Chinese Yam Extracts Containing β‐Sitosterol and Ethyl Linoleate Protect against Atherosclerosis in Apolipoprotein E‐Deficient Mice and Inhibit Muscular Expression of VCAM‐1 In Vitro

Atherosclerosis is a chronic inflammatory disease, which is associated with increased expression of adhesion molecules and monocyte recruitment into the arterial wall. This study evaluated whether hexane extracts from the edible part (DB‐H1) or bark region (DB‐H2) of Dioscorea. batatas Decne have anti‐atherosclerotic properties in vivo and in vitro experiments. We also identified bioactive components in the hexane extracts. Thirty‐six apolipoprotein E (ApoE^?/?) mice and 12 control (C57BL/6J) mice were given a Western‐type diet for 11 or 21 wk. To examine the effects of yam extracts on lesion development, ApoE^?/? mice were orally administered DB‐H1 or DB‐H2 for the duration of the study (200 mg/kg b.w./day, 3 times per wk). Both DB‐H1 and DB‐H2 significantly reduced the total atherosclerotic lesion area in the aortic root. In addition, plasma concentrations of total cholesterol, oxidized‐low‐density lipoprotein, and c‐reactive protein were decreased by administration of DB‐H1 and DB‐H2. Consistent with the in vivo observations, DB‐H1 and DB‐H2 inhibited tumor necrosis factor (TNF)‐α–induced vascular cell adhesion molecule‐1 expression and adhesion of THP‐1 monocytes to TNF‐α–activated vascular smooth muscle cells. It was also found that treatment with DB‐H1 or DB‐H2 resulted in the inhibition nitric oxide (NO) and reactive oxygen species production and iNOS expression in macrophages. Thus, DB‐H1 and DB‐H2 seem to influence atherosclerosis by affecting the production of inflammatory mediators in vivo. Our results suggest that yam extracts have the potential to be used in the prevention of atherosclerosis.     

Alterations of the Profiles of Iso‐α‐Acids During Beer Ageing,Marked Instability of Trans‐Iso‐α‐Acids and Implications for Beer Bitterness Consistency in Relation to Tetrahydroiso‐α‐Acids

Age‐induced decomposition of iso‐α‐acids, the main bittering principles of beer, determines the consistency of the beer bitter taste. In this study, the profiles of iso‐α‐acids in selected high‐quality top‐fermented and lager beers were monitored by quantitative high‐performance liquid chromatography at various time intervals during ageing. The degradation of the iso‐α‐acids as a function of time is represented by the ratio, in percentage, of the sum of the concentrations of trans‐isocohumulone and trans‐isohumulone to the sum of the concentrations of cis‐isocohumulone and cis‐isohumulone. This parameter is relevant with respect to the evaluation of bitterness deterioration in aged beers. Trans‐iso‐α‐acids having a shelf half‐life of less than one year proved to be significantly less stable than cis‐iso‐α‐acids, but it appears feasible to counteract degradation if a suitable beer matrix is available. The fate of the trans‐iso‐α‐acids in particular adversely affects beer bitterness consistency. In addition to using hop products containing low amounts of trans‐iso‐α‐acids, brewers may profit of the remarkable stability of tetrahydroiso‐α‐acids, even on prolonged storage, for the production of consistently bitter beers.     

Salvianolic acid B inhibits low‐density lipoprotein oxidation and neointimal hyperplasia in endothelium‐denuded hypercholesterolaemic rabbits

BACKGROUND: Atherosclerosis and restenosis are inflammatory responses involving free radicals and lipid peroxidation and may be prevented/cured by antioxidant‐mediated lipid peroxidation inhibition. Salvianolic acid (Sal B), a water‐soluble antioxidant obtained from a Chinese medicinal herb, is believed to have multiple preventive and therapeutic effects against human vascular diseases. In this study the in vitro and in vivo inhibitory effects of Sal B on oxidative stress were determined. RESULTS: In human aortic endothelial cells (HAECs), Sal B reduced oxidative stress, inhibited low‐density lipoprotein (LDL) oxidation and reduced oxidised LDL‐induced cytotoxicity. Sal B inhibited Cu²⁺‐induced LDL oxidation in vitro (with a potency 16.3 times that of probucol) and attenuated HAEC‐mediated LDL oxidation as well as reactive oxygen species (ROS) production. In cholesterol‐fed New Zealand White rabbits (with probucol as positive control), Sal B intake reduced Cu²⁺‐induced LDL oxidation, lipid deposition in the thoracic aorta, intimal thickness of the aortic arch and thoracic aorta and neointimal formation in the abdominal aorta. CONCLUSION: The data obtained in this study suggest that Sal B protects HAECs from oxidative injury‐mediated cell death via inhibition of ROS production. The antioxidant activity of Sal B may help explain its efficacy in the treatment of vascular diseases. Copyright © 2010 Society of Chemical Industry     

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.     

