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Vanin-1 is an amidohydrolase that catalyses the conversion of pantetheine into the amino-thiol cysteamine and pantothenic acid (coenzyme A precursor), which plays a vital role in multiple physiological and pathological processes. In this study, an enzyme-activated near-infrared (NIR) fluorescent probe (DDAV) has been constructed for sensitively detecting Vanin-1 activity in complicated biosamples on the basis of its catalytic characteristics. DDAV exhibited a high selectivity and sensitivity toward Vanin-1 and was successfully applied to the early diagnosis of kidney injury in cisplatin-induced kidney injury model. In addition, DDAV could serve as a visual tool for in situ imaging endogenous Vanin-1 in vivo. More importantly, Enterococcus faecalis 20247 which possessed high expression of Vanin-1 was screened out from intestinal bacteria using DDAV, provided useful guidance for the rational use of NSAIDs in clinic. Finally, oleuropein as a potent natural inhibitor for Vanin-1 was discovered from herbal medicines library using a high-throughput screening method using DDAV, which held great promise for clinical therapy of inflammatory bowel disease.
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Background: Oleuropein is a form of phenoliccompound which can be majorly found in the oliveleaves. Previous studies have shown several biologicalfunctions of oleuropein against different cancer cells.Aim and Objectives: This research was designed tostudy the pre-initiation effect of oleuropein on the earlyskin tumour development using a mouse model.Material and Methods: Female Institute of CancerResearch (ICR) mice (n=6 per group) were divided into2 groups (group 1 as a carcinogen control and group 2 asa vehicle control) and 1 treatment group (group 3: 10mg/kg of oleuropein). Results:After 10 weeks, Group 3showed delay in epidermal hyperplasia formation and asignificant reduction (p<0.05) in the epidermalthickness as compared to Group 1. Data were alsodisplayed a significant increase (p<0.05) in theapoptotic rate in Group 3 as compared to Group 1 and 2.For biochemical assays, the level of Malondialdehyde(MDA) was significantly (p<0.05) decreased whilst thelevels of Glutathione (GSH) and Superoxide Dismutase(SOD) were significantly (p<0.05) increased in Group 3as compared to Group 1. Conclusion: Our resultsindicate that pre-initiation treatment of oleuropein mayprevent skin tumour development through itsantioxidant and apoptotic activities.
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silica gel column chromatography, Sephadex LH-20 gel column chromatography, medium pressure column chromatography, high pressure flash chromatography, and semi-preparative HPLC, and their structures were elucidated on the basis of physico-chemical constants and spectral analysis. Results: Fourteen compounds were identified as syringin (1), 3, 4-dihydroxyphenyl ethanol (2), oleuropein (3), salidroside (4), oleoside 11-methyl ester (5), (8E)-nuezhenide (6), (8Z)-ligstroside (7), oleoacteoside (8), oleoside dimethyl ester (9), olivil-4'-O-β-D-glucoside (10), (+)-cyclo-olivil-6-O-β-D-glucoside (11), (+)-cyclo-olivil-4'-O-β-D-glucoside (12), ligstroside (13), and wilfordiol B (14). Conclusion: Compounds 2, 4, and 12-14 are obtained from this genus for the first time, and compounds 1, 3, and 5-11 are obtained from this plant for the first time.
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Objective To establish the HPLC fingerpint method for simultaneous determination of four representative components (salidroside, echinacoside, specnuezhenide and oleuropein) of Ligustri Lucidi Fructus, so as to provide a reference for the quality control. Methods The method was performed on an Diamonsil C18 anlytical column (250 mm × 4.6 mm, 5 μm) at the column temperature of 30 ℃. The gradient mobile phase consisted of acetonitrile (A)-0.1% formic acid (B) with a flow rate of 1.0 mL/min. The detection wavelengths were 224 nm. HPLC-Q/TOF-MS were used for identifing the common peaks. Results By studying comparatively the fingerprints of 11 samples, 14 common peaks have been confirmed. There were 12 common peaks were identified by HPLC-Q/TOF-MSE. The similarity of 10 batches are greater than 0.990. Salidroside, echinacoside, specnuezhenide and oleuropein were baseline separated with good linearity relationships (r > 0.999) between concentration and peak areas over the linear ranges. The average recoveries of the investigated compounds were 97.40%, 98.99%, 97.03%, and 100.55%, respectively. Conclusion The method is accurate, reliable and with good reproducibility. It could be used for quality control and evaluation of Ligustri Lucidi Fructus.
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This study have been designed to study the effect of extracted pure oleuropein from Oleaeuropaealeaf against alloxan induced type 1 diabetic rats.Diabetic male ratwas induced by injectingsingle subcutaneous injection of 100 mg/kg b.wof alloxan.Respectively, pure oleuropein compound (5, 10, 15 and 20 mg/kg.b.w)was orally administered once per a day during a period of 40 days ofexperiment.Then, the serum blood was collected for the determination of glucose level,haematological analysis, enzymatic and non-enzymatic antioxidant. Further, pancreatic tissue was evaluated for histological examination. Oleuropein showed a significant rolein attenuating the blood glucose levels and elevation of in-vivo antioxidantafter treating diabetic rats with 5 and 10 mg/kg. b.w.The haematologicaltest did not show any significant differences. The histological sections of diabetic rats treated with 5mg/kg/ b.w ofoleuropein showed regularity in size appearance of pancreatic islet with normal distribution of islet cells.Oleuropein as a natural active compound have antioxidant activity to attenuate the effect of alloxan against diabetic disease.Therefore, it can be recommended to use oleuropein as an additive food to cure type 1 diabetic.
