α‐Glucosidase and α‐amylase inhibitory activities of phloroglucinal derivatives from edible marine brown alga,Ecklonia cava

BACKGROUND: Diabetes mellitus (DM) is a chronic metabolic disorder characterized by defects in insulin secretion and action, which can lead to damaged blood vessels and nerves. With respect to effective therapeutic approaches to treatment of DM, much effort has being made to investigate potential inhibitors against α‐glucosidase and α‐amylase from natural products. The edible marine brown alga Ecklonia cava has been reported to possess various interesting bioactivities, which are studied here. RESULTS: In this study, five phloroglucinal derivatives were isolated from Ecklonia cava: fucodiphloroethol G ( 1 ), dieckol ( 2 ), 6,6′‐bieckol ( 3 ), 7‐phloroeckol ( 4 ) and phlorofucofuroeckol A ( 5 ); compounds 1, 3 and 4 were obtained from this genus for the first time and with higher yield. The structural elucidation of these derivatives was completely assigned by comprehensive analysis of nuclear magnetic spectral data. The anti‐diabetic activities of these derivatives were also assessed using an enzymatic inhibitory assay against rat intestinal α‐glucosidase and porcine pancreatic α‐amylase. Most of these phlorotannins showed significant inhibitory activities in a dose‐dependent manner, responding to both enzymes, especially compound 2 , with the lowest IC₅₀ values at 10.8 µmol L^?1 (α‐glucosidase) and 124.9 µmol L^?1 (α‐amylase), respectively. Further study of compound 2 revealed a non‐competitive inhibitory activity against α‐glucosidase using Lineweaver‐Burk plots. CONCLUSION: These results suggested that Ecklonia cava can be used for nutritious, nutraceutical and functional foods in diabetes as well as for related symptoms. Copyright © 2009 Society of Chemical Industry     

Isolation of eriocitrin (eriodictyol 7‐O‐rutinoside) as an arachidonate lipoxygenase inhibitor from Lumie fruit (Citrus lumia) and its distribution in Citrus species

An inhibitory compound acting against rat platelet 12‐lipoxygenase was isolated from the peel of Lumie fruit (Citrus lumia) by activity‐guided separation. It was identified as eriocitrin (eriodictyol 7‐O‐rutinoside) by spectroscopic analyses. Eriocitrin inhibited 5‐lipoxygenase (IC₅₀29.1 µmol L^?1) from rat peritoneal polymorphonuclear leukocytes in addition to 12‐lipoxygenase (IC₅₀22.3 µmol L^?1). Its aglycone, eriodictyol (5,7,3′, 4′‐tetrahydroxyflavanone), was a much more potent inhibitor of both 12‐lipoxygenase (IC₅₀0.07 µmol L^?1) and 5‐lipoxygenase (IC₅₀0.20 µmol L^?1). It also inhibited the production of leukotriene B₄ in intact peritoneal polymorphonuclear leukocytes stimulated with calcium ionophore A23187 (IC₅₀12.7 µmol L^?1). The distribution of eriocitrin in 39 citrus fruits was investigated by high‐performance liquid chromatography analysis. Lumie, eureka lemon (Citrus limon), Sambokan (Citrus sulcata), Sudachi (Citrus sudachi) and Koji (Citrus leiocarpa) fruits were found to contain high levels of eriocitrin in both peel and juice vesicles. Copyright © 2006 Society of Chemical Industry     

Antioxidant and melanogenesis‐inhibitory activities of collagen peptide from jellyfish (Rhopilema esculentum)

BACKGROUND: Jellyfish collagen was hydrolysed with trypsin and properase E, and jellyfish collagen peptide (JCP) was purified from the enzymatic hydrolysate using ion exchange chromatography and gel filtration. The antioxidant activity of JCP in a linoleic acid emulsion system, its superoxide anion‐ and hydroxyl radical‐scavenging activities and its copper‐chelating ability were evaluated in vitro. Initial investigations of JCP's ability to inhibit melanogenesis were carried out using cultured B16 melanoma cells. RESULTS: The molecular weight distribution of JCP was from 400 to 1200 Da. Amino acid analysis showed that JCP was rich in Gly, Pro, Ser, Ala, Glu and Asp and had a total hydrophobic amino acid content of 384.2 g kg^?1. JCP showed high antioxidant activity (IC₅₀147.8 µg mL^?1), superoxide anion‐scavenging activity (IC₅₀21.9 µg mL^?1), hydroxyl radical‐scavenging activity (IC₅₀16.7 µg mL^?1) and copper‐chelating ability (IC₅₀88.7 µg mL^?1) in vitro. It also significantly inhibited intracellular tyrosinase activity, decreased melanin content and enhanced glutathione synthesis (P < 0.05). Furthermore, JCP decreased intracellular cAMP levels and suppressed tyrosinase mRNA expression. CONCLUSION: Based on the results of this study, JCP exerts anti‐melanogenic actions via its antioxidant properties and copper‐chelating ability. JCP could be used as a natural skin‐lightening agent in the medicine and food industries. Copyright © 2009 Society of Chemical Industry     

