Suppression of IL‐8 Release by Sweet Olive Ethanolic Extract and Compounds in WiDr Colon Adenocarcinoma Cells

Oxidative stress can stimulate the secretion of pro‐inflammatory cytokines. Interleukin‐8 (IL‐8) has been implicated in the pathogenesis of inflammatory bowel disease and the metastatic spread of colorectal cancer. The flowers of Osmanthus fragrans (sweet olive) are used to alleviate dysentery with blood in the bowel, as well as stomach ache and diarrhea. However, the evidence of their therapeutic effects on these symptoms remains unclear. In the present study, the protective effects of sweet olive flower ethanolic extract (OFE) against oxidative stress in WiDr cells was assessed by evaluating its 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) free radical scavenging activity. In addition, cellular IL‐8 secretion was evaluated. Notably, high‐performance liquid chromatography showed verbascoside to be the primary constituent in OFE; it exhibited a DPPH scavenging activity with an IC₅₀ of 8.23 μg/mL. Moreover, OFE (1 to 100 μg/mL) showed a potent, dose‐dependent inhibitory effect on H₂O₂‐induced IL‐8 secretion in WiDr cells. Nine compounds were isolated from OFE based on a protective effect‐guided purification process. Of these compounds, 5 phenolic compounds—verbascoside, phillygenin, tyrosol, methyl 4‐hydroxycinnamate, and eutigoside A—reduced IL‐8 secretion at 10 μg/mL treatment concentrations. Further analysis showed that the anti‐inflammatory effects of OFE likely occurred via nuclear factor‐κB pathway inhibition, which attenuates IL‐8 secretion in cells. Collectively, these data suggest that OFE could be developed as an agent that suppresses IL‐8 secretion to treat chronic inflammatory diseases.     

Anti‐inflammatory Potential of Quercetin‐3‐O‐β‐D‐(“2”‐galloyl)‐glucopyranoside and Quercetin Isolated from Diospyros kaki calyx via Suppression of MAP Signaling Molecules in LPS‐induced RAW 264.7 Macrophages

Diospyros kaki (DK) contains an abundance of flavonoids and has been used in folk medicine in Korea for centuries. Here, we report for the first time the anti‐inflammatory activities of Quercetin (QCT) and Quercetin 3‐O‐β‐(“2”‐galloyl)‐glucopyranoside (Q32G) isolated from DK. We have determine the no cytotoxicity of Q32G and QCT against RAW 264.7 cells up to concentration of 50 μM. QCT and Q32G demonstrated potent anti‐inflammatory activities by reducing expression of nitric oxide (NO), tumor necrosis factor (TNF)‐α, interleukin (IL)‐1β, IL‐6 inducible NO synthase (iNOS), cyclooxygenase (COX)‐2, and mitogen‐activated protein kinase (MAPKs) in mouse RAW 264.7 macrophages activated with lipopolysaccharide (LPS). Both QCT or Q32G could decrease cellular protein levels of COX‐2 and iNOS as well as secreted protein levels of NO, PGE₂, and cytokines (TNF‐α, IL‐1β, and IL‐6) in culture medium of LPS‐stimulated RAW 264.7 macrophages. Immunoblot analysis showed that QCT and Q32G suppressed LPS‐induced MAP kinase pathway proteins p‐p38, ERK, and JNK. This study revealed that QCT and Q32G have anti‐inflammatory potential, however Q32G possess comparable activity as that of QCT and could be use as adjuvant to treat inflammatory diseases.     