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This study aimed to elucidate the mechanism behind the effects of oleuropein (OL) on improving insulin resistance in obese db/db mice.Twelve 6-to 8-week-old male db/db mice were randomly divided into the model group and the OL group with 6 in each group according to their levels of blood glucose and body weight,while six C57BL/6J mice with the same age were made up for the normal group.Mice of the OL group was intragastrically administered with (50 mg·kg-1) once a day.The mice of the other groups were treated with the saline solution with the same dosage.After treatment for four weeks,OGTT test was carried out,while fast blood glucose and serum insulin were tested.RT-PCT and western blot were used to quantify the mRNA and protein expressions of certain targets in the liver.As a result,it was found that the body weight,fast blood glucose,serum insulin level and insulin resistance index were significantly decreased in the mice of the OL group when compared with model group after the treatment for 4 weeks (P＜0.05 or P＜0.01).Plasma glucose levels at each time point of OGTT tests were lower in the mice of the OL group than those of the model group (P＜0.01).The mRNA and protein expressions of InsR,IRS-1 and GLUT-2 in the mice of the OL group increased significantly (P＜0.01).In conclusion,it was demonstrated that oleuropein may reduce the blood glucose and improve the insulin resistance in db/db mice through up-regulating the mRNA and protein expressions of InsR,IRS-1 and GLUT-2 in the liver.
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Objective: To investigate the chemical constituents from the berries of Physalis pubescens. Methods: The constituents from the 80% ethanol extract of berries of P. pubescens were separated and purified by all several chromatographic technologies. The isolated compounds' structures were elucidated by physicochemical properties and spectral data analysis. Results: Nine compounds were isolated and purified. They were identified as 5-hydroxymethylfurfural (1), ethyl caffeate (2), β-sitosterol (3), trans-p-hydroxyl ethyl cinnamate (4), quercetin 3,5,7-trimethyl ether 3'-O-β-D-glucopyranoside (5), quercetin-3-O-(6'-O-trans-p-coumaroyl)-β-D-glucopyranoside (6), kaempferol-3-O-β-D-rutinoside (7), oleuropein (8), and 4,4'-diol-2'-methoxychalcone (9). Conclusion: Compounds 4-9 are obtained from the plants of genus Physalis L. for the first time, and compound 1 is isolated from P. pubescens for the first time.
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Azeitona de mesa é o produto vegetal fermentado de maior importância no mundo ocidental. Apesar de não possuir produção significativa, o Brasil está entre os dez maiores consumidores de azeitona de mesa do mundo. Para o ano safra 2013/2014 (período entre os dias 01 de outubro até 30 de setembro), estima-se que o país seja o segundo maior importador e o nono maior consumidor do fruto. No entanto, as características do fruto e os principais processos de elaboração de azeitonas de mesa são pouco conhecidos no Brasil. Dessa maneira, este trabalho objetiva realizar um levantamento do mercado, as principais tecnologias utilizadas e os aspectos legais associadas à produção de azeitona de mesa.
Table olives is the greater importance fermented vegetable product in the western world. Despite not having significant production, Brazil is among the ten largest consumers of table olives in the world. For the crop year of 2013/2014 (period between 01 October to 30 September) it is estimated that the country becomes the second largest importer and the ninth-largest consumer of the fruit. However, knowledge about the fruit characteristics and the main processes of elaboration of table olives are scarce. Thus, this research aims to survey the market, main technologies and the associated legal aspects of the production of table olives.
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AIM:To investigate the effect of oleuropein on interleukin-1β( IL-1β)-induced SD rat articular chondrocytes .METHODS:The SD rat articular chondrocytes were isolated by 2 step enzyme digestions .The chondrocytes were cultured in vitro.Inverted microscopic observation was performed during the culture .Alcian blue staining and type II collagen immunohistochemical staining were used to identify the chondrocytes .The effects of oleuropein on the viability of chondrocytes were determined by CCK-8 assay.The cells in 3rd passage were pretreated with oleuropein at 10, 50 or 100 μmol/L and subsequently stimulated with IL-1βat 10 μg/L for 24 h.Production of prostaglandin E 2 ( PGE2 ) and ni-tric oxide (NO) were evaluated by the Griess reaction and an enzyme linked immunosorbent assay (ELISA).The mRNA expression of matrix metalloproteinase ( MMP)-1 and MMP-13 was measured by real-time PCR.The protein levels of in-ducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and nuclear factor-kappa B (NF-κB) were detected by Western blotting .RESULTS:The cell viability of chondrocytes was not significantly impaired by treating with oleuropein at concentration of 10, 50 or 100μmol/L for 24 h compared with control group .Pretreatment with oleuropein significantly in-hibited the production of PGE 2 and NO induced by IL-1β.Oleuropein also significantly decreased the IL-1β-stimulated MMP-1 and MMP-13 mRNA expression in articular chondrocytes .Pretreatment with oleuropein inhibited the IL-1β-media-ted activation of NF-κB by suppressing the degradation of its inhibitory protein IκBαin the cytoplasm .CONCLUSION:Oleuropein inhibits IL-1β-induced inflammatory gene expression by suppressing NF-κB activation at the transcriptional le-vel, suggesting a new mechanism for the anti-inflammatory effects of oleuropein as a novel agent on treating with osteoarthri-tis.