Polygonum viviparum L. inhibits the lipopolysaccharide‐induced inflammatory response in RAW264.7 macrophages through haem oxygenase‐1 induction and activation of the Nrf2 pathway

BACKGROUND: Polygonum viviparum L. (PV) is a member of the family Polygonaceae and is widely distributed in high‐elevation areas. It is used as a folk remedy to treat inflammation‐related diseases. This study was focused on the anti‐inflammatory response of PV against lipopolysaccharide (LPS)‐induced inflammation in RAW264.7 macrophages. RESULTS: Treatment with PV did not cause cytotoxicity at 0–50 µg mL^?1 in RAW264.7 macrophages, and the IC₅₀ value was 270 µg mL^?1. PV inhibited LPS‐stimulated nitric oxide (NO), prostaglandin (PG)E₂, interleukin (IL)‐1β and tumour necrosis factor (TNF)‐α release and inducible NO synthase (iNOS) and cyclooxygenase (COX)‐2 protein expression. In addition, PV suppressed the LPS‐induced p65 expression of nuclear factor (NF)‐κB, which is associated with the inhibition of IκB‐α degradation. These results suggest that, among mechanisms of the anti‐inflammatory response, PV inhibits the production of NO and these cytokines by down‐regulating iNOS and COX‐2 gene expression. Furthermore, PV can induce haem oxygenase (HO)‐1 protein expression through nuclear factor E2‐related factor 2 (Nrf2) activation. A specific inhibitor of HO‐1, zinc(II) protoporphyrin IX, inhibited the suppression of iNOS and COX‐2 expression by PV. CONCLUSION: These results suggest that PV possesses anti‐inflammatory actions in macrophages and works through a novel mechanism involving Nrf2 actions and HO‐1. Thus PV could be considered for application as a potential therapeutic approach for inflammation‐associated disorders. © 2012 Society of Chemical Industry     

Development of a sensitivity‐improved immunoassay for the determination of carbaryl in food samples

BACKGROUND: With the aim of developing a highly sensitive immunoassay for carbaryl, a hapten which had high similarity to carbaryl was synthesised using a safer and more practical approach. After it was conjugated to horseradish peroxidase, direct competitive heterologous enzyme‐linked immunosorbent assay (CD‐ELISA) was optimised and characterised. The assay performance conditions were investigated in details. Enhanced chemiluminescence ELISA (ECL‐ELISA) was also used in preliminary studies. RESULTS: The assay obtained an IC₅₀ value (the concentration causing 50% inhibition) of 2 µg kg^?1, which was 12‐fold more sensitive than previous results of homologous CD‐ELISA. In ECL‐ELISA, the IC₅₀ was further decreased 10‐fold to 0.2 µg kg^?1. The CD‐ELISA developed was applicable for broad conditions, and could be applied on various food samples with a more convenient pre‐treatment. Average recoveries were in a range of 88.3–101.7%. The results correlated well with those obtained using high‐performance liquid chromatography (HPLC) analysis (R² = 0.989). CONCLUSION: The ELISA developed was a great improvement in the determination of carbaryl, showing that the immunoassay developed was a simple, rapid and efficient method that was reliable for the detection of carbaryl and suitable for rapid quantitative or qualitative determination in food samples. Copyright © 2010 Society of Chemical Industry     