Sarcodon aspratus Extract Ameliorates Dextran Sulfate Sodium‐Induced Colitis in Mouse Colon and Mesenteric Lymph Nodes

Mushrooms have been previously investigated for their immune‐modulating and anti‐inflammatory properties. We examined whether the anti‐inflammatory properties of Sarcodon aspratus ethanol extract (SAE) could elicit protective effects against dextran sulfate sodium (DSS)‐induced colitis in vivo. Male C57/BL6 mice were randomly assigned to 1 of 4 treatment groups: control (CON; n = 8), DSS‐treated (DSS; n = 9), DSS+SAE at 50 mg/kg BW (SAE50; n = 8), and DSS+SAE at 200 mg/kg BW groups (SAE200; n = 9). DSS treatment induced significant weight loss, which was significantly recovered by SAE200. Although SAE did not affect DSS‐mediated reductions in colon length, it improved diarrhea and rectal bleeding induced by DSS. SAE at 200 mg/kg BW significantly attenuated IL‐6 and enhanced IL‐10 expression in mesenteric lymph nodes (MLN), and significantly reduced IL‐6 levels in splenocytes. SAE200 also significantly attenuated DSS‐induced increase in IL‐6 and IL‐1β, and reductions in IL‐10 in colon tissue. High levels of SAE were also observed to significantly decrease inflammatory COX‐2 expression that was upregulated by DSS in mice colon. These findings may have relevance for novel therapeutic strategies to mitigate inflammatory bowel disease‐relevant inflammatory responses, via the direct and indirect anti‐inflammatory activity of SAE. We also found that SAE harbors significant quantities of total fiber and β‐glucan, suggesting a possible role for these components in protection against DSS‐mediated colitis.     

Anti‐inflammatory activity of rosemary extracts obtained by supercritical carbon dioxide enriched in carnosic acid and carnosol

The in vitro anti‐inflammatory activity of supercritical rosemary (Rosmarinus officinalis L.) extracts (rosemary A and B) is been reported in this study. To achieve that, THP‐1 macrophages were activated using lipopolysaccharide or human ox‐LDL and secretion and gene expression of TNF‐α, IL‐1β, IL‐6 and IL‐10 were evaluated, as well as COX‐2 gene expression. Results indicated that both rosemary extracts (A & B) exhibit high anti‐inflammatory activity although at a higher extent in case of rosemary B extract (5 μg mL^?1), representing a higher quantity of carnosic acid and carnosol than rosemary A. When comparing the activity of the extract to the standard itself, the anti‐inflammatory activity of standards of carnosic acid and carnosol was not as intense as that obtained with rosemary B. These data indicated that although carnosic acid content in the extracts is considered as the main anti‐inflammatory compound, a synergistic interaction with other compounds may play a significant role in enhancing its activity. Results provided the grounds for possible increase in the application of supercritical rosemary extracts in food formulations for mitigation or prevention of inflammatory diseases.     

Anti‐obesity effect of Liupao tea extract by modulating lipid metabolism and oxidative stress in high‐fat‐diet‐induced obese mice

Liupao tea (LPT) is traditional dark Chinese tea. The effect of LPT extract on high‐fat‐diet‐induced obese mice was investigated systematically. The results showed that LPT extract could reduce body weight and significantly alleviate liver damage and fat accumulation. LPT could also decrease the levels of alanine aminotransferase (ALT), aspartate transaminase (AST), alkaline phosphatase (AKP), total cholesterol (TC), triglycerides (TG), and low‐density lipoprotein cholesterol (LDL‐C) and increase the level of high‐density lipoprotein cholesterol (HDL‐C) in the liver. It also decreased the serum levels of inflammatory cytokines, including tumor necrosis factor alpha (TNF‐α), interferon gamma (IFN‐γ), interleukin (IL)‐1β, and IL‐6 and increased the serum levels of anti‐inflammatory cytokines, including IL‐10 and IL‐4. Moreover, LPT improved the levels of total superoxide dismutase (T‐SOD), glutathione peroxidase (GSH‐Px), and catalase (CAT) and reduced the level of malondialdehyde (MDA) in the liver. Moreover, LPT could upregulate the mRNA and protein expressions of peroxisome proliferator‐activated receptor alpha (PPAR‐α), lipoprotein lipase (LPL), carnitine palmitoyltransferase 1(CPT1), and cholesterol 7 alpha‐hydroxylase (CYP7A1) and downregulate those of PPAR‐γ and CCAAT/enhancer‐binding protein alpha (C/EBP‐α) in the liver. It also increased the mRNA expression of copper/zinc superoxide dismutase (SOD1), manganese superoxide dismutase (SOD2), CAT, gamma‐glutamylcysteine synthetase 1 (GSH1), and GSH‐Px. The components of LPT extract include catechin, rutin, taxifolin, and astragalin, which possibly have a wide range of biological activities. In conclusion, our work verified that LPT extract possessed an anti‐obesity effect and alleviated obesity‐related symptoms, including lipid metabolism disorder, chronic low‐grade inflammation, and liver damage, by modulating lipid metabolism and oxidative stress.     

