RESUMO: "O papel controvertido da kava (Piper methysticum G. Foster) -Fitoterápico ansiolítico, na hepatite tóxica". Kava é um fi toterápico ansiolítico usado no tratamento da insônia e da ansiedade. Alguns casos de hepatotoxicidade induzida pela kava foram relatados na literatura, levando à proibição do seu uso em muitos países. Clinicamente, o espectro dessas alterações variou de elevações transitórias das enzimas hepáticas, até à falência hepática fulminante e morte. Em alguns casos, realizou-se transplante hepático. Este artigo revisa a literatura atual sobre a hepatite tóxica provavelmente relacionada à kava, discute os possíveis mecanismos responsáveis pela hepatotoxicidade potencialmente grave e descreve alguns aspectos que devem ser considerados quando eventos adversos hepáticos pareçam ser relacionados à administração dessa substância. Conclui-se que a possível toxicidade hepática pela kava ainda deve ser investigada e que algumas medidas antes e durante o seu uso são importantes, dada a possibilidade de disfunção hepática grave. Unitermos:Piper methysticum, Piperaceae, kava, hepatite tóxica. ABSTRACT:Kava is an anxiolytic herbal medicine used in the treatment of sleep and anxiety disorders. Some cases of kava-induced hepatotoxicity have been reported in the literature leading to its banishment in most countries worldwide. Clinically, the spectrum ranged from transient elevations of liver enzyme levels to fulminant liver failure and death. Liver transplantation was performed in a few cases. This paper provides a review of the currently available literature on kava-related toxic hepatitis which may result from its use, discusses the possible mechanisms for the potentially severe hepatotoxicity and describes some features which must be considered when adverse liver effects seem to be associated to kava administration. In conclusion, the incidence of kava toxicity on the liver remains to be investigated; however, some concerns before or during kava use are important, due to the possibility of severe liver dysfunction.
Trachylobane-360 (ent-7α-acetoxytrachyloban-18-oic acid) was isolated from Xylopia langsdorffiana. Studies have shown that it has weak cytotoxic activity against tumor and non-tumor cells. This study investigated the in vitro and in vivo antitumor effects of trachylobane-360, as well as its cytotoxicity in mouse erythrocytes. In order to evaluate the in vivo toxicological aspects related to trachylobane-360 administration, hematological, biochemical and histopathological analyses of the treated animals were performed. The compound exhibited a concentration-dependent effect in inducing hemolysis with HC50 of 273.6 µM, and a moderate in vitro concentration-dependent inhibitory effect on the proliferation of sarcoma 180 cells with IC50 values of 150.8 µM and 150.4 µM, evaluated by the trypan blue exclusion test and MTT reduction assay, respectively. The in vivo inhibition rates of sarcoma 180 tumor development were 45.60, 71.99 and 80.06% at doses of 12.5 and 25 mg/kg of trachylobane-360 and 25 mg/kg of 5-FU, respectively. Biochemical parameters were not altered. Leukopenia was observed after 5-FU treatment, but this effect was not seen with trachylobane-360 treatment. The histopathological analysis of liver and kidney showed that both organs were mildly affected by trachylobane-360 treatment. Trachylobane-360 showed no immunosuppressive effect. In conclusion, these data reinforce the anticancer potential of this natural diterpene.