ANTIFUNGAL,AFLATOXIN INHIBITORY AND FREE RADICAL‐SCAVENGING ACTIVITIES OF SOME MEDICINAL PLANTS EXTRACTS

ABSTRACT

The antifungal, aflatoxin inhibitory and antioxidant activity of methanol–aqueous extract (2:1) of 62 medicinal plants was explored. Based on the antifungal results, the extracts of 25 plants showed more than 50% antifungal activity and were further investigated for their aflatoxin inhibition and antioxidant properties. Methanol–aqueous extracts of Phyllanthus emblica and Terminalia chebula fruits caused 100% inhibition of aflatoxin production by the toxigenic strain of Aspergillus flavus in semisynthetic medium at 1 mg/mL. In addition, P. emblica (IC₅₀ = 4.1 µg/mL) and T. chebula (IC₅₀ = 6.9 µg/mL) fruits extracts exhibited strong antioxidant activity during the 2,2‐diphenyl‐1‐picrylhydrazyl radical‐scavenging assay in comparison with butylated hydroxytoluene (IC₅₀ = 8.1 µg/mL) and butylated hydroxyanisole (IC₅₀ = 6 µg/mL).

PRACTICAL APPLICATIONS

Based on the results of the present study, methanol–aqueous extracts of Phyllanthus emblica and Terminalia chebula, being endowed with strong antifungal, aflatoxin inhibitory and antioxidant activity, may be recommended as plant‐based preservatives for the enhancement of shelf life of food items and their protection from the undesirable harmful effects of molds, aflatoxin and free radical‐mediated damages.     

Large‐scale submerged fermentation of Antrodia cinnamomea for anti‐hepatoma activity

BACKGROUND: Submerged cultivation of Antrodia cinnamomea was carried out for manufacturing the fermentation product with anti‐hepatoma activity. The fermentation process was optimized for different parameters at shake flask level to obtain products with high inhibition potency against Hep G2 hepatoma cells. Scale‐up of the fermentation process was then achieved from 250 mL shake flask to 5 L, 500 L and 5‐ton fermenters. RESULTS: Glucose and malt extract were found to be the best carbon and nitrogen sources, respectively. The initial pH of 5.0 and an operating temperature of 22 °C were the best for a product with lowest IC₅₀ value. A shorter cultivation time was required when the scale of fermentation increased from 5 L to 5 tons. The reducing sugar and solids contents of the broth filtrate were correlated exponentially with the IC₅₀ of the ethanolic extract of mycelium for hepatoma cells, and the level of ergosterol in the mycelium extract follows the same profile as the increase in Hep G2 cells inhibition. CONCLUSION: When Antrodia cinnamomea is cultured in a 5‐ton fermenter, 4 weeks are required for the fermentation product to reach the highest anti‐hepatoma activity. The solid and reducing sugar contents of the broth filtrate as well as the ergosterol content in the ethanol extract of mycelium can serve as the marker during fermentation for manufacturing product with anti‐hepatoma activity. Copyright © 2008 Society of Chemical Industry     

Antioxidant and semicarbazide‐sensitive amine oxidase inhibitory activities of alginic acid hydroxamates

The commercial polysaccharides of alginic acid (medium (3500 cps, 2% solution) and low (250 cps, 2% solution) viscosities) were esterified with acidic methanol (1 mmol L^?1 HCl) at 4 °C with gentle stirring for 5 days to obtain methyl esters of medium‐viscosity alginic acid (ME‐MVA) and low‐viscosity alginic acid (ME‐LVA). These ME‐MVA and ME‐LVA were reacted with alkaline hydroxylamine to obtain medium‐viscosity alginic acid hydroxamates (MVA‐NHOH) and LVA‐NHOH. The percentages of hydroxamic acid content in MVA‐NHOH and LVA‐NHOH were calculated as 25% and 20%, respectively. The hydroxamate derivatives of alginic acid were used to test the antioxidant and semicarbazide‐sensitive amine oxidase (SSAO) inhibitory activities in comparison with original materials (MVA and LVA). The half‐inhibition concentrations, IC₅₀, of scavenging activity against 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) were 24.5 and 29.8 µg mL^?1 for MVA‐NHOH and LVA‐NHOH, respectively. However, few scavenging activities of the MVA and LVA were found at the same concentrations. The IC₅₀ of the positive control of butylated hydroxytoluene was 5 µg mL^?1. The scavenging activity of DPPH radical was pH‐dependent, and the optimal pH for both of MVA‐NHOH and LVA‐NHOH was the Tris‐HCl buffer (pH 7.9). Using electron spin resonance (ESR) to detect the activity of scavenging hydroxyl radicals, both alginic acid hydroxamates showed dose‐dependent scavenging activities, and the IC₅₀ was 90 and 92 µg mL^?1, respectively, for MVA‐NHOH and LVA‐NHOH. Both alginic acid hydroxamates also exhibited protection against hydroxyl radical‐mediated DNA damage. Both MVA‐NHOH and LVA‐NHOH showed dose‐dependent inhibitory activities against bovine SSAO (2.53 units); the IC₅₀ was 0.16 and 0.09 µg mL^?1, respectively, for MVA‐NHOH and LVA‐NHOH, compared with 3.81 µg mL^?1 of semicarbazide (positive controls). Amine oxidase activity staining also revealed that both MVA‐NHOH and LVA‐NHOH exhibited SSAO inhibitory activities. Both MVA‐NHOH and LVA‐NHOH showed mixed non‐competitive inhibition against bovine SSAO. It was found that the V′_max value was reduced and the K′_m value was either increased (added MVA‐NHOH, 0.05 µg mL^?1) or reduced (added LVA‐NHOH, 0.11 µg mL^?1) in the presence of alginic acid hydroxamate. Copyright © 2006 Society of Chemical Industry     

