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.     

Phytosterols in banana (Musa spp.) flower inhibit α‐glucosidase and α‐amylase hydrolysations and glycation reaction

Three phytosterols were isolated from Musa spp. flowers for evaluating their capabilities in inhibiting glucosidase and amylase activities and glycation of protein and sugar. The three phytosterols were identified as β‐sitosterol (PS1), 31‐norcyclolaudenone (PS2) and (24R)‐4α, 14α, 4‐trimethyl‐5α‐cholesta‐8, 25(27)‐dien‐3β‐ol (PS3). IC₅₀ values (the concentration of inhibiting 50% of enzyme activity) of PS1, PS2 and PS3 against α‐glucosidase were 283.67, 11.33 and 43.10 μg mL^?1, respectively. For inhibition of α‐amylase, the IC₅₀ values of PS1, PS2 and PS3 were 52.55, 76.25 and 532.02 μg mL^?1, respectively. PS1 was an uncompetitive inhibitor against α‐amylase with K_m at 5.51 μg mL^?1, while PS2 and PS3 exhibited a mixed‐type inhibition with K_m at 52.36 and 2.49 μg mL^?1, respectively. PS1 and PS2 also significantly inhibited the formation of advanced glycation end products (AGEs) in a BSA–fructose model. The results suggest that banana flower could possess the capability in prevention of the diseases associated with abnormal blood sugar and AGEs levels, such as diabetes.     

Inhibitory activity towards human α‐amylase in wheat flour and gluten

Wheat α‐amylase inhibitors (AI) have been targeted as potential triggers of noncoeliac gluten or wheat sensitivity (NCGS). The aim of this study was to determine AI activity towards α‐amylase from human source in wheat cultivars. Contrary to barley, buckwheat, or oats, high level of AI activity was found in wheat and, to a lesser extent, rye. AI activity (mean IC₅₀ = 137 μg mL^?1) did not vary with respect to ancient or recently developed wheat cultivars. Vital wheat gluten had very high and heat‐stable AI activity (mean IC₅₀ = 23 μg mL^?1), higher than wheat starch (?10 000 μg mL^?1) or acarbose (40 μg mL^?1), a medication for the management of hyperglycaemia and potentially causing digestive disorders due to the accumulation of undigested carbohydrates in the intestine. Data suggest that eating raw wheat gluten, flour or dough could pose a health risk.     

Chemical composition,antioxidant activity and anti‐lipase activity of Origanum vulgare and Lippia turbinata essential oils

This study reported the chemical composition, phenolic content, antioxidant and anti‐lipase activity of oregano and Lippia essential oils. The major compounds found in oregano essential oil were γ‐terpinene (32.10%), α‐terpinene (15.10%), p‐cymene (8.00%) and thymol (8.00%). In Lippia essential oil, α‐limonene (76.80%) and 1,8‐cineole (4.95%) represented the major compounds. Oregano essential oil had higher phenolic content (12.47 mg gallic acid mL^?1) and DPPH scavenging activity (IC₅₀ 0.357 μg mL^?1) than Lippia essential oil (7.94 mg gallic acid mL^?1 and IC₅₀ 0.400 μg mL^?1, respectively). Both essential oils had similar antioxidant indexes (about 1.2) determined by Rancimat. Moreover, oregano essential oil had also higher anti‐lipase activity (IC₅₀ 5.09 and 7.26 μg mL^?1). Higher phenolic content in the essential oils was related with higher scavenging and anti‐lipase activities. Oregano and Lippia essential oils could be used as natural antioxidants on food products.     

Tannin fraction from Ampelopsis grossedentata leaves tea (Tengcha) as an antioxidant and α‐glucosidase inhibitory nutraceutical

Leaf of Ampelopsis grossedentata is a new resource of functional foods with healthful properties. Antioxidant and α‐glucosidase inhibitory activities of water extract (made in the style of drinking), tannin fraction (TF) and dihydromyricetin (DMY) from A. grossedentata leaves were evaluated. The main component of TF was identified as gallotannins. DPPH and ABTS radical scavenging activities and reducing power of TF were superior to those of water extract, however, inferior to those of DMY. In no PBS wash protocol of cellular antioxidant activity assay, DMY and TF exhibited similarly, while in PBS wash protocol, the value of TF was higher than that of DMY. In addition, TF possessed the highest α‐glucosidase inhibitory activities (IC₅₀ = 1.94 μg mL^?1), followed by water extract (IC₅₀ = 23.10 μg mL^?1) and DMY (IC₅₀ = 72.21 μg mL^?1). The strong α‐glucosidase inhibitory activity of TF may attribute to the binding capacity to enzymes, as confirmed by fluorescence analysis.     

Anti‐acetylcholinesterase,antidiabetic, anti‐inflammatory,antityrosinase and antixanthine oxidase activities of Moroccan propolis

Biological properties of Moroccan propolis have been scarcely studied. In the present work, the total phenols and flavonoids from 21 samples of propolis collected in different places of Morocco or 3 supplied in the market were determined, as well as the in vitro capacity for inhibiting the activities of acetylcholinesterase, α‐glucosidase, α‐amylase, lipoxygenase, tyrosinase, xanthine oxidase and hyaluronidase. The results showed that samples 1 (region Fez‐Boulemane, Sefrou city) (IC₅₀ = 0.065, 0.006, 0.020, 0.050, 0.014 mg mL^?1) and 23 (marketed) (IC₅₀ = 0.018, 0.002, 0.046, 0.037, 0.008 mg mL^?1) had the best in vitro capacity for inhibiting the α‐amylase, α‐glucosidase, lipoxygenase, tyrosinase and xanthine oxidase activities, respectively. A negative correlation between IC₅₀ values and concentration of phenols, flavones and flavanones was found. These activities corresponded to the generally higher amounts of phenols and flavonoids. In the same region, propolis samples have dissimilar phenol content and enzyme inhibitory activities.     

Inhibitory potential of phenylpropanoid glycosides from Ligustrum purpurascens Kudingcha against α‐glucosidase and α‐amylase in vitro

The leaves of Ligustrum purpurascens are used in a Chinese traditional tea called small‐leaved kudingcha, which is rich in phenylpropanoid glycosides (PPGs) and