxicity were observed when mice were treated with extract dose up to 2000 mg/kgb.w. A chemical analysis of the extract allowed the identification of phenolic compounds as the major components. Glycosylated quercetin, amentoflavone derivate and a tetramer of proanthocyanidin were identified by liquid chromatography coupled to mass spectrometry. The level of total phenolics in the extract was evaluated at 35.5% and flavonoid content was 2.58%.
Assuntos
Anacardium/química , Antiulcerosos/farmacologia , Antiulcerosos/toxicidade , Animais , Antiulcerosos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Etanol , Feminino , Masculino , Camundongos , Fenóis/química , Fenóis/isolamento & purificação , Folhas de Planta/química , Solventes , Espectrometria de Massas por Ionização por Electrospray , Taninos/isolamento & purificação , Taninos/farmacologia , Taninos/toxicidade , ÁguaRESUMO
Anacardium occidentale L. (Anacardiaceae), popularly known as cajueiro is a native plant to Brazil, and largely used in popular medicine to treat ulcers, hypertension and diarrhea. In the present study, acute, 30-day subacute toxicity and genotoxicity assays were carried out. The crude extract did not produce toxic symptoms in rats in doses up to 2000 mg/kg. Based on biochemical analyses of renal and hepato-biliary functions, such as the level of urea, creatinine, transaminases and alkaline phosphatase, we determined that the extract is generally tolerated by rats. This was also confirmed by hematological and histopathological exams. Genotoxicity was accessed by the Ames test in Salmonella typhimurium strains TA97, TA98, TA100, TA102 and by the bone marrow micronucleus test in mice. The extract was shown to induce frameshift, base pair substitution and damage to the chromosomes. However, this effect was less deleterious than the clastogenic effect of ciclophosphamide.
Assuntos
Anacardium/química , Extratos Vegetais/toxicidade , Animais , Brasil , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Etanol , Testes de Mutagenicidade , Mutagênicos , Mutação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , RatosRESUMO
Os extratos totais, assim como os compostos fenólicos isolados de diferentes partes de Anacardium occidentale conhecido popularmente no Brasil como cajueiro mostraram atividades antiúlcera e antibacteríana. O objetivo deste trabalho foi a verificação destas atividades nas folhas após estudo farmacobotânico, químico e toxicológico. Para a analise anatômica foram utilizados cortes do terço mediano inferior da lâmina foliar. Nesta, as epidermes em vista frontal apresentam cutrcula estriada, na face abaxial, a epiderme é constituída de células de formato poligonal, com paredes bem justapostas. Na face adaxial, as células são de paredes espessas, ligeiramente onduladas. A mesma é constituída de estômatos de tipo anomocítico e de tricomas glandulares de forma ovóide. O mesófilo é constituído de duas camadas de parênquima paliçádico, espessas, de forma quase regular e de parênquima lacunoso com células de forma irregular, envolvendo os feixes vasculares de nervuras secundarias. Extensões de fibras são observadas no mesófilo. A nervura mediana possui um colênquima desenvolvido e ductos são encontrados no floema assim como no parênquima medular. Drusas são encontradas no parênquima lacunoso assim como no parênquima fundamental e no colênquima. A partir da triagem fitoquímica, da cromatografia em camada delgada, cromatografia liquida de alta eficiência e cromatografia liquida acoplada a espectrometria de massa, verificou-se a presença nas folhas de cajueiro de compostos polifenólicos, particularmente de heterosfdeos flavonóidicos. As estruturas de flavon6ide que parecem ser mais evidentes, de acordo com a cromatografia liquida acoplada a massa, são principalmente os heterosídeos da quercetina...
Crude extracts as well as phenolics isolated from the bark or the fruit of Anacardium occidentale popularly known as cajueiro in Brazil, showed antiulcer and antibacterial effects. The aim of this work was to verify those effects in the leaf, botanical, chemical and toxicological studies. Ultrastructure of the leaf was carried on. Cross-sections from the third inferior part of the leaf blade were used. Cashew leaf contains uniseriate epidermis with a sub-eperdimic layer, anomocytic stomata and glandular ovoid trichomes on the inferior surface. The mesophyll exhibits two cell layers of palisadic parenchyma and a lacunose parenchyma containing vascular bundles of the secondary nervures. The median nervure contains a developed collenchyma. Several druses of calcium oxalate are present in the fundamental parenchyma, lacunose parenchyma and in the collenchyma. Resin ducts are also observed in the phloem as well as in the medullar parenchyma. Extensions of sclerenchymatous fibres are observed in the mesophyll. By phytochemical analyses using TLC, HPLC-DAD and positive ions LC-ESIMS, we verified the presence of polyphenols in cashew leaves particularly heterosids of flavonoids. From LC-ESI-MS, evident structures of flavonoids seemed to be heterosids of quercetin. Ethanol 70% extract of cashew leaves was used for antiulcer and antibacterial essays. With extract dose 400mg/kg, ulcer lesions induced by HCL/ethanol 60% in rats, decreased about 98%. By a dose-response effect study, ED50 was evaluated about 150 mg/kg. Extract doses higher than 100mg/kg showed potential of lesion inhibition superior to lansoprazol 30mg. Extract methanolic fraction that gave 88,20% of ulcer inhibition likely contains the principie active of the antiulcer effect. Using bacterial strains, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 35218 and ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and a clinical isolate Campylobacter coli, for antibacterial essay, the ethanolic extract and one fraction rich in flavonoids were only active in S. aureus with MIC and MBC equal to 320 µg/mL. Acute, 30-day and 90-day subacute toxicity studies were carried out. Crude extract DL50 was superior to 2000mg/kg. Based on biochemical analyses for the evaluation of renal and hepato-biliary functions, level of urea, creatinine, transaminases, total protein, albumin, bilirubin, cholesterol and calcium proved that the extract is biologically tolerated by rat organismo This result was also confirmed by studies in hematology and histopathology. Genotoxity was accessed by Ames test in Salmonella typhimurium strains TA97, TA98, TA100, TA102 and bone marrow micronucleus test in mice. The extract exhibited sign of frameshift and base pairs substitution. Extract dose 2000mglkg seemed to induce damage in the chromosomes however; the activity was extremely inferior to the c1astogenic effect induced by ciclophosphamide.