Vitamin B6 suppresses serine protease inhibitor 3 expression in the colon of rats and in TNF-α-stimulated HT-29 cells

Scope: Previous reports in the areas of animal studies and, recently epidemiology, have linked anti‐tumorigenic and anti‐inflammatory effects to dietary vitamin B6. This study investigated the molecular mechanism of these effects of vitamin B6. Methods and results: DNA microarray analysis was used to obtain information on changes in colon gene expression from vitamin B6 (pyridoxine) repletion in vitamin B6‐deficient rats. Pyridoxine supplementation down‐regulated the inflammatory molecule, serine protease inhibitor clade A member 3 (SPI‐3) mRNA expression in the colon. This study also showed that tumor necrosis factor α (TNF‐α) induced SPI‐3 mRNA expression in HT‐29 human colon cancer cells, and vitamin B6 (pyridoxal hydrochloride) pretreatment of HT‐29 cells inhibited TNF ‐induced mRNA expression of SPI‐3. Vitamin B6 inhibited TNF‐α‐induced NF‐κB activation via suppression of IκBα degradation in HT‐29 cells. HT‐29 cells stably expressing epitope‐tagged ubiquitin were generated and vitamin B6 pretreatment was shown to inhibit ubiquitination of the IkB protein in response to TNF‐α‐i. Conclusion: Vitamin B6 suppressed SPI‐3 expression in the colon of rats and in TNF‐α‐stimulated HT‐29 cells. Further, this study showed a possible role of vitamin B6 in the regulation of protein ubiquitination.     

Riboflavin at High Doses Enhances Lung Cancer Cell Proliferation,Invasion, and Migration

The influence of riboflavin (vitamin B₂) upon growth, invasion, and migration in non‐small cell lung cancer cell lines was evaluated. Riboflavin at 1, 10, 25, 50, 100, 200, or 400 μmol/L was added into A549, H3255, or Calu‐6 cells. The effects of this compound upon level and/or expression of reactive oxygen species (ROS), inflammatory cytokines, intercellular adhesion molecule (ICAM)‐1, fibronectin, matrix metalloproteinase (MMP)‐9, MMP‐2, focal adhesion kinase (FAK), nuclear factor kappa B (NF‐κB), and mitogen‐activated protein kinase (MAPK) were examined. Results showed that riboflavin at test doses did not affect the level of ROS and glutathione. Riboflavin at 200 and 400 μmol/L significantly enhanced cell growth in test lung cancer cell lines, and at 400 μmol/L significantly increased the release of interleukin‐6, tumor necrosis factor‐alpha, and vascular endothelial growth factor. This agent at 200 and 400 μmol/L also upregulated protein production of ICAM‐1, fibronectin, MMP‐9, MMP‐2, NF‐κB p50, p‐p38 MAPK, and FAK; and at 400 μmol/L enhanced invasion and migration in test cell lines. These findings suggested that riboflavin at high doses might promote lung cancer progression.     

The contents of lignans in commercial sesame oils of Taiwan and their changes during heating

Sesame lignans have multiple functions and were recently reported to have potential as sources of phytoestrogens. Sesame oils used in Taiwan are expelled from roasted sesame seeds with dark colour and strong flavour. This study analyzed lignan contents of 14 brands of sesame oils, and found their mean of total lignans to be 11.5 mg/g; 82% and 15% of the lignans were sesamin, and sesamolin, respectively. Sesamol contents were relatively higher in those with darker colour. In use as a cooking oil, heating at 180 °C for 4 min did not change the content of lignans, but the level of sesamol increased after heating at 180 °C for 20 min. Heating at 200 °C for 20 min caused a significant loss of sesamolin and sesamol. From our calculation, ingestion of 10 g of sesame oil is adequate to provide the level of lignans that might benefit cardiovascular health, as found by other studies. Cooking at temperatures above 200 °C will cause loss of some lignans, but sesamin, a source of phytoestrogen, is relatively heat-stable.     

Liquid Chromatography‐Diode Array and Electrospray High‐Accuracy Mass Spectrometry of Iso‐α‐Acids in DCHA‐Iso Standard and Beer

Excellent liquid chromatographic (LC) separation of cis/trans stereoisomers of iso‐α‐acids has been achieved with reversed‐phase sorbent XTerra MS C18. An isocratic alkaline mobile phase, consisting of a mixture of 5 mmol l^?1 ammonium acetate (pH 8)‐acetonitrile‐methanol, 62:21:17 (v/v/v), was used. In the DCHA‐Iso international calibration standard trans‐isoposthumulone was identified combining photo diode array (PDA) spectra and electrospray high‐accuracy mass spectrometric (MS) data. Moreover, the molecular mass of two degradation products resulting from the in‐solution storage of the DCHA‐Iso standard was determined. The presence of trans and cis isomers of isoposthumulone, isocohumulone, isoadhumulone and iso‐n‐humulone in beer samples was confirmed. The trans isomers of iso‐α‐acids showed characteristic and reproducibly slightly different ultraviolet absorbance spectra with respect to cis isomers.     

Extraction of Lignan Compounds from Roasted Sesame Oil and their Effects on the Autoxidation of Methyl Linoleate

ABSTRACT:  Lignan compounds were extracted from roasted sesame oil and their effects on the autoxidation of methyl linoleate (ML) were studied. Lignan compounds extracted from roasted sesame oil, sesamol, sesamin, and sesamolin, were added to ML, which was then oxidized at 60 ^oC for 18 h in the dark. Alpha-tocopherol was separately added to ML for a reference antioxidant. Degree of ML oxidation was monitored by conjugated dienoic acid (CDA) contents and p -anisidine value (PAV) by AOCS methods, and ML retention by gas chromatography. CDA contents and PAV of samples increased with the oxidation time at 60 ^oC in the dark, and ML decreased. Sesamol-, sesamin-, or sesamolin-added samples showed lower CDA contents, PAV, and ML loss than the samples without lignans during oxidation in the dark, which indicated that lignan compounds lowered the ML autoxidation. The antioxidant activity of sesamol was significantly higher ( P < 0.05) than that of sesamin, sesamolin, or α-tocopherol. Lignan compounds added to ML were degraded during the autoxidation of ML, and the degradation rate was higher in sesamol- than in sesamin-, or sesamolin-added ML, but was lower than in tocopherol-added samples. As the lignan compounds concentration in ML increased, the degradation rate of lignans decreased, and the inhibition of the ML autoxidation by lignan compounds increased. The results strongly suggested that the autoxidative stability of ML could be improved by the addition of sesamol, sesamin, or sesamolin extracted from the roasted sesame oil.     

芝麻中木脂素的组成、结构及其生理功能

介绍了芝麻中木脂素类物质(lignans):芝麻素、芝麻林素、芝麻酚以及芝麻林素酚等生物活性物质的结构、含量以及其所具有的抗氧化、抗癌、保护肝脏、降低血浆中的胆固醇、调节脂质代谢等诸多生理功能特性.     

Resveratrol Regulates Activated Hepatic Stellate Cells by Modulating NF‐κB and the PI3K/Akt Signaling Pathway

In the present study, we investigated whether resveratrol could suppress the hepatic fibrogenesis in activated hepatic stellate cells. The immortalized rat hepatic stellate cells, t‐HSC/Cl‐6, were treated with resveratrol 1 h prior to lipopolysaccharide (LPS, 1 μg/mL). Resveratrol decreased t‐HSC/Cl‐6 cell viability at much lower concentrations within 24 h. Resveratrol pretreatment also decreased the LPS‐induced protein expression of α‐SMA and collagen I. In addition, resveratrol significantly reduced the protein expression of Toll‐like receptor 4 (TLR4) and myeloid differentiation primary response gene 88 (MyD88), and the expression of phosphorylated phosphatidylinositol 3‐kinase (PI3K) and phosphorylated serine/threonine kinase B (Akt). Moreover, resveratrol markedly blocked the translocation of nuclear factor (NF)‐κB in LPS‐activated HSCs. Furthermore, resveratrol inhibited HSCs activation through stimulating LXRβ, but did not influence LXRα. Overall, we conclude that the antifibrotic effect of resveratrol is the result of blocking NF‐κB activation and PI3K/Akt phosphorylation, which inhibits HSC activation to obstruct liver fibrosis. Thus, resveratrol may be a natural agent for preventing hepatic fibrosis.     