Accounting for co‐extractable compounds (blank correction) in spectrophotometric measurement of extractable and total‐bound proanthocyanidin in Leucaena spp

Methods to account for the spectral interference of co‐extractable compounds (blank correction) in the spectrophotometric analysis of both extractable and bound proanthocyanidin (PA) using the proanthocyanidin (butanol/HCl) assay were evaluated. Crude extractable and bound PA sample matrices of PA‐free Leucaena magnifica were used. Extractable PA blanks generated in heated 95% butanol/5% H₂O reagent underestimated the optical density (absorbance) of co‐extractable compounds by 24% (P < 0.01), whereas unheated 95% butanol/5% HCl blanks, incubated at room temperature, accurately measured the absorbance of the background matrix (P < 0.01). Current procedures that estimate bound PA concentrations using the proanthocyanidin assay produce intensely coloured background matrices. Recovery measurements from total‐bound PA extracts spiked with 1071 and 2142 µg anthocyanidin per tube indicated that existing analytical procedures that do not account for the spectral interference of co‐extractable compounds overestimated (P < 0.01) bound PA concentrations by 69 and 38% respectively. An innovative technique that generated an internal correction factor for each sample, using wavelength‐scanning spectrophotometry and non‐linear curve‐fitting computer software, was developed. This procedure recovered 100% of added anthocyanidins from bound PA matrices. © 2002 Society of Chemical Industry     

Chemical composition,antioxidant and cytotoxicity activities of the essential oils of Myristica fragrans and Morinda citrifolia

BACKGROUND: In this study the chemical composition, antioxidant activities and cytotoxic effect of the essential oils of Myristica fragrans (nutmeg) and Morinda citrifolia (mengkudu) were determined. RESULTS: Thirty‐eight compounds in nutmeg oil and six compounds in mengkudu oil were identified by gas chromatography–mass spectrometry. The free radical scavenging activity of nutmeg oil was superior of that mengkudu oil. The MTT assay of nutmeg oil on human colorectal carcinoma (HCT‐116) and human breast carcinoma (MCF‐7) cell lines showed IC₅₀ values of 78.61 and 66.45 µg mL^?1, respectively. The mengkudu oil exhibited IC₅₀ values of 91.46 and 78.15 µg mL^?1 for HCT‐116 and MCF‐7, respectively. CONCLUSION: The results showed that nutmeg oil can be developed as potent anti‐cancer and antioxidant drugs. Copyright © 2011 Society of Chemical Industry     

Polyphenols and phenolic acids from strawberry and apple decrease glucose uptake and transport by human intestinal Caco‐2 cells

