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 (CE 50 =41.91 µg/mL) by DPPH in comparison with Trolox ® and 11.33 mmol Trolox ® 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.Uniterms: Gastric ulcer/study/rats. Gastric ulcer/treatment. Kalanchoe pinnata/chromatographic profile. Kalanchoe pinnata/gastroprotective activity. Quercetrin. Quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside. INTRODUCTIONFor the past two centuries, peptic ulcers have caused high morbidity and mortality (Malfertheiner, Chan, Mccoll, 2009). This disease is a serious and prevalent pathology (Calam, Baron, 2001). A peptic ulcer is a chronic lesion, usually single, that can be located in the gastric or duodenal mucosae (Kumar, Abbas, Fausto, 2005). In the UK, the incidence of this disease was 12% higher in men than in women (Araujo, Borini, Guimarães, 2014). A review article (January 1980 to February 2009 showed that the incidence rate of uncomplicated peptic ulcers was approximately one case per 1000 people per year in the general population; the incidence rate for complicated peptic ulcers that included bleeding and perforation was approximately 0.7 cases per 1000 people per year (Lin, Rodrígues, Hernándes-Diaz, 2011).The pathophysiology of peptic ulcers suggests that this disease is caused by an imbalance between defensive factors (mucus and bicarbonate secretion, mucosal barrier, blood flow, and prostaglandins) and destructive factors (reactive oxygen species and acid and pepsin secretion), resulting in the acute inflammation of the gastrointestinal mucosae (Laine, Takeuchi, Tarnawski, 2008). Several stimuli serve as offensive factors, including Helicobacter pylori, the use of nonsteroidal anti-inflammatory drugs (NSAIDs), stress, alcohol and cigarette smoking (Malfertheiner, Chan, Mccoll, 2009;Malnick et al., 2014). The current medical treatment for peptic ulcers is generally based on proton pump inhibitors and histamine H 2 -receptor blockers (Jain et al., 2007). However, the long-term use of these therapeutic agents can produce adverse effects, such as hypergastrinemia and hyperplasia in the enterochromaffinlike (ECL) cells, the risk of pneumonia, diarrhea and the disturbance of ...
RESUMO: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. Unitermos:Baccharis trimera, carqueja, anti-inflamatório, hipoglicemiante, antiúlcera, problemas digestivos.ABSTRACT: "Antiulcerogenic and antioxidant activities of Baccharis trimera (Less) DC (Asteraceae)". 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-diphenyl-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.
It is well established in reconstructive surgery the repair of great bone defects is a difficult goal to be achieved. The aim of this study was to evaluate the influence of an extract rich in icariin on bone neoformation in critically sized defects in rat calvaria. Under continual saline irrigation, a circular bone defect was created in 40 rat calvarias with an 8-mm diameter trephine drill. Animals were randomly divided into a test group that received an Epimedium sagittatum extract (containing 5.8 mg/mL of icariin) and a control group that received an equal volume of saline solution. Substances were administered daily through a feeding tube until euthanasia. After 7, 14, 21, and 42 days, 5 animals from each group were euthanized. Calvaria defect samples were fixed in 10% formalin for 48 hours, X-rayed, and histologically processed. In the test group, there was a significant reduction in the bone defect area on X-ray images and an increase in new bone area in all of the experimental periods in the test group. At 42 days, the bone in the test group also exhibited a significant reduction in osteocyte (P = 0.002) and osteoclast density (P = 0.041). The authors conclude that administration of systemic Epimedium extracts containing high concentrations of icariin can induce bone neoformation and reduce osteocyte and osteoclast densities, thereby altering the normal deposition and remodeling patterns that are present in critically sized bone defects.
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