oleuropein and Colitis

The phenolic compounds present in olive leaves (Olea europaea L.) confer benefits to the human health.. To review the scientific literature about the benefits of the polyphenols of olive leaves to human health.. Literature review in the LILACS-BIREME, SciELO and MEDLINE databases for publications in English, Portuguese and Spanish with the descriptors "Olea europaea", "olive leaves", "olive leaf", "olive leaves extracts", "olive leaf extracts", "phenolic compounds", "polyphenols", "oleuropein", "chemical composition", and "health". There were identified 92 articles, but only 38 related to the objectives of the study and 9 articles cited in the works were included due to their relevance.. The phenolic compounds present in olive leaves, especially the oleuropein, are associated to antioxidant, antihypertensive, hypoglycemic, hypocholesterolemic and cardioprotective activity. Furthermore, studies associate the oleuropein to an anti-inflammatory effect in trauma of the bone marrow and as a support in the treatment of obesity.. Introducción: Los compuestos fenólicos presentes en las hojas del olivo (olea europaea l.) conferir beneficios para la salud humana. Objetivos: Revisar la literatura científica sobre los beneficios de los polifenoles de hojas de olivo para la salud humana. Método: Revisión de la literatura en las bases de datos lilacs-bireme, scielo y medline para publicaciones en inglés, portugués y español con los descriptores “olea europaea”, “hojas de olivo”, “hoja de olivo”, “hojas de olivo extractos”, “los extractos de hoja de olivo”, “compuestos fenólicos”, “polifenoles”, “oleuropeína”, “composición química”, y “salud”. Se identificaron 92 artículos, pero sólo 38 en relación con los objetivos del estudio y 9 artículos citados en las obras se incluyeron debido a su relevancia. Resultados y discusión: Los compuestos fenólicos presentes en las hojas del olivo, especialmente la oleuropeína, se asocian a antioxidante, antihipertensivo, hipoglucemiante, actividad hipocolesterolémico y cardioprotector. además, los estudios asocian la oleuropeína a un efecto anti-inflamatorio en trauma de la médula ósea y como soporte en el tratamiento de la obesidad.

Topics: Animals; Anti-Inflammatory Agents; Anti-Obesity Agents; Antihypertensive Agents; Antioxidants; Cardiotonic Agents; Clinical Trials as Topic; Colitis; Drug Evaluation, Preclinical; Food, Organic; Humans; Hypoglycemic Agents; Hypolipidemic Agents; Iridoid Glucosides; Iridoids; Olea; Phytotherapy; Plant Leaves; Polyphenols

Inflammation and oxidative stress pathways have emerged as novel targets in the management of inflammatory bowel diseases (IBD). Targeting the drug to the inflamed colon remains a challenge. Nanostructured lipid carriers (NLCs) have been reported to accumulate in inflamed colonic mucosa. The antioxidant/antiinflamatory polyphenol oleuropein (OLE) was loaded in NLCs (NLC-OLE). NLC-OLE showed to be more effective in decreasing the TNF-α secretion and intracellular reactive oxygen species (ROS) by activated macrophages (J774) compared to the conventional form of OLE. OLE efficacy was preserved within NLC-OLE ameliorating inflammation in a murine model of acute colitis: reduced levels of TNF-α and IL-6, decreased neutrophil infiltration and improved histopathology of the colon were reported. In addition, NLC-OLE enhanced the ROS scavenging activity of OLE in the colon after oral administration. These data suggest that the proposed NLC-OLE could be a promising drug delivery system for OLE in IBD treatment.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Antioxidants; Cell Line; Colitis; Disease Models, Animal; Drug Carriers; Drug Delivery Systems; Inflammation; Iridoid Glucosides; Iridoids; Lipids; Macrophages; Male; Mice; Mice, Inbred C57BL; Nanostructures; Oxidative Stress; Reactive Oxygen Species

The main phenolic secoiridoid oleuropein and active constituent from olive tree (Olea europaea, Oleaceae), has demonstrated anti-inflammatory properties in intestinal inflammation and anti-tumoral effects in different cancer cells. In this study, we evaluated the chemoprevention of oleuropein in a model of azoxymethane (AOM)/Dextran sulfate sodium (DSS)-induced colorectal cancer (CRC) in C57BL/6 mice and the modulatory effect on the Th17 response in DSS acute colitis.. Oleuropein protected from AOM/DSS-induced CRC by improving clinical symptoms, disease activity index score as well as suppressed the growth and multiplicity of colonic tumors. Treatment with oleuropein reduced intestinal IL-6, IFN-γ, TNF-α, and IL-17A concentration, and decreased cyclooxygenase-2, Bax and proliferating cell nuclear antigen protein expression. Western blot analysis also showed a markedly downregulation of CRC-related pathways as nuclear factor-κB (NF-κB), Wnt/β-catenin, phosphatidylinositol-3-kinase (P3IK)/Akt, and signal transducer and activators of transcription (STAT)3. In DSS acute model, oleuropein inhibited Th17 response, by decreasing CD4(+) Rorγt(+) IL-17(+) IFN-γ(+) T-cell subsets in the lamina propria, as well as IL-17A and IFN-γ expression.. Oleuropein as a dietary supplementation could be a promising protective agent against colitis-associated CRC.

Topics: Animals; Anticarcinogenic Agents; Azoxymethane; Cell Proliferation; Colitis; Colon; Colorectal Neoplasms; Cytokines; Dextran Sulfate; Female; Iridoid Glucosides; Iridoids; Mice, Inbred C57BL; Neoplasms, Experimental; Th17 Cells

The anti-inflammatory effect of oleuropein (1), the major phenolic secoiridoid in Olea europaea, was evaluated in an experimental model of chronic colitis in mice. Animals were exposed to four repeated cycles of dextran sodium sulfate in drinking water followed by a 7-day rest period. Animals receiving a standard diet supplemented with 0.25% of 1 (equivalent to 500 mg/kg/day) for 56 days exhibited a decrease of inflammatory symptoms, as reflected by improvement of disease activity index and histopathological changes. It was found that 1 decreased inflammatory cell recruitment and the release of inflammatory cytokines interleukin (IL)-1β and IL-6 with increased IL-10 levels in colon tissue. Colon expression of cyclooxygenase-2 and inducible nitric oxide synthase was reduced significantly by 1. The anti-inflammatory molecular mechanism of 1 was associated with the suppression of the phosphorylation of p38 mitogen-activated protein kinase and might be mediated by up-regulation of annexin A1. In addition, 1 ameliorated intestinal wound healing in IEC-18 monolayers. Therefore, oleuropein seems to be a promising active molecule in experimental ulcerative colitis.

Topics: Animals; Anti-Inflammatory Agents; Colitis; Cyclooxygenase 2; Dextran Sulfate; Interleukin-10; Interleukin-1beta; Interleukin-6; Intestinal Mucosa; Iridoid Glucosides; Iridoids; Mice; Mice, Inbred C57BL; Molecular Structure; Nitric Oxide Synthase Type II; Olea; p38 Mitogen-Activated Protein Kinases; Pyrans; T-Lymphocytes

Oleuropein, the major secoiridoid in olive tree leaves, possesses a wide range of health promoting properties. It has recently been shown to exhibit anti-inflammatory activity. We have evaluated the effect of oleuropein on dextran sulfate sodium (DSS)-induced experimental colitis in mice in order to provide insight into its mechanisms of action. Oral administration of oleuropein notably attenuated the extent and severity of acute colitis while reducing neutrophil infiltration; production of NO, IL-1β, IL-6, and TNF-α; expression of iNOS, COX-2, and MMP-9; and the translocation of the NF-κB p65 subunit to the nucleus in colon tissue. In LPS-stimulated peritoneal macrophages, the oleuropein metabolite, hydroxytyrosol, was shown to inhibit NO production, iNOS expression, NF-κB p65 subunit translocation, mRNA expression, and the release of IL-1β, IL-6, and TNF-α. These results suggest that the effect of oleuropein on DSS-induced colitis is associated with a decrease in the production of interleukins and expression of proteins, principally through reduction of NF-κB activation.

Topics: Acute Disease; Animals; Anti-Inflammatory Agents; Colitis; Cytokines; Dextran Sulfate; Female; Iridoid Glucosides; Iridoids; Macrophages, Peritoneal; Mice; Mice, Inbred BALB C; Nitric Oxide; Phenylethyl Alcohol; Pyrans