The effect of polyphenols, phenolic acids and tannins (PPTs) from strawberry and apple on uptake and apical to basolateral transport of glucose was investigated using Caco‐2 intestinal cell monolayers. Substantial inhibition on both uptake and transport was observed by extracts from both strawberry and apple. Using sodium‐containing (glucose transporters SGLT1 and GLUT2 both active) and sodium‐free (only GLUT2 active) conditions, we show that the inhibition of GLUT2 was greater than that of SGLT1. The extracts were analyzed and some of the constituent PPTs were also tested. Quercetin‐3‐O‐rhamnoside (IC₅₀=31 μM), phloridzin (IC₅₀=146 μM), and 5‐caffeoylquinic acid (IC₅₀=2570 μM) contributed 26, 52 and 12%, respectively, to the inhibitory activity of the apple extract, whereas pelargonidin‐3‐O‐glucoside (IC₅₀=802 μM) contributed 26% to the total inhibition by the strawberry extract. For the strawberry extract, the inhibition of transport was non‐competitive based on kinetic analysis, whereas the inhibition of cellular uptake was a mixed‐type inhibition, with changes in both V_max and apparent K_m. The results in this assay show that some PPTs inhibit glucose transport from the intestinal lumen into cells and also the GLUT2‐facilitated exit on the basolateral side.     

Isolation of a free radical‐scavenging antioxidant from water spinach (Ipomoea aquatica Forsk)

Ipomoea aquatica Forsk, a green leafy vegetable that is a rich source of vitamins and amino acids with many health benefits, has been explored for the isolation and identification of its bioactive compounds. Activity‐guided repeated fractionation of a methanol extract on a silica gel column followed by an XAD column yielded a compound that exhibited antioxidant activity with an EC₅₀ value of 83 ± 1.02 µg ml^?1 reaction mixture. It also showed very strong lipid peroxidation‐inhibitory activity in a liposome model system with an EC₅₀ value of 72.2 ± 0.9 µg ml^?1. However, it showed negligible metal‐chelating activity. Based on UV, 2D nuclear magnetic resonance and gas chromatography/mass spectrometry studies, the compound was tentatively identified to be 7‐O‐β‐D ‐glucopyranosyl‐dihydroquercetin‐3‐O‐α‐D ‐glucopyranoside. This is the first report on the antioxidant properties of I aquatica leaf extracts. Copyright © 2005 Society of Chemical Industry     

Identification of α‐glucosidase inhibitors from a new fermented tea obtained by tea‐rolling processing of loquat (Eriobotrya japonica) and green tea leaves

BACKGROUND: A new fermented tea produced by tea‐rolling processing of loquat (Eriobotrya japonica) leaf with green tea leaf (denoted as LG tea) showed a potent antihyperglycaemic effect in maltose‐loaded rats. The aim of this study, therefore, was to identify α‐glucosidase inhibitors in the antihyperglycaemic tea product. RESULTS: LG tea had a threefold higher maltase‐inhibitory activity (IC₅₀ 0.065 mg dried extract mL^?1) than either the constituent loquat leaf or green tea alone. In addition, LG tea favourably inhibited maltase action rather than sucrase action. As a result of bio‐guided high‐performance liquid chromatography separations of LG tea, theasinensin A, theasinensin B, strictinin and 1,6‐digalloylglucose were newly identified as maltase inhibitors with IC₅₀ values of 142, 225, 398 and 337 µmol L^?1 respectively, along with previously identified catechins and theaflavins. CONCLUSION: Judging from the magnitude of the α‐glucosidase‐inhibitory contribution of each isolated compound to the overall inhibition of LG tea, catechins were the main candidates responsible for α‐glucosidase or maltase inhibition in LG tea, followed by theaflavins, theasinensins, strictinin and 1,6‐digalloylglucose. Copyright © 2010 Society of Chemical Industry     

Isolation and characterisation of a novel angiotensin I‐converting enzyme‐inhibitory peptide derived from douchi,a traditional Chinese fermented soybean food

BACKGROUND: Douchi, a traditional fermented soybean food, has recently attracted a great deal of attention owing to its superior physiological activity. In the present study the angiotensin I‐converting enzyme (ACE)‐inhibitory activity of typical douchi procured from various regions of China was analysed. An ACE‐inhibitory peptide derived from the most potent douchi was also isolated and characterised. The pattern of ACE inhibition and resistance to hydrolysis by gastrointestinal proteases of this peptide are described. RESULTS: ACE‐inhibitory activities were detected in all douchi samples, with IC₅₀ values ranging from 0.204 to 2.011 mg mL^?1. Among the douchi samples, a Mucor‐type douchi exhibited the most potent ACE‐inhibitory activity (IC₅₀ = 0.204 mg mL^?1). A novel ACE‐inhibitory peptide was then isolated from this Mucor‐type douchi using ultrafiltration followed by Sephadex G‐25 column chromatography and reverse phase high‐performance liquid chromatography. The amino acid sequence of the purified peptide was identified by Edman degradation as His‐Leu‐Pro (IC₅₀ = 2.37 µmol L^?1). The peptide is a competitive inhibitor and maintained its inhibitory activity even after incubation with some gastrointestinal proteases. CONCLUSION: The present study shows that peptides derived from soybean fermentation during douchi processing could be the main contributor to the ACE‐inhibitory activity observed. Copyright © 2009 Society of Chemical Industry     