Ginger Extract Suppresses Inflammatory Response and Maintains Barrier Function in Human Colonic Epithelial Caco‐2 Cells Exposed to Inflammatory Mediators

The beneficial effects of ginger in the management of gastrointestinal disturbances have been reported. In this study, the anti‐inflammatory potential of ginger extract was assessed in a cellular model of gut inflammation. In addition, the effects of ginger extract and its major active compounds on intestinal barrier function were evaluated. The response of Caco‐2 cells following exposure to a mixture of inflammatory mediators [interleukin [IL]‐1β, 25 ng/mL; lipopolysaccharides [LPS], 10 ng/mL; tumor necrosis factor [TNF]‐α, 50 ng/mL; and interferon [INF]‐γ, 50 ng/mL] were assessed by measuring the levels of secreted IL‐6 and IL‐8. In addition, the mRNA levels of cyclooxygenase‐2 and inducible nitric oxide synthase were measured. Moreover, the degree of nuclear factor (NF)‐κB inhibition was examined, and the intestinal barrier function was determined by measuring the transepithelial electrical resistance (TEER) and fluorescein isothiocyanate (FITC)‐dextran transfer. It was observed that ginger extract and its constituents improved inflammatory responses by decreasing the levels of nitrite, PGE2, IL‐6, and IL‐8 via NF‐κB inhibition. The ginger extract also increased the TEER and decreased the transfer of FITC‐dextran from the apical side of the epithelium to the basolateral side. Taken together, these results show that ginger extract may be developed as a functional food for the maintenance of gastrointestinal health.     

Phenethyl isothiocyanate suppresses nitric oxide production via inhibition of phosphoinositide 3‐kinase/Akt‐induced IFN‐γ secretion in LPS‐activated peritoneal macrophages

Phenethyl isothiocyanate (PEITC), a constituent of many cruciferous vegetables, is well known to have versatile physiological activities, including chemopreventive effects. On the other hand, its anti‐inflammatory effects are poorly reported. Nitric oxide (NO) is associated with a wide variety of inflammatory diseases. In this study, we investigated the effects of PEITC on NO production in LPS‐activated peritoneal macrophages from ICR mice. The signaling pathway of LPS‐induced NO production was examined using neutralizing antibodies [anti‐interferon (IFN)‐γ and anti‐interleukin (IL‐12)] and specific protein kinase inhibitors, as well as others. The activity of PEITC toward NOx production was assessed in mice that received LPS via intraperitoneal administration. The neutralizing antibody of anti‐IFN‐γ, but not anti‐IL‐12, suppressed LPS‐induced NO production by 90%. LY294002, a specific inhibitor of phosphoinositide‐3‐kinase, suppressed Akt and IFN‐γ mRNA expression up‐regulated by LPS, whereas PEITC exhibited a similar inhibition profile. Furthermore, oral administration of PEITC significantly suppressed the serum concentration of NOx in ICR mice. Our results suggest that PEITC suppresses LPS‐induced NO production via inhibition of Akt activation and the resultant decrease in expression of IFN‐γ. This is one of the first reports to demonstrate a marked anti‐inflammatory effect of PEITC following its oral administration.     