A critical review of methodologies used in determination of relative bio‐availability ratio of RRR‐α‐tocopheryl acetate and all‐rac‐α‐tocopheryl acetate

Bio‐availability of different α‐tocopherol forms in livestock animals is measured by the increase in plasma or tissue concentrations of α‐tocopherol after oral administration. It is generally accepted that RRR‐α‐tocopheryl acetate (natural source vitamin E derived from vegetable oil) has a higher bio‐availability compared to all‐rac‐α‐tocopheryl acetate (synthetic vitamin E, i.e. α‐tocopherol produced by chemical synthesis). However, different bio‐availability ratios have been reported in the literature. The major reason for conflicting results in literature studies was the inability to separate the proportion of α‐tocopherol originating from test materials, from the proportion of α‐tocopherol originating from basal dietary ingredients and pre‐feeding. This causes significant variability. For bio‐availability determination, a baseline or control treatment is essential. The estimation of bio‐availability without correction for basal vitamin E status will lead to incorrect interpretation of the results. When using proper methodologies, it is possible to correct for the impact of α‐tocopherol intake from basal ingredients and α‐tocopherol originating from pre‐feeding, therefore yielding results reflecting the true relative bio‐availability of different α‐tocopherol substances. When reviewing literature data a critical evaluation of the method used in determination of relative bio‐availability is recommended. Copyright © 2010 Society of Chemical Industry     

芝麻素在芝麻种子亚细胞结构中的分布

芝麻素等木脂素是芝麻种子中一种重要的天然抗氧化剂,具有多种生理活性功能。阐明芝麻素在芝麻种子亚细胞结构中的分布,对于芝麻深加工,尤其是芝麻素的提取和利用具有重要意义。芝麻素为脂溶性成分,故以芝麻脂质主要存在状态——油体作为主要研究对象。结果表明：芝麻中约95%的芝麻素和约95%的脂质分布在油体中,而其余部分则分布在内质网等膜结构中,显示了芝麻素和脂质之间有极规律的量化关系;碱洗对油体的芝麻素含量影响不大,而尿素则可一定程度溶出油体中的芝麻素;高速剪切可破坏油体微结构,导致芝麻素释放,而石磨制浆可极大程度保护油体微结构。     

The Significance of Iso‐α‐Acids for Beer Quality Cambridge Prize Paper

The iso‐α‐acids and their chemically‐modified variants play a disproportionately large role in the final quality of beer. Here, fundamental aspects of two of these quality issues — foam and bitterness — are discussed. A common feature of both issues is the dependence on the hydrophobic character of the hop compounds on both bitterness potency and ability to stabilise foams. Thus the isocohumulones appear significantly less bitter than the other, more hydrophobic hop compounds. Also apparent were the differences in bitterness between the cis‐ and the trans‐isomers, with the former being the more potent. Also described are the differences in the partitioning of the cis‐ and trans‐iso‐α‐acids into beer foam. The trans‐isomers are enriched in foam relative to their cis‐counterparts and may account for the observed enrichment of cis‐isomers in the final beer relative to the common ratios observed upstream.     

The preventive role of breadfruit against inflammation‐associated epithelial carcinogenesis in mice

Artocarpus communis has been identified as a rich source of flavonoids and has been gaining attention for its potential chemopreventive abilities. In this study, methanol extracts from the fruit of A. communis (MEFA) and leaf of A. communis (MELA) were prepared, and their effects on inflammation‐associated skin tumorigenesis were assessed using mouse models, including 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA) induced cutaneous inflammation as well as 7,12‐dimethylbenz[α]anthracene (DMBA) initiated and TPA‐promoted skin tumorigenesis. According to the results, both MEFA and MELA decreased the intensity of leukocyte infiltration in mouse dorsal skin and cutaneous edema induced by TPA, which appeared to be mediated by inhibition of proinflammatory genes (inducible nitric oxide synthase, cyclooxygenase‐2 (COX‐2), tumor necrosis factor‐α (TNF‐α), IL‐1β, and IL‐6) and proinflammatory mediators (TNF‐α, IL‐1β, and Prostaglandin E₂). In addition, topical application with MEFA or MELA effectively attenuated tumor incidence, multiplicity, volume, malignancy as well as angiogenesis of TPA‐stimulated skin tumor promotion in DMBA‐initiated mice. Notably, immunohistochemical stain showed that MEFA and MELA attenuated COX‐2 expression of both skin and tumor tissues in different animal tests, which may be closely related to the suppression of nuclear factor kappa B/activator protein signaling networks. These findings first demonstrate that flavonoid‐rich A. communis may exert potent anti‐inflammatory activity through modulation of COX‐2 in TPA‐activated skin and tumor tissues.