ABSTRACT
Fractionation of the EtOH extract from aerial parts of Baccharis uncinella C. DC. (Asteraceae) led to isolation of caffeic and ferulic acids, which were identified from spectroscopic and spectrometric evidence. These compounds exhibit antioxidant and anti-inflammatory properties and have been shown to be effective in the prevention/treatment of metabolic syndrome. This study investigated whether the combined treatment of caffeic and ferulic acids exhibits a more significant beneficial effect in a mouse model with metabolic syndrome. The combination treatment with caffeic and ferulic acids was tested for 60 days in C57 mice kept on a high-fat (40%) diet. The data obtained indicated that treatment with caffeic and ferulic acids prevented gain in body weight induced by the high-fat diet and improved hyperglycemia, hypercholesterolemia and hypertriglyceridemia. The expression of a number of metabolically relevant genes was affected in the liver of these animals, showing that caffeic and ferulic acid treatment results in increased cholesterol uptake and reduced hepatic triglyceride synthesis in the liver, which is a likely explanation for the prevention of hepatic steatosis. In conclusion, the combined treatment of caffeic and ferulic acids displayed major positive effects towards prevention of multiple aspects of the metabolic syndrome and liver steatosis in an obese mouse model.
Subject(s)
Animals , Male , Baccharis/chemistry , Caffeic Acids/administration & dosage , Coumaric Acids/administration & dosage , Metabolic Syndrome/prevention & control , Protective Agents/administration & dosage , Caffeic Acids/chemistry , Cholesterol/metabolism , Coumaric Acids/chemistry , Diet, High-Fat/adverse effects , Drug Therapy, Combination/methods , Fatty Liver/metabolism , Fatty Liver/pathology , Metabolic Syndrome/drug therapy , Mice, Inbred C57BL , Models, Animal , Protective Agents/chemistry , Triglycerides/metabolismABSTRACT
ABSTRACT: he Lantana camara L. belongs to the family Verbenaceae, which contains several active compounds in leaves and roots and which are reported to have medicinal and insecticidal properties. Studies of plants within the same family show the existence of anti-inflammatory activity in paw edema induced by carrageenan, serotonin and histamine and analgesic activity in the acetic acid writhing and tail-flick tests. The present study investigated whether the L. camara extract (ACE) also exerts these effects. The ACE toxicity was studied in male mice, and the percentage of mortality recorded 7 days after treatment was assessed. The ACE was evaluated as an antinociceptive agent in the hot plate, tail-flick and acetic acid writhing tests at a nontoxic dose of 1.0 g/Kg. The results showed that 1.5 g/Kg of ACE was not able to cause death, and doses of 3.0 and 4.0 g/Kg caused 50% and 60% death, respectively, in male mice. In all of the antinociceptive tests, 1 g/Kg of ACE markedly reduced responses to pain. Our findings suggest that ACE may have active anti-inflammatory and antinociceptive properties in much smaller doses than toxic.
RESUMO: Lantana camara L. pertence à família Verbenaceae, a qual contem muitos princípios ativos em suas folhas e raízes com propriedade medicinais e inseticidas. Estudos com plantas da mesma família mostram a existência de propriedades antinflamatórias no modelo de edema de pata induzido pela carragenina, serotonina e histamina, além da atividade analgésica nos testes de contorção induzida pelo ácido acético e da retirada da cauda por estímulo térmico. O presente trabalho investigou os efeitos tóxicos e antinociceptivos do extrato de L. camara (ACE) em camundongos. Para tanto, investigou-se a porcentagem de mortes em 7 dias após a administração de diferentes doses do extrato. Avaliou-se também os efeitos antinociceptivos do ACE pelos testes da placa quente, estimulação térmica da cauda e contorções abdominais induzidas pelo ácido acético com a dose não-tóxica [1,0 g/Kg]. Os resultados mostraram que 1,5 g/Kg do ACE não causou mortalidade, enquanto que 3,0 e 4,0 g/Kg promoveram 50 e 60% de mortalidade, respectivamente. Em todos os testes antinociceptivos, a dose de 1,0 g/Kg do ACE reduziu a resposta à dor. Os presentes resultados indicam que o ACE apresenta propriedades antinflamatórias e analgésicas em doses muito menores que a tóxica.
Subject(s)
Animals , Male , Mice , Lantana/anatomy & histology , Analgesics/adverse effects , Mice/classification , Toxicity/analysis , Anti-Inflammatory Agents/pharmacologyABSTRACT
RESUMO Hypericum cordatum é uma espécie do cerrado que foi selecionada em triagem de plantas com atividade fungitóxica. O objetivo do presente trabalho foi isolar e identificar compostos com atividade antifúngica em extratos de folhas em diclorometano. O pó das folhas das plantas foi submetido à extração exaustiva com éter de petróleo e diclorometano. O extrato em diclorometano, e as frações ativas, foram submetidos à fracionamentos biomonitorados em coluna de Sephadex LH-20, respectivamente, com os eluentes clorofórmio:metanol (1:1) e com um gradiente de hexano:diclorometano (1:4); diclorometano:acetona (3:2 e 1:4), metanol, e água. As frações que mostraram atividade foram submetidas à cromatografia em camada delgada preparativa de sílica gel GF254, sendo que o material de maior massa foi analisado em CLAE semipreparativa. A fração ativa foi analisada por RMN de 1H, tendo sido identificado o aloaromadendrano - 4α -10ß - diol como componente principal da fração. Conclui-se, portanto, que este é um dos compostos responsáveis pela atividade fungitóxica de Hypericum cordatum.
The Hypericum cordatum is a species of the Brazilian Cerrado that was selected in a screening of plants with fungitoxic activities. The aim of this work was to isolate and identify the compounds with antifungal activity in leaf extracts in dichloromethane. For this end, the powder made from the leaves of the plants was submitted to exhaustive extraction with petroleum ether and dichloromethane. The extract in dichloromethane and the active fractions were submitted to bioassay-guided fractionation in Sephadex LH - 20 column, respectively, with the following eluents chloroform:methanol (1:1) and a gradient of hexane:dichlorometane (1:4); dichloromethane:acetone (3:3 and 1:4), methanol and water. Afterward, the fractions that showed some activity were submitted to preparative thin layer chromatography of silica gel GF254 and the material with the greatest mass was submitted to semi-preparative HPLC. The active fraction obtained was analyzed by 1H NMR, and the main component identified was alloaromadendrene-4α-10ß - diol. We may then conclude that this is one of the compounds responsible for the fungitoxic activity of Hypericum cordatum.