Isolation and anti-inflammatory effect of astragalin synthesized by enzymatic hydrolysis of tea seed extract

BACKGROUND: The application of tea seed extract (TSE) has been widely investigated because of its biological activities. In this paper, two flavonol triglycosides in TSE—camelliaside A (CamA) and camelliaside B (CamB)—were subjected to hydrolysis in the presence of two commercial enzyme complexes (Pectinex^? series): Smash and Mash. RESULTS: Smash hydrolyzed only the xylosyl moiety of CamB, and the main product was kaempferol diglycoside (nicotiflorin, NF). On the other hand, Mash induced the hydrolysis of both CamA and CamB, and kaempferol monoglycoside (astragalin, AS) was found to be a main product. Pure AS with > 96% purity was prepared by enzymatic hydrolysis of TSE using Mash, and the chemical structure of AS was confirmed by ¹H‐ and ¹³C‐nuclear magnetic resonance analyses. The prepared pure AS showed anti‐inflammatory activities by significantly inhibiting cellular nitrite oxide (IC₅₀ = 363 µg mL^?1), prostaglandin E₂ (IC₅₀ = 134 µg mL^?1) and interleukin‐6 production (IC₅₀ = 289 µg mL^?1) by lipopolysaccharide ‐stimulated RAW 264.7 cells. CONCLUSION: It was concluded that pure AS can be prepared by enzymatic partial hydrolysis of TSE and employed as an anti‐inflammatory material. This is the first study to address the preparation of pure AS from natural sources. Copyright © 2011 Society of Chemical Industry     

In vitro inhibitory effects of cranberry bean (Phaseolus vulgaris L.) extracts on aldose reductase, α‐glucosidase and α‐amylase

The in vitro inhibitory activities of different seed extracts prepared from cranberry bean mutant SA‐05 and its wild‐type variety Hwachia against aldose reductase, α‐glucosidase and α‐amylase were examined. The results indicated that the polyphenolics‐rich extracts obtained using 800 g kg^?1 methanol and 500 g kg^?1 ethanol demonstrated inhibitory activities against aldose reductase (IC₅₀ of 0.36–0.46 mg mL^?1) and α‐glucosidase (IC₅₀ of 1.32–1.94 mg mL^?1). The 500 g kg^?1 ethanol extracts also showed α‐amylase inhibitory activities (IC₅₀ of 70.11–80.22 μg mL^?1). Subsequent extracts, prepared further with NaCl and H₂O from precipitates of 800 g kg^?1 methanol or 500 g kg^?1 ethanol extracts, exhibited potent α‐amylase inhibitory activities (IC₅₀ of 17.68–38.68 μg mL^?1). A combination of 500 g kg^?1 ethanol extraction plus a subsequent H₂O extraction produced highest polyphenolics and α‐amylase inhibitors. The SA‐05 α‐amylase inhibitor extracts showed greater inhibitory activities than that of Hwachia. Thus, cranberry bean mutant SA‐05 is an advantageous choice for producing anti‐hyperglycaemic compounds.     

Selected bioactivities of Vaccinium berries and other fruit crops in relation to their phenolic contents

Antioxidant activity, urinary tract protective activity, and cardioprotective anti‐platelet effects are among the bioactivities associated with dietary phenolics. These bioactivities were measured in vitro in fruit extracts from seven Vaccinium species and five non‐Vaccinium species to determine their relationship to total phenolic content and to anthocyanin and proanthocyanidin content. Berries belonging to the genus Vaccinium were particularly high in antioxidant activity and urinary tract protective anti‐adhesion activity, while anti‐platelet activity varied among species. There was a positive relationship between antioxidant activity (using the oxygen radical absorbing capacity (ORAC) assay) and both the total phenolic (R² = 0.76) and anthocyanin content (R² = 0.43) of the fruit, although there was no relationship between ORAC and proanthocyanidin content. There were no relationships between anti‐adhesion activity and total phenolic content, anthocyanin content, or proanthocyanidin content. Likewise, no relationships were observed between anti‐platelet activity and total phenolic content, anthocyanin content, or proanthocyanidin content. These results suggest that while antioxidant properties are characteristic of all fruit phenolics, in vitro anti‐adhesion and anti‐platelet bioactivities may be due to less abundant phenolic subgroups. Copyright © 2007 Crown in the right of Canada and Society of Chemical Industry     