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Objective: To investigate the effect of oleuropein (OE) on long term potentiation (LTP) at hippocampal perforant path-dentate gyrus synapses in vivo. Methods: An outer guide cannula, a monopolar recording electrode, and a bipolar stimulating electrode were implanted in the skull and extracellular recording technique was used to record the population spike in the dentate gyrus of anesthetized rats. Results: Oleuropein significantly increased the basal synaptic transmission and the amplitude of population spike was increased from (117.6 ± 2.3)% to (134.9 ± 3.7)% after administration with OE. OE also accelerated LTP induction and maintenance, the population spike amplitude after high frequency stimulation was increased from (167.2 ± 12.8)% to (225.5 ± 15.5)% and the maintenance phase of LTP was from (182.1 ± 15.1)% to (210.5 ± 9.0)% respectively after administration with OE. Conclusion: Present study showed that OE significantly improved different stages of LTP, which could be the molecular mechanism of its efficacy on attenuating AD-like pathology and delaying cognitive decline. OE can be a promising drug for AD and dementia.
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Nonalcoholic steatohepatitis (NASH) is characterized by hepatocyte injury and inflammatory cell infiltration, which has been linked to peripheral insulin resistance and increased levels of triglycerides in the liver. The purposes of this study were to establish a mouse model of NASH by feeding mice a 60% high-fat diet (HFD) and to demonstrate the anti-fibrotic effects of oleuropein, which has been shown to have anti-oxidant and anti-inflammatory properties, in this HFD-induced mouse model of NASH. C57BL/6 mice were divided into three groups: a regular diet group (Chow), a HFD group and an oleuropein-supplemented HFD group (OSD), which was fed a 0.05% OSD for 6 months. The effects of oleuropein in this model were evaluated using biochemical, histological and molecular markers. The expression levels of alpha-smooth muscle actin (alpha-SMA)and collagen type I in the HFD and OSD groups were evaluated using real-time PCR and western blotting. The body weight, biochemical marker levels, nonalcoholic fatty liver disease activity score, homeostasis model of assessment-insulin resistance (HOMA-IR) and leptin levels observed in the HFD group at 9 and 12 months were higher than those observed in the Chow group. The HOMA-IR and leptin levels in the OSD group were decreased compared with the HFD group. In addition, alpha-SMA and collagen type I expression were decreased by oleuropein treatment. We established a NASH model induced by HFD and demonstrated that this model exhibits the histopathological features of NASH progressing to fibrosis. Our results suggest that oleuropein may be pharmacologically useful in preventing the progression of steatohepatitis and fibrosis and may be a promising agent for the treatment of NASH in humans.
Subject(s)
Animals , Mice , Actins/genetics , Antihypertensive Agents/therapeutic use , Collagen Type I/genetics , Diet, High-Fat/adverse effects , Fatty Liver/drug therapy , Fibrosis/etiology , Iridoids/therapeutic use , Leptin/genetics , Liver/metabolism , Mice, Inbred C57BLABSTRACT
Objective: To prepare hydroxytyrosol (HT) by alkaline hydrolysis of oleuropein and to investigate its anti-oxidative property. Methods: According to single factor experiments, four variables: temperature, sodium hydroxide concentration, time, and the ratio of solid to liquid, were selected. On the basis of single factor experiments, orthogonal tests of L9(34) were carried out. HPLC-MS method was also further applied for the qualitative analysis on HT. Under the same conditions, contrast experiments on the acid and alkaline actions were made. Finally, anti-oxidative activity of HT was evaluated. Results: The results showed that the selected variables were all highly significant. Also, the descending influence orders on HT were temperature > sodium hydroxide concentration > time > the ratio of solid to liquid. Lastly, the optimal conditions on HT yield were obtained as follow: temperature 90°C, sodium hydroxide concentration 0.2 mol/L, time 45 min, and the ratio of solid to liquid 1:15. The HPLC retention time of HT was about 10.3 min, and its relative molecular weight of fragment ion by MS was 134.8. By comparison with the acid action, it was proved that the alkaline action was better in HT yield. In addition, the anti-oxidative activity of HT was carried out on scavenging DPPH radical. The results showed that DPPH scavenging capability of HT was 2.45 times of BHT. Conclusion: HT yield is well obtained under the alkaline condition and has a good anti-oxidation.