Combined treatment with caffeic and ferulic acid from Baccharis uncinella C. DC. (Asteraceae) protects against metabolic syndrome in mice

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.

Combined treatment with caffeic and ferulic acid from Baccharis uncinella C. DC. (Asteraceae) protects against metabolic syndrome in mice.

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.

Antinociceptive and anti-inflammatory effects of Lantana camara L. extract in mice / Efeitos antinociceptivos do extrato de Lantana camara L. em camundongos

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.

Anti-malarial, anti-trypanosomal, and anti-leishmanialactivities of jacaranone isolated from Pentacalia desiderabilis(Vell.) Cuatrec. (Asteraceae)

Leishmaniasis, Chagas disease, and malaria affectthe poorest population around the world, with an elevatedmortality and morbidity. In addition, the therapeutic alternativesare usually toxic or ineffective drugs especially thoseagainst the trypanosomatids. In the course of selection of newanti-protozoal compounds from Brazilian flora, the CH2Cl2phase from MeOH extract obtained from the leaves ofPentacalia desiderabilis (Vell.) Cuatrec. (Asteraceae)showed in vitro anti-leishmanial, anti-malarial, and antitrypanosomalactivities. The chromatographic fractionationof the CH2Cl2 phase led to the isolation of thebioactive compound, which was characterized as jacaranone[methyl (1-hydroxy-4-oxo-2,5-cyclohexandienyl)acetate], by spectroscopic methods. This compoundshowed activity against promastigotes of Leishmania (L.)chagasi, Leishmania (V.) braziliensis, and Leishmania(L.). amazonensis showing an IC50 of 17.22, 12.93, and11.86 μg/mL, respectively. Jacaranone was also tested invitro against the Trypanosoma cruzi trypomastigotes andPlasmodium falciparum chloroquine-resistant parasites(K1 strain) showing an IC50 of 13 and 7.82 μg/mL,respectively, and was 3.5-fold more effective than benznidazolein anti-Trypanosoma cruzi assay. However, despiteof the potential against promatigotes forms, this compoundwas not effective against amastigotes of L. (L.) chagasiand T. cruzi. The cytotoxicity study using Kidney Rhesusmonkey cells, demonstrated that jacaranone showedselectivity against P. falciparum (21.75 μg/mL) and aselectivity index of 3. The obtained results suggested thatjacaranone, as other similar secondary metabolites orsynthetic analogs, might be useful tolls for drug designfor in vivo studies against protozoan diseases...

Toxicity of apolar and polar Lantana camara L. crude extracts in mice.

Lantana camara L, widely used in folk medicine, presents toxicity for farm animals. The acute poisoning effects of the apolar and polar L. camara L. extracts in mice were done. The percentage of death during 7 days after treatment, the acute signs of toxicity as well as the general activity observed in open field were assessed. The extracts were administered by i.p. route at 1.5, 3.0 and 5.0 g/kg. Animals were evaluated during the first 2 h after the treatments to assess the acute signs of toxicity and daily observations were done for the presence of death. In the end of the experiment, at day 7, or immediately after death the animals had their organs removed, weighted and observed for macroscopic alterations. (1)H NMR and TLC analysis suggest the presence of triterpenoids in the apolar phase but not in the polar phase. Results showed also that both extracts produced similar percentage of death, mainly after 2 days of treatment; only the apolar extract presented a dose-dependent increased lethality. At necropsy, mice treated by both apolar and polar extracts were severely icteric, dehydrated and constipated, with hepatosis, showed congested heart and lung, and nephrosis; no skin lesions were shown. The main signs of toxicity revealed a decreased spontaneous general activity. In addition, it was observed a decreased duration of locomotion and animal rearing parallel to an increased immobility in the open field. The similarity of the signs related to the acute toxicity for both apolar and polar extracts suggested that the extracts have some of the active toxic principles in common. Data from open field behavior and spontaneous signs of toxicity suggest that the toxic principles have depressive properties on central nervous system.

Flavonoids as chemotaxonomic markers for Asteraceae.

Flavonoids have been shown to be good taxonomic markers for Asteraceae. More than 800 compounds comprising 4700 flavonoid occurrences were included in a computational system specially made for chemotaxonomic purposes. Some implications of flavonols, flavones and other types as well as structural features of them are discussed for tribes and subtribes of Asteraceae.