RESUMO: "Avaliação da toxicidade e atividade antiulcerogênica do extrato etanólico das folhas de Maytenus obtusifolia Mart." Maytenus obtusifolia é utilizada na medicina popular para o tratamento de úlceras graves, infl amações gerais e câncer. Apesar da importância etnofarmacológica desta espécie, nenhum estudo foi realizado para avaliar a sua toxicidade e atividade antiulcerogênica. Neste estudo, nós avaliamos a toxicidade e propriedade antiulcera do extrato etanólico das folhas de Maytenus obtusifolia (MO-EtOH). O MO-EtOH (10-1000 g/mL) mostrou baixa toxicidade para as larvas de A. salina com CL 50 maior que 1000 g/mL. O MOEtOH (2000 mg/kg, p.o.) não alterou o peso corporal e peso dos órgãos dos camundongos, mas foi observado um aumento no consumo de água dos machos e uma diminuição do consumo alimentar das fêmeas. Durante o estudo não foram observadas mortes e nem alterações macroscópicas nos órgãos dos camundongos. 5, 125, 250 e 500 mg/kg) e lansoprazol (30 mg/kg) reduziram signifi cativamente o índice ulcerativo para 65,58 8,74, 43,00 9,53, 15,50 7,56, 54,75 8,88 ABSTRACT:Maytenus obtusifolia is used in folk medicine for the treatment of serious ulcers, general infl ammations and cancer. Despite of the ethnopharmacological importance of this species, no study was conducted to evaluate its toxicity and antiulcerogenic activity. In this study, we evaluated the toxicity and antiulcerogenic property of the ethanol extract of the leaves of Maytenus obtusifolia (MO-EtOH). The MO-EtOH (10-1000 g/mL) showed low toxicity for larvae of A. salina with LC 50 higher than 1000 g/mL. The MO-EtOH (2000 mg/kg, p.o.) did not change the body and organs weight of the mice, but it was observed an increase in the water consumption of males and a decrease in the food consumption of females. During the study no deaths and no macroscopic changes in the organs were observed in the mice. 125, 250 and 500 mg/kg) and lansoprazole (30 mg/kg) signifi cantly reduced the ulcerative index for 65.58 8.74, 43.00 9.53, 15.50 7.56, 54.75 8.88 and 36.13 9.55, respectively, in comparison with saline 82.13 12.48. In conclusion, the MO-EtOH showed low toxicity and antiulcerogenic activity, confi rming the popular use of M. obtusifolia.
The chemical composition, antitumor activity and toxicity of the essential oil from Lippia microphylla leaves (OEL) were investigated. The major constituents were thymol (46.5%), carvacrol (31.7%), p-cymene (9%), and γ-terpinene (2.9%). To evaluate the toxicity of OEL in non-tumor cells, the hemolytic assay with Swiss mice erythrocytes was performed. The concentration producing 50% hemolysis (HC50) was 300 μg/mL. Sarcoma 180 tumor growth was inhibited in vivo 38% at 50 mg/kg, and 60% at 100 mg/kg, whereas 5-FU at 50 mg/kg caused 86% inhibition. OEL displays moderate gastrointestinal and hematological toxicity along with causing some alteration in liver function and morphology. However, the changes were considered reversible and negligible in comparison to the effects of several anticancer drugs. In summary, OEL displays in vivo antitumor activity and a moderate toxicity, which suggests further pharmacological study.
BackgroundThe essential oil from Mesosphaerum sidifolium (L’Hérit.) Harley & J.F.B.Pastore (syn. Hyptis umbrosa), Lamiaceae (EOM), and its major component, have been tested for toxicity and antitumor activity.MethodsEOM was obtained from aerial parts of M. sidifolium subjected to hydro distillation, and gas chromatography-mass spectrometry was used to characterize the EOM chemical composition. The toxicity was evaluated using haemolysis assay, and acute toxicity and micronucleus tests. Ehrlich ascites carcinoma model was used to evaluate the in vivo antitumor activity and toxicity of EOM (50, 100 and 150 mg/kg), and fenchone (30 and 60 mg/kg) after 9 d of treatment.ResultsThe EOM major components were fenchone (24.8%), cubebol (6.9%), limonene (5.4%), spathulenol (4.5%), β-caryophyllene (4.6%) and α-cadinol (4.7%). The HC50 (concentration producing 50% haemolysis) was 494.9 μg/mL for EOM and higher than 3000 μg/mL for fenchone. The LD50 for EOM was approximately 500 mg/kg in mice. The essential oil induced increase of micronucleated erythrocytes only at 300 mg/kg, suggesting moderate genotoxicity. EOM (100 or 150 mg/kg) and fenchone (60 mg/kg) reduced all analyzed parameters (tumor volume and mass, and total viable cancer cells). Survival also increased for the treated animals with EOM and fenchone. For EOM 150 mg/kg and 5-FU treatment, most cells were arrested in the G0/G1 phase, whereas for fenchone, cells arrested in the S phase, which represents a blockage in cell cycle progression. Regarding the toxicological evaluation, EOM induced weight loss, but did not induce hematological, biochemical or histological (liver and kidneys) toxicity. Fenchone induced decrease of AST and ALT, suggesting liver damage.ConclusionsThe data showed EOM caused in vivo cell growth inhibition on Ehrlich ascites carcinoma model by inducing cell cycle arrest, without major changes in the toxicity parameters evaluated. In addition, this activity was associated with the presence of fenchone, its major component.
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