Effects of Catechol O‐Methyl Transferase Inhibition on Anti‐Inflammatory Activity of Luteolin Metabolites

Although luteolin is known to have potent anti‐inflammatory activities, much less information has been provided on such activities of its hepatic metabolites. Luteolin was subjected to hepatic metabolism in HepG2 cells either without or with catechol O‐methyl transferase (COMT) inhibitor. To identify hepatic metabolites of luteolin without (luteolin metabolites, LMs) or with COMT inhibitor (LMs+CI), metabolites were treated by β‐glucuronidase and sulfatase, and found that they were composed of glucuronide and sulfate conjugates of diosmetin in LMs or these conjugates of luteolin in LMs+CI. LMs and LMs+CI were examined for their anti‐inflammatory activities on LPS stimulated Raw 264.7 cells. Expression of iNOS and production of nitric oxide and pro‐inflammatory cytokines such as TNF‐α, IL‐1β, and IL‐6 were suppressed more effectively by the treatment with LMs+CI than LMs. Our data provide a new insight on possible improvement in functional properties of luteolin on target cells by modifying their metabolic pathway in hepatocytes.     

Dietary grape seed extract ameliorates symptoms of inflammatory bowel disease in IL10‐deficient mice

Grape seed extract (GSE) is a by‐product of the wine industry, with abundant polyphenolic compounds known for their anti‐inflammatory and anti‐oxidative effects. Using IL10‐deficient mice (IL10KO), here we showed that GSE (1% of dry feed weight) ameliorated inflammatory bowel disease indices, increased colonic goblet cell numbers and decreased myeloperoxidase levels in the large intestine. Concomitantly, GSE supplementation attenuated inflammation, decreased the expression of pore forming tight junction protein claudin2, and increased levels of Lactobacilli and Bacteroides in the gut microbiota of IL10KO mice. In summary, our study shows that GSE has protective roles on inflammatory bowel disease through altering gut inflammation, tight junction protein expression, and gut microbiota composition.     

Amino acids stimulate Akt phosphorylation,and reduce IL‐8 production and NF‐κB activity in HepG2 liver cells

Hepatic insulin resistance and inflammatory cytokine production contribute to the manifestation of the metabolic syndrome. As amino acids have been implicated in modulating insulin signaling and inflammation, we have investigated the effects of glutamine, leucine and proline on markers of inflammation and insulin sensitivity in HepG2 liver cells. Cells were incubated with IL‐1β (5 ng/mL) to stimulate IL‐8 production. After 24 h, glutamine inhibited IL‐8 production significantly (p<0.05) at 2, 5 and 10 mM (to 82, 73 and 72% of control), whereas leucine reduced IL‐8 production significantly only at 10 mM (66%) and proline at 5 and 10 mM (71 and 52%). Glutamine, leucine and proline all reduced NF‐κB activity after 3 h of IL‐1β stimulation at 2, 5 and 10 mM (p<0.001). Insulin‐induced (1 nM) Akt phosphorylation was reduced in cells treated with tumour necrosis factor‐α (10 ng/mL) for 24 h, but was partly restored by simultaneous incubation with glutamine, leucine and proline (25 mM). Phosphorylation of glycogen synthase kinase‐3β was unaffected by insulin stimulation and amino acid treatment. Our results indicate that glutamine, leucine and proline attenuate IL‐8 production, probably through inhibition of NF‐κB, and that they increase Akt phosphorylation in HepG2 cells.     

Antioxidant,Antibacterial, and Antiproliferative Activities of Free and Bound Phenolics from Peel and Flesh of Fuji Apple

