Anti-Inflammatory and Chemopreventive Effects of Bryophyllum pinnatum (Lamarck) Leaf Extract in Experimental Colitis Models in Rodents

Inflammatory bowel diseases, mainly ulcerative colitis and Crohn’s disease are characterized by chronic inflammation in the intestine. Currently several therapeutic strategies available to treat inflammatory bowel diseases. Though, most treatments can be associated with serious adverse effects what justifies the search for new treatments. In this sense, we highlight the interest in herbal products rich in bioactive compounds which immunomodulatory and antioxidant properties as is the case of Bryophyllum pinnatum (Crassulaceae). This plant is used in traditional medicine in Brazil for treating inflammatory diseases. We hypothesized that hydroethanolic B. pinnatum leaf extract has intestinal anti-inflammatory effects on two experimental colitis models: 2.4-dinitrobenzene sulfonic acid (DNBS) in rats, and dextran sulfate sodium (DSS) in mice. Ultra-fast liquid chromatography method used for the quantification of the main compounds indicated good linearity, specificity, selectivity, precision, robustness and accuracy. The major flavonoids (mg/g of the extract) quantified were: quercetin 3-O-a-L-arabinopyranosyl-(1!2)-a-L-rhamnopyranoside (35.56 ± 0.086 mg/g), kaempferol 3-O-a-L-arabinopyranosyl-(1!2)-a-L-rhamnopyranoside (4.66 ± 0.076 mg/g) and quercetin-3-O-rhamnopyranoside (4.56 ± 0.026 mg/g). The results obtained in the DNBS and DSS models indicate that extract has both chemopreventive and antiinflammatory effects, observing a significant reduction in the disease activity index score, and less macroscopic and microscopic damage. The extract promoted downregulation of Tolllike receptor and kappa B p65 nuclear factor gene expression, leading to a reduction in pro-inflammatory and oxidative mediators, chemokines, and cell adhesion molecules. This immunomodulatory property was proposed that one of the possible action mechanisms of extract. An improvement in intestinal damage was also associated with a reduction in oxidative stress and infiltration of leukocytes, as evidenced by the reduction in malonaldialdehyde and myeloperoxidase activity and increase in total glutathione in the colonic tissue. Moreover, the extract improved the cytoarchitecture of the colonic tissue and the integrity of the intestinal epithelial barrier by restoring the expression of the proteins associated with mucosa protection. In view of the beneficial effects showed by the B. pinnatum leaf extract in preclinical rodent models of colitis there is the potential to conduct some future clinical studies to ensure safe and effective development of a phytotherapeutic treatment for human inflammatory bowel diseases.CAPESJunta de Andalucia CTS 164Spanish Ministry of Economy and Competitiveness AGL2015-67995-C3-3-REuropean Union (EU)Instituto de Salud Carlos II

AGATISFLAVONA, UM BIFLAVONOIDE COM APLICAÇÕES FARMACOLÓGICAS PARA O SISTEMA NERVOSO CENTRAL: REVISÃO

Os compostos fenólicos formam uma das principais classes de metabólitos secundários sintetizados por plantas e, entre estes, é possível destacar os flavonoides. Os biflavonoides, uma das classes de flavonoides, possuem diversas propriedades biológicas inerentes ao grupo, como antioxidante, anti-inflamatória, antitumoral, dentre outras. A agatisflavona é um biflavonoide que demonstrou, em estudos anteriores, in vitro e in vivo, atividades: neuroprotetora e antiepiléptica. O objetivo desta pesquisa foi realizar uma prospecção científica e tecnológica sobre o biflavonoide agatisflavona e suas aplicações farmacêuticas em algumas patologias relacionadas ao Sistema Nervoso Central (SNC). O EndNote-X5 software foi utilizado como referência, com as palavras-chave: agatisflavona, antioxidante, ansiolítico, neuroprotetor, antidepressivo e suas correlações em Inglês e Português. Foram utilizados documentos publicados nos bancos de dados PubMed, Science Direct, Scopus, Periódicos da Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Web of Science e American Chemical Society Publications, no Banco Europeu de Patentes, da Organização Mundial de Propriedade Intelectual, no Banco Americano de Marcas e Patentes e do Instituto Nacional de Propriedade Industrial do Brasil. Do ponto de vista científico, a agatisflavona apresenta um extenso número de publicações no que se refere à suas atividades farmacológicas (antimicrobiana, antivirais, anticarcinogênica) e se destaca como composto potencialmente ativo sobre o SNC (neurogênese e diminuição da excitabilidade do SNC). Porém, não foram verificados depósitos de patentes que correlacionam o biflavonoide agatisflavona a desordens neurológicas. Este fato, por sua vez, permite o desenvolvimento de pesquisas inovadoras referentes às ações farmacológicas da agatisflavona, em especial ao SNC

Avaliação da rotulagem e qualidade de diferentes marcas de cerveja tipo pilsen

A cerveja tipo caracteriza-se pela sua refrescância, leveza, amargor e baixo teor alcoólico. Sua qualidade está constantemente associada à satisfação do consumidor. Este estudo buscou verificar o cumprimento das determinações estabelecidas pela legislação brasileira no seguimento cervejeiro. Investigaram-se os parâmetros físico-químicos de seis marcas de cervejas do tipo Pilsen e as informações presentes na rotulagem. Os resultados obtidos demostraram que todas as marcas estudadas apresentaram em seus rótulos os itens obrigatórios, exceto a Marca D. Admitiu-se que houve diferença significativa (p < 0,05) de alguns parâmetros com as especificações previstas na legislação e descritas na rotulagem. Dentro das condições experimentais deste trabalho, concluiu-se que as empresas cervejeiras cumprem as determinações estabelecidas pela legislação brasileira, quanto à rotulagem, exceto as que produzem a Marca D. As marcas A, B, D e E não atenderam alguns dos parâmetros físico-químicos analisados, apresentando desvio na qualidade