MALDI‐TOF MS characterization of proanthocyanidins from cranberry fruit (Vaccinium macrocarpon) that inhibit tumor cell growth and matrix metalloproteinase expression in vitro

Proanthocyanidin‐rich extracts were prepared by fractionation of the fruit of the North American cranberry (Vaccinium macrocarpon). In vitro growth inhibition assays in eight tumor cell lines showed that selected fractions inhibited the growth of H460 lung tumors, HT‐29 colon and K562 leukemia cells at GI₅₀ values ranging from 20 to 80 µg ml^?1. Matrix‐assisted laser desorption/ionization time‐of‐flight mass spectrometry (MALDI‐TOF MS) of one of these fractions found it to be composed of polyflavan‐3‐ols, which are primarily tetramers through heptamers of epicatechin containing one or two A‐type linkages. Whole cranberry extract and the proanthocyanidin fractions were screened for effect on the expression of matrix metalloproteinases in DU 145 prostate carcinoma cells. The expression of MMP‐2 and MMP‐9 was inhibited in response to whole cranberry extract and to a lesser degree by the proanthocyanidin fractions. Copyright © 2005 Society of Chemical Industry     

Antiproliferative effects of prenylflavonoids from hops on human colon cancer cell lines

In recent years, interest in hop‐derived constituents, especially for prenylflavonoids has grown, as they have a wide range of biological properties including antioxidant, anticarcinogenic and antimicrobial activities. Two main hop prenylflavonoids, xanthohumol and isoxanthohumol, and hop extract enriched in prenylflavonoids, were tested for their antiproliferative activities on colon cancer cell lines, HT‐29 and SW620, and a noncancerous cell line, IEC‐6. It was confirmed that both xanthohumol and isoxanthohumol inhibited cell proliferation, even at micromolar concentrations. For cell line HT‐29, the IC₅₀ was 1.2 ± 0.9 and 16.9 ± 0.9 µmol dm^?3 for xanthohumol and isoxanthohumol, respectively. Similar values were obtained for SW620 cells (2.5 ± 0.2 and 37.3 ± 3.2 µmol dm^–3). None of the pure prenylflavonoids that were tested affected the proliferation of the noncancerous cell line, IEC‐6. The effect of the hop extract containing xanthohumol was also tested for antiproliferative activities on the cancer cell lines, HT‐29 (IC₅₀ = 3.1 ± 0.2 µmol dm^–3) and SW620 (IC₅₀ = 1 ± 0.2 µmol dm^?3), and on the cell line, IEC‐6 (IC₅₀ = 65.5 ± 11.3 µmol dm^?3). The results showed a similar trend to that for pure compounds, suggesting a possible future application of hop extracts in the pharmaceutical industry. Copyright © 2014 The Institute of Brewing & Distilling     

Antioxidant and anti‐acetylcholinesterase activities of anchovy (Coilia mystus) protein hydrolysates and their memory‐improving effects on scopolamine‐induced amnesia mice

Anchovy protein hydrolysates (APHs) were prepared through hydrolysis for 2, 4 or 8 h (APH‐2, APH‐4 and APH‐8, respectively). The chemical analyses, in vitro assessments [antioxidant activity and acetylcholinesterase (AchE) inhibitory activity] and in vivo mice tests were evaluated. Results revealed that APH‐8 exhibited the strongest reducing power and AchE inhibitory capacity (IC₅₀ = 159.76 ± 0.03 mg mL^?1), which may be due to its specific amino acid composition and newly formed peptides. In addition, AchE inhibitory kinetics of amino acids suggested that lysine was featured of both competitive and noncompetitive inhibitors. Furthermore, the results of in vivo study showed that all APHs exhibited memory‐improving action on scopolamine‐induced amnesia mice especially, APH‐8, indicating that anchovy protein is a potential source for health‐promoting peptides.