This study was conducted to investigate the antioxidant, antibacterial, and antiproliferative activities of flesh free (FF), flesh bound (FB), peel free (PF), and peel bound (PB) phenolics from Fuji apple. The PB, which had highest total phenolic contents (126.15 ± 2.41 mg/100 g wet weight) and lowest total carbohydrate contents (34.68 ± 2.78 mg/100 g wet weight), showed the strongest 2,2’‐azinobis‐(3‐ethylbenthiazoline‐6‐sulphonate) (ABTS) radical scavenging activity (EC₅₀ = 0.36 ± 0.02 mg/mL), 1,1‐diphenyl‐2‐picryhydrazyl (DPPH) radical scavenging activity (EC₅₀ = 0.26 ± 0.01 mg/mL), and ferric reducing antioxidant power (Ferric reducing antioxidant power; EC₅₀ = 0.19 ± 0.02 mg/mL) compared with those of FF, FB, and PF. The PB also showed the strongest antibacterial activities on Escherichia coli, Staphylococcus aureus, and Listeria monocytogenes and it also showed the highest antiproliferative effects on Caco‐2 human colonic cancer cell (EC₅₀ = 1.44 ± 0.01 mg/mL) and Hela human cervical cell (EC₅₀ = 2.81 ± 0.01 mg/mL). Both free and bound phenolics from Fuji apple showed good antioxidant, antibacterial, and antiproliferative activities in our study, and bound phenolics had significantly higher activities compared with those of free phenolics.     

The Correlation Between In Vitro Antioxidant Activity and Immunomodulatory Activity of Enzymatic Hydrolysates from Selenium‐Enriched Rice Protein

The antioxidant and immunomodulatory activities of selenium‐enriched rice protein hydrolysates (Se‐PH) were evaluated by a cellular antioxidant activity test and macrophage proliferation and phagocytosis assays, respectively. The results showed that trypsin hydrolysate provided the highest proliferation rate of 60.91% at a concentration of 100 μg/mL. Moreover, a remarkable rise in the phagocytosis rates for trypsin hydrolysate (64.1%) and pepsin–trypsin hydrolysate (54.5%) was observed when the sample concentrations were increased to 50 μg/mL. A positive correlation was found between the phagocytic ability of macrophages and both the selenium concentration and the degree of hydrolysis of Se‐PH, and the correlation coefficients R obtained were 0.792 and 0.930 (P < 0.05), respectively. The capacity of Se‐PH to inhibit the oxidation of dichlorodihydrofluorescein had a significant negative correlation with the phagocytic ability of macrophages (R = –0.840, P < 0.05). In conclusion, a positive correlation was found between the antioxidant activity and the immunomodulatory activity of Se‐PH, which could be used as potential functional food additives for improving human health.     

p‐Coumaric acid and its conjugates: dietary sources,pharmacokinetic properties and biological activities

p‐Coumaric acid (4‐hydroxycinnamic acid) is a phenolic acid that has low toxicity in mice (LD₅₀ = 2850 mg kg^?1 body weight), serves as a precursor of other phenolic compounds, and exists either in free or conjugated form in plants. Conjugates of p‐coumaric acid have been extensively studied in recent years due to their bioactivities. In this review, the occurrence, bioavailability and bioaccessibility of p‐coumaric acid and its conjugates with mono‐, oligo‐ and polysaccharides, alkyl alcohols, organic acids, amine and lignin are discussed. Their biological activities, including antioxidant, anti‐cancer, antimicrobial, antivirus, anti‐inflammatory, antiplatelet aggregation, anxiolytic, antipyretic, analgesic, and anti‐arthritis activities, and their mitigatory effects against diabetes, obesity, hyperlipaemia and gout are compared. Cumulative evidence from multiple studies indicates that conjugation of p‐coumaric acid greatly strengthens its biological activities; however, the high biological activity but low absorption of its conjugates remains a puzzle. © 2015 Society of Chemical Industry     

Extraction and Purification of Quercitrin,Hyperoside, Rutin,and Afzelin from Zanthoxylum Bungeanum Maxim Leaves Using an Aqueous Two‐Phase System

In this study, an aqueous two‐phase system (ATPS) based on ethanol/NaH₂PO₄ was developed for the extraction and purification of quercitrin, hyperoside, rutin, and afzelin from Zanthoxylum bungeanum Maxim leaves. These 4 flavonoids were 1st extracted from dried Z. bungeanum leaves using a 60% ethanol solution and subsequently added to the ATPS for further purification. The partition behavior of the 4 flavonoids in ATPS was investigated. The optimal ATPS conditions were: 29% (w/w) NaH₂PO₄, 25% (w/w) ethanol concentration, 1% (w/w) added amount of leaf extracts, no pH adjustment, and repeated 1 h extractions at 25 °C. Under the optimal conditions for the 10 g ATPS, the absolute recovery of quercitrin, hyperoside, rutin, and afzelin reached 90.3%, 83.5%, 92.3%, and 89.1%, respectively. Compared to the 60% ethanol extracts, the content of quercitrin (44.8 mg/g), hyperoside (65.6 mg/g), rutin (56.4 mg/g), and afzelin (6.84 mg/g) in the extracts increased by 49.9%, 38.8%, 45.6%, and 36.8% respectively. The extracts after ATPS also exhibited stronger antioxidant activities, the 2,2‐diphenyl‐1‐picrylhydrazyl IC₅₀ value (10.5 μg/mL) decreased by 41.8%, and the 2,2‐azinobis(3‐ethylbenzothiazoline‐6‐sulfonic acid) diammonium salt value (966 μmol Trolox/g) and ferric reducing power value (619 μmol Trolox/g) increased by 29.8% and 53.7%, respectively. Furthermore, scale‐up experiments indicated that a larger scale experiment was feasible for the purification of the 4 flavonoids.     

Enhanced antiviral activity of soybean β-conglycinin-derived peptides by acylation with saturated fatty acids

Abstract: Peptide mixtures prepared from soybean β‐conglycinin (7S‐peptides) were acylated with saturated fatty acids of different chain length (6C‐18C) in order to improve their antiviral activity against Feline calicivirus (FCV) strain F9 which is a typical norovirus surrogate. Among the fatty acids varieties, it was revealed that 7S‐peptides acylated with myristic and palmitic acids potently inhibited FCV replication. Myristorylation and palmitoylation of 7S‐peptides kept host cells viability at 91.51% and 98.90%, respectively. The infectivity of FCV on Crandell–Reese feline kidney cells was further determined after exposure of initial titer of 10^6.47 TCID₅₀/mL. Myristoylated and palmitoylated 7S‐peptides significantly (P < 0.006) reduced FCV infectivity as compared to native 7S‐peptides. Native 7S‐peptides showed 25% FCV inhibitory activity while myristoylated and palmitoylated 7S‐peptides exhibited 98.59% and 99.98% reduction in FCV infectivity, respectively. Myristoylated and palmitoylated 7S‐peptides demonstrated higher anti‐FCV activity in a wide range of concentration with complete reduction at 25 μg/mL. Surface hydrophobicity was significantly (P < 0.05) increased after attachment of long hydrocarbon fatty acids to 7S‐peptides as supported by changes in fluorescence intensity. Enzymatic hydrolysis together with acylation will give an insight into surface and physiological functional lipopeptides derived from soy β‐conglycinin.     

Antioxidant and anti‐inflammatory activities of water distillate and its dichloromethane extract from licorice root (Glycyrrhiza uralensis) and chemical composition of dichloromethane extract

BACKGROUND: Licorice root is one of the most widely used medicinal herbs and its medicinal properties, such as antibacterial, anti‐ulcer, anti‐tumorigenic and anti‐atherosclerotic activities, have been widely reported. However, there are only a few reports on basic chemical and biological studies of the water distilled components of licorice root. RESULTS: Chinese licorice root was water distilled and the distillate was subsequently extracted with dichloromethane. Residual aqueous solution from the extraction was fractionated using column chromatography. A total of 127 chemicals were identified in the dichloromethane extract, which inhibited hexanal oxidation by over 90% for 45 days at the level of 50 µg mL^?1. A fraction eluted from the residual aqueous solution with acetone exhibited potent antioxidant activities both in a thiobarbituric acid assay and in a malonaldehyde/gas chromatography assay. The acetone fraction also exhibited strong anti‐inflammatory activity (77.9% inhibition at the level of 62 µg mL^?1) in a lipoxygenenase inhibitor screening anti‐inflammatory assay. CONCLUSION: This study demonstrated the antioxidant and anti‐inflammatory activities of the water distillate obtained from Chinese licorice root. Some volatile chemicals among the many components identified in the water distillate exhibited antioxidant activity, suggesting that many medicinal compounds escape with water vapor into the ambient air during the preparation of herbal medicine. Copyright © 2008 Society of Chemical Industry     

Sulfonation of Lactobacillus plantarum WLPL04 exopolysaccharide amplifies its antioxidant activities in vitro and in a Caco-2 cell model

Exopolysaccharide (EPS) of Lactobacillus plantarum WLPL04 and its sulfated EPS were systematically investigated for their antioxidant activities and effects on protecting the oxidative damage of Caco-2 cells from H₂O₂. Exopolysaccharide was successfully sulfonated from purified EPS as confirmed by Fourier-transform infrared spectroscopy, and the degree of sulfonation was 0.30. Both EPS and sulfated EPS showed antioxidant activities in vitro determined by 1,1-diphenyl-2-picrylhydrazyl, superoxide, and hydroxyl radical scavenging tests, and those activities of sulfated EPS were significantly enhanced at 1,000 μg/mL. Cell viabilities of Caco-2 in the range of 1 to 100 μg/mL of EPS and sulfated EPS showed no significant difference. In H₂O₂-damaged Caco-2 cells models, EPS and sulfated EPS significantly inhibited the enhancement of reactive oxygen species and malondialdehyde levels, and sulfated EPS enhanced the effects by 40.86% and 61.11% when compared with the purified EPS at the same concentration of 100 μg/mL, respectively. For the activities of antioxidant-related enzymes (superoxide dismutase, catalase, and glutathione peroxidase) and expression of genes (SOD2, GPX2, MT1M) on Caco-2 cells, strong protection abilities against the oxidative stress were displayed from both EPS and sulfated EPS, and sulfated EPS exhibited significant enhancement as compared with either EPS or control groups. In summary, sulfonation is an effective strategy for improving the antioxidant activities of EPS from L. plantarum WLPL04 in vitro and on Caco-2 cells.     

Sesamin attenuates intercellular cell adhesion molecule‐1 expression in vitro in TNF‐α‐treated human aortic endothelial cells and in vivo in apolipoprotein‐E‐deficient mice

Sesame lignans have antioxidative and anti‐inflammatory properties. We focused on the effects of the lignans sesamin and sesamol on the expression of endothelial‐leukocyte adhesion molecules in tumor necrosis factor‐α (TNF‐α)‐treated human aortic endothelial cells (HAECs). When HAECs were pretreated with sesamin (10 or 100 μM), the TNF‐α‐induced expression of intercellular cell adhesion molecule‐1 (ICAM‐1) was significantly reduced (35 or 70% decrease, respectively) by Western blotting. Sesamol was less effective at inhibiting ICAM‐1 expression (30% decrease at 100 μM). Sesamin and sesamol reduced the marked TNF‐α‐induced increase in human antigen R (HuR) translocation and the interaction between HuR and the 3'UTR of ICAM‐1 mRNA. Both significantly reduced the binding of monocytes to TNF‐α‐stimulated HAECs. Sesamin significantly attenuated TNF‐α‐induced ICAM‐1 expression and cell adhesion by downregulation of extracellular signal‐regulated kinase 1/2 and p38. Furthermore, in vivo, sesamin attenuated intimal thickening and ICAM‐1 expression seen in aortas of apolipoprotein‐E‐deficient mice. Taken together, these data suggest that sesamin inhibits TNF‐α‐induced extracellular signal‐regulated kinase/p38 phosphorylation, nuclear translocation of NF‐κB p65, cytoplasmic translocalization of HuR and thereby suppresses ICAM‐1 expression, resulting in reduced adhesion of leukocytes. These results also suggest that sesamin may prevent the development of atherosclerosis and inflammatory responses.