In vitro antioxidant properties of the biflavonoid agathisflavone

Abstract Purpose Free radicals are considered as the causative agents of a variety of acute and chronic pathologies. Natural antioxidants have drawn attention of the researchers in recent years for their ability to scavenge free radicals with minimal or even no side effects. This study evaluates the antioxidant capacity of agathisflavone, a naturally occurring biflavonoid by a number of in vitro methods. Methods Agathisflavone was subjected to DPPH, ABTS, OH and NO radical scavenging assay, reducing potential and inhibition of lipid peroxidation (TBARS) test using trolox as a standard. Results Agathisflavone showed concentration-dependent antioxidant activity against all types of free radicals used in this study. The antioxidant capacity, reducing potential and inhibition of lipid peroxidation showed by agathisflavone were comparable to that of trolox. Conclusion Agathisflavone exhibited antioxidant capacity, which suggests considering this biflavonoid for the use in the prevention and/or treatment of diseases precipitated by oxidative stress

Anti-Inflammatory and Chemopreventive Effects of Bryophyllum pinnatum (Lamarck) Leaf Extract in Experimental Colitis Models in Rodents.

Inflammatory bowel diseases, mainly ulcerative colitis and Crohn's disease are characterized by chronic inflammation in the intestine. Currently several therapeutic strategies available to treat inflammatory bowel diseases. Though, most treatments can be associated with serious adverse effects what justifies the search for new treatments. In this sense, we highlight the interest in herbal products rich in bioactive compounds which immunomodulatory and antioxidant properties as is the case of Bryophyllum pinnatum (Crassulaceae). This plant is used in traditional medicine in Brazil for treating inflammatory diseases. We hypothesized that hydroethanolic B. pinnatum leaf extract has intestinal anti-inflammatory effects on two experimental colitis models: 2.4-dinitrobenzene sulfonic acid (DNBS) in rats, and dextran sulfate sodium (DSS) in mice. Ultra-fast liquid chromatography method used for the quantification of the main compounds indicated good linearity, specificity, selectivity, precision, robustness and accuracy. The major flavonoids (mg/g of the extract) quantified were: quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside (35.56 ± 0.086 mg/g), kaempferol 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside (4.66 ± 0.076 mg/g) and quercetin-3-O-rhamnopyranoside (4.56 ± 0.026 mg/g). The results obtained in the DNBS and DSS models indicate that extract has both chemopreventive and anti-inflammatory effects, observing a significant reduction in the disease activity index score, and less macroscopic and microscopic damage. The extract promoted downregulation of Toll-like receptor and kappa B p65 nuclear factor gene expression, leading to a reduction in pro-inflammatory and oxidative mediators, chemokines, and cell adhesion molecules. This immunomodulatory property was proposed that one of the possible action mechanisms of extract. An improvement in intestinal damage was also associated with a reduction in oxidative stress and infiltration of leukocytes, as evidenced by the reduction in malonaldialdehyde and myeloperoxidase activity and increase in total glutathione in the colonic tissue. Moreover, the extract improved the cytoarchitecture of the colonic tissue and the integrity of the intestinal epithelial barrier by restoring the expression of the proteins associated with mucosa protection. In view of the beneficial effects showed by the B. pinnatum leaf extract in preclinical rodent models of colitis there is the potential to conduct some future clinical studies to ensure safe and effective development of a phytotherapeutic treatment for human inflammatory bowel diseases

Toxicity and Anti-Inflammatory Activity of Phenolic-Rich Extract from Nopalea cochenillifera (Cactaceae): A Preclinical Study on the Prevention of Inflammatory Bowel Diseases

Phenolic compounds have been scientifically recognized as beneficial to intestinal health. The cactus Nopalea cochenillifera, used as anti-inflammatory in traditional medicine, is a rich source of these bioactive compounds. The present study aimed to investigate the phytochemical profile of N. cochenillifera extract and evaluate its acute toxicity and anti-inflammatory effect on 2,4-dinitrobenzenesulfonic acid (DNBS)-induced colitis in rats. The total phenolic content per gram of dry extract was 67.85 mg. Through HPLC-IES-MSn, a total of 25 compounds such as saccharides, organic acids, phenolic acids and flavonoids were characterized. The dose of 2000 mg/kg of extract by an oral route showed no signs of toxicity, mortality or significant changes in biochemical and hematological parameters. Regarding intestinal anti-inflammatory effects, animals were treated with three different doses of extract or sulfasalazine. Macroscopic analysis of the colon indicated that the extract decreased the disease activity index. Levels of IL-1&beta; and TNF-&alpha; decreased, IL-10 increased and MDA and MPO enzyme levels decreased when compared with the control group. In addition, a down-regulation of MAPK1/ERK2 and NF-&kappa;B p65 pathway markers in colon tissue was observed. The epithelial integrity was improved according to histopathological and immunohistological analysis. Thus, the extract provided strong preclinical evidence of being effective in maintaining the remission of colitis