ellagitannin and Disease-Models--Animal

This study aimed to evaluate the protective role of ground raspberry seeds (RBS) as a source of polyphenols and essential fatty acids on blood plasma enzymatic antioxidant status, lipid profile, and endothelium-intact vasodilation during physiological and pathological conditions. Young normotensive Wistar-Kyoto rats (WKYs) and spontaneously hypertensive rats (SHRs) at ten weeks of age were fed with either a control diet or were supplemented with added 7% RBS for six weeks (

Topics: Acetylcholine; Animals; Aspartate Aminotransferases; Atherosclerosis; Cardiovascular Diseases; Catalase; Cyclooxygenase 2; Dietary Fiber; Dietary Supplements; Disease Models, Animal; Epoprostenol; Flavonoids; Hydrolyzable Tannins; Hypertension; Liver; Male; Nitric Oxide Synthase Type II; Rats, Inbred SHR; Rats, Inbred WKY; Rubus; Vasodilation

Pomegranate shows neuroprotective effects against Alzheimer's disease (AD) in several reported animal studies. However, whether its constituent ellagitannins and/or their physiologically relevant gut microbiota-derived metabolites, namely, urolithins (6H-dibenzo[b,d]pyran-6-one derivatives), are the responsible bioactive constituents is unknown. Therefore, from a pomegranate extract (PE), previously reported by our group to have anti-AD effects in vivo, 21 constituents, which were primarily ellagitannins, were isolated and identified (by HPLC, NMR, and HRESIMS). In silico computational studies, used to predict blood-brain barrier permeability, revealed that none of the PE constituents, but the urolithins, fulfilled criteria required for penetration. Urolithins prevented β-amyloid fibrillation in vitro and methyl-urolithin B (3-methoxy-6H-dibenzo[b,d]pyran-6-one), but not PE or its predominant ellagitannins, had a protective effect in Caenorhabditis elegans post induction of amyloid β(1-42) induced neurotoxicity and paralysis. Therefore, urolithins are the possible brain absorbable compounds which contribute to pomegranate's anti-AD effects warranting further in vivo studies on these compounds.

Topics: Age Factors; Alzheimer Disease; Amyloid beta-Peptides; Animals; Animals, Genetically Modified; Biophysics; Blood-Brain Barrier; Caenorhabditis elegans; Chromatography, Liquid; Computer Simulation; Coumarins; Disease Models, Animal; Dose-Response Relationship, Drug; Humans; Hydrolyzable Tannins; Lythraceae; Mass Spectrometry; Models, Biological; Neuroprotective Agents; Peptide Fragments

Pomegranate (Punica granatum L.) has been used for centuries for the treatment of inflammatory diseases. However, there is a lack of comprehensive information focused on the properties of a certain pomegranate (poly)phenolic profile to cure pain and gastric injury induced by anti-inflammatory drugs. This study investigated the systemic effects of different doses of a HPLC-characterized pomegranate extract on the formalin-induced nociceptive behavior in mice. The effect of the extract against gastric injury caused by non-steroidal anti-inflammatory drugs and ethanol was also assessed. Pomegranate reduced nociception in both phases of the formalin test, suggesting central and peripheral activities to inhibit nociception. Indomethacin-induced gastric injury was not produced in the presence of pomegranate, which also protected against ethanol-induced gastric lesions. The present results reinforce the benefits of pomegranate (poly)phenolics in the treatment of pain as well as their anti-inflammatory properties.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Chromatography, High Pressure Liquid; Disease Models, Animal; Dose-Response Relationship, Drug; Hydrolyzable Tannins; Lythraceae; Male; Mice; Nociceptive Pain; Plant Extracts; Polyphenols

Hepatocellular carcinoma (HCC) is the fifth most common cancer worldwide and is the third most common cause of cancer-related deaths. Currently available treatment options for HCC patients are scarce resulting in an urgent need to develop a novel effective cure. Polygonum capitatum is a medicinal herb which has been used to treat inflammatory diseases in Miao nationality of China. We recently isolated a pure compound davidiin from P. capitatum extract. Four HCC cell lines were treated with davidiin. Cell viability was recorded by MTT assay. siRNAs targeting enhancer of zeste homolog 2 (EZH2) were applied to modulate the expression of EZH2. Established xenograft mice models of HCC were applied to evaluate the in vivo anticancer activity of davidiin. We investigated the anticancer activity and the underlying mechanism of davidiin. The compound inhibited HCC cell growth and also suppressed tumor growth in xenografted HCC mouse. Such inhibition was facilitated by specifically downregulation on EZH2. The compound possesses anticancer activity both in vitro and in vivo which warrants further clinical investigation as a potential anti-HCC agent.

Topics: Animals; Apoptosis; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Proliferation; Disease Models, Animal; Drug Resistance, Neoplasm; Enhancer of Zeste Homolog 2 Protein; Gene Expression Regulation, Neoplastic; Gene Knockdown Techniques; Humans; Hydrolyzable Tannins; Liver Neoplasms; Male; Mice; Polycomb Repressive Complex 2; Proteasome Endopeptidase Complex; Tannins; Tumor Burden; Xenograft Model Antitumor Assays

Urolithin A is a major metabolite produced by rats and humans after consumption of pomegranate juice or pure ellagitannin geraniin. In this study, we investigated the anti-inflammatory effect of urolithin A on carrageenan-induced paw edema in mice. The volume of paw edema was reduced at 1h after oral administration of urolithin A. In addition, plasma in treated mice exhibited significant oxygen radical antioxidant capacity (ORAC) scores with high plasma levels of the unconjugated form at 1h after oral administration of urolithin A. These results indicate strong associations among plasma urolithin A levels, the plasma ORAC scores, and anti-inflammatory effects and may help explain a mechanism by which ellagitannins confer protection against inflammatory diseases.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Coumarins; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Discovery; Drug Evaluation, Preclinical; Edema; Free Radical Scavengers; Glucosides; Glucuronides; Humans; Hydrolyzable Tannins; Lythraceae; Mice; Mice, Inbred ICR; Rats