Antiulcerogenic and antioxidant activities of Baccharis trimera (Less) DC (Asteraceae)

A "carqueja", Baccharis trimera (Less) DC (Asteraceae), é uma espécie vegetal característica de regiões tropicais, muito utilizada na medicina popular como antiinflamatória, hipoglicemiante e em tratamento de problemas digestivos. A avaliação da atividade antiúlcera do extrato bruto liofilizado e do extrato liofilizado da "resina" (porção que durante a concentração dos extratos ficava depositada no fundo do recipiente com aspecto viscoso e pegajoso) foi realizada através de indução aguda por etanol acidificado. O extrato bruto liofilizado, na dose de 400 mg/ kg, reduziu a área de lesão em 90%, 200 mg/kg, 87%, 100 mg/kg, 66% e o fármaco controle (lansoprazol), 66%. O extrato liofilizado da "resina", administrado na dose de 400 mg/kg, reduziu a área de lesão em 82%, 200 mg/kg, 82%, 100 mg/kg, 53% e o fármaco controle (lansoprazol), 70%. A atividade antioxidante foi ensaiada com extrato bruto liofilizado, extrato liofilizado da "resina", pó da droga e frações clorofórmica, acetato de etila, etanol e etanol 50% através do método que reduz o radical 2,2'-difenil-1-picril-hidrazil (DPPH), permitindo após o equilíbrio da reação, calcular a quantidade de antioxidante gasta para reduzir 50% do DPPH, apresentando resultado evidente, comparado à vitamina E. Não foram verificados sinais de alteração aparente no ensaio de toxicidade na dose única de 5g/kg, em camundongos.Baccharis trimera (Less) DC (Asteraceae) is a medicinal Brazilian plant well-known by "carqueja". Natural from tropical regions, used as home-made medicine as anti-inflammatory, hypoglycemiant and for the treatment of digestive problems. The evaluation of the antiulcer activity of the extract and the "resin" (portion which during the extracts concentration was settled at the bottom of the recipient, showing a viscous and clammy aspect), was accomplished through the acute induction by acidified ethanol. The lyophilized extract, at a dose of 400 mg/kg, reduced the lesion area at 90%; 200 mg/kg, at 87%; 100 mg/kg, at 66%; and the control (lansoprazol) at 66%. The "resin" administered at the 400 mg/kg dose reduced the lesion area at 82%; 200 mg/kg, at 82%, 100 mg/kg, at 53% and the control (lansoprazol), at 70%. The antioxidant activity of the lyophilized extract, of the "resin" of the powdered drug, of the chloroform, ethyl acetate, ethanol and 50% ethanol fractions was tested following the method which reduces the 2,2-dipheny l-1 -picrylhydrazyl (DPPH) radical, permitting after the reaction balance, to calculate the amount of antioxidant spent to reduce 50% of the DPPH. The result was meaningful, when compared with the vitamin E result. The acute toxicity test performed in mice showed no apparent alteration

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids

Study of the gastroprotective action and healing effects of Kalanchoe pinnata (Lam.) against acidified ethanol- and acetic acid-induced gastric ulcers in rats / Estudo da acção gastroprotectora e dos efeitos curativos de Kalanchoe pinnata (Lam.) contra úlceras gástricas induzidas por etanol acidificado e ácido acético em ratos

Kalanchoe pinnata (Lam.) Pers. (Crassulaceae) is a commonly used species in traditional medicine in Brazil for the treatment of various diseases, including gastric ulcers. This research aims to evaluate the antiulcer aspects of Kalanchoe pinnata leaves. The LD50 value of the hydroethanolic extract (HE) of K. pinnata was 1341.46 mg/kg, after the in vitro cytotoxicity assay. In the phytochemical analysis, several flavonoids were identified in the HE and ethyl acetate fraction (EAF) of K. pinnata. It was verified that the gastroprotective activity of the HE of K. pinnata involved prostaglandins and sulfhydryl compounds. However, the mechanism of gastroprotection of the EAF of K. pinnata is dependent on prostaglandins and nitric oxide. The ulcer healing activity of the HE of K. pinnata was also evaluated. According to the macroscopic results, doses of 200 mg/kg and 400 mg/kg reduced the injury area, with rates of 33% and 39%, respectively, after 7 days of treatment (p <0.05). Histological analysis showed regeneration of the gastric mucosa and re-establishment of the glandular architecture in groups treated with the HE (200 and 400 mg/kg). Antioxidant enzymes (CAT, SOD and GPx) were evaluated in the mechanism of gastric ulcer healing. The results showed that the antiulcerogenic activity was mediated by SOD. The anti-Helicobacter pylori activity was also evaluated; however, the HE did not show anti-H. pylori activity. Analysis of the results suggests that K. pinnata has therapeutic potential against gastric ulcers and that the flavonoids may be linked to the biological effects

Pharmacology and phytochemistry of extracts and formulations from Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L.

Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. e Piper umbellatum L. são plantas nativas do Brasil, presentes no estado de São Paulo, com relatos de uso popular para atividade antiúlcera. Este trabalho teve como objetivo avaliar a atividade antiúlcera de J. caroba, J. decurrens e formulações de nanocápsulas contendo P. umbellatum. Também pretendeu-se caracterizar a fitoquímica de tais formulações e extratos. Adicionalmente, foi avaliada a toxicidade aguda e subaguda de J. caroba. Os extratos de Jacaranda apresentaram compostos fenólicos em seus perfis cromatográficos obtidos por CCD e CLAE, característicos para cada espécie. Os diferentes extratos de J. caroba variaram sua composição química conforme a procedência e idade da planta. As espécies J. decurrens e J. caroba de três diferentes regiões não apresentaram ação antiúlcera aguda em ratos em modelo de indução por etanol acidificado, embora o extrato e as frações de J. caroba apresentaram potencial atividade anti Helicobacter pylori, com CIM variando entre 125 e 1.000 µg/mL. O extrato de J. caroba não promoveu sintomas de toxicidade aguda e subaguda em ratos. A DL50 observada foi maior que 5.000 mg/kg. Não foram relatadas alterações significativas na aparência macroscópica e peso dos órgãos, porém houve indicação de atividade mutagênica em teste de Ames na linhagem TA98 de S. typhimurium, o qual apresentou uma tendência dose-resposta para concentrações entre 7,5 e 15,0 mg/placa após ativação metabólica (S9). A formulação de nanocápsulas de poli-ε- caprolactona com extrato de P. umbellatum apresentou partículas com diâmetro médio de 181,6 ± 0,9 nm e potencial zeta de -31 ± 4 mV. Através de análise por CLAE observou-se maior eficiência de encapsulamento para a porção mais apolar da fração, enquanto que os compostos mais polares ficaram dispersos no meio. As nanocápsulas poliméricas apresentaram atividade gastroprotetora mesmo sem a adição de ativos e tiveram sua atividade aumentada pela fração clorofórmica de P. umbellatum.Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L. are native plants in Brazil, present in the state of São Paulo, with popular usage reports for anti-ulcer activity. This study aimed to evaluate the anti-ulcer activity of J. caroba, J. decurrens and nanocapsules formulations containing P. umbellatum. Also, we intended to characterize the phytochemistry of such formulations and extracts. Additionally, we evaluated the acute and subacute toxicity of J. caroba. Extracts from Jacaranda presented phenolic compounds in their chromatographic profiles obtained by TLC and HPLC, with variations between species. Samples of J. caroba extracts showed different chemical composition according to the origin and age of the plant. The species J. decurrens and J. caroba from three different regions showed no acute anti-ulcer action when tested in rats by acidified ethanol induction model. However, extract and fractions from J. caroba showed potential anti Helicobacter pylori activity, with MIC ranging from 125 and 1,000 ug/mL. J. caroba extract did not cause symptoms of acute and subacute toxicity in rats. The DL50 was determined above 5,000 mg/kg. Also, there were no significant changes to the macroscopic appearance of organs or changes in their weights. Meanwhile, an indication of mutagenic activity was observed in the Ames test. The TA98 strain of S. typhimurium, showed a tendency of dose-response for concentrations between 7.5 and 15.0 mg/plate after metabolic activation (S9). The nanocapsules formulation of poly-ε-caprolactone containing P. umbellatum extract had an average particle diameter of 181.6 ± 0.9 nm and zeta potential of -31 ± 4 mV. HPLC analysis showed better entrapping efficiency for the more apolar portion of the fraction, while the more polar compounds were dispersed in the medium. The polymeric nanocapsules showed gastroprotective activity even without the addition of active molecules and had their activity increased by chloroform fraction of P. umbellatum

Antiulcer directed phamacology and phytochemistry of Pothomorphe umbellata (L.) Miq. extracts

Este trabalho aborda a espécie Pothomorphe umbellata (L.) Miq. (Piperaceae), conhecida popularmente como pariparoba. Nos últimos anos foram atribuídas diversas atividades a essa espécie, entre elas uma potente atividade antioxidante, atividade anti-inflamatória e ainda inibição in vitro do crescimento de Helicobacter pylori. Tais estudos tornam interessante a investigação da atividade antiúlcera e dos principais grupos de compostos que possam ser relacionados à esta ação, sendo estes os principais objetivos do trabalho. Para cumprir os objetivos propostos, foram utilizados diferentes modelos de ulceração gástrica em animais. Em modelo de indução por etanol acidificado, extratos brutos de folhas e raízes não inibiram significativamente a formação de lesões, porém frações do extrato de raízes conseguiram desempenho semelhante ao do lansoprazol. Em modelo de ligadura do piloro e indução por indometacina o extrato bruto de raízes (EB) não mostrou diferença em relação ao controle negativo. Em modelo de indução por ácido acético, o EB reduziu o tamanho, a presença de necrose e infiltrado inflamatório nas lesões. Com os resultados obtidos, é proposto que sua atividade esteja relacionada à capacidade antioxidante já relatada na literatura. Através de análise e separação por CLAE, foram identificadas três moléculas na fração mais ativa em relação à ação antiúlcera. Duas delas (piperumbellactamas A e B) já haviam sido descritas nessa espécie, porém nas partes aéreas. A terceira (caldensina) havia sido isolada de Piper caldense, e não foram encontrados na literatura relatos de sua ocorrência em P. umbellata. Para melhorar a solubilidade do extrato em água, foi preparada uma suspensão de nanocápsulas, que associou as substâncias mais apolares com sua matriz polimérica. Ao mesmo tempo, formou partículas de tamanho e índice de polidispersão adequados, indicando a viabilidade da formulação.This work is based on a research of Pothomorphe umbellata (L.) Miq. (Piperaceae) extracts, popularly known as pariparoba. Through the past years, many activities have been attributed to this species, including strong antioxidant activity, anti-inflammatory effect and in vitro growth inhibition of Helicobacter pylori. On that account, the investigation of the antiulcer activity and the research for related chemical compounds was proposed, trying to establish a relationship between these compounds and the activity. To accomplish the proposal, some distinct ulcer models (in rats) were used. The crude extracts from leaves and roots had no significant effect over mucosal damage when tested in acidified ethanol model. By contrast, some fractions from the roots extract showed similar performance when compared to lansoprazole. Also, the crude extract from roots (CE) was not different from water when tested in pylorus ligation and indomethacin induction models. When tested in acetic acid model, the CE significantly reduced the lesion area, the presence of necrosis and inflammatory infiltrate. With these results, a correlation between the antioxidant (previously reported) and antiulcer activities is suggested. The chemical analysis was performed through high-performance liquid chromatography (HPLC) and three molecules were identified in the fraction which showed the stronger antiulcer activity. Two of them (piperumbellactam A and B) had been described in branches of this species. The third (caldensin) had been isolated from Piper caldense, and no record was found about its occurence in P. umbellata. In order to increase CE water solubility, a nanoparticles suspension was prepared. This formulation was able to associate the hydrophobic components to its polymeric matrix. At the same time, it exhibited adequate particle size and polydispersity index, indicating a viability of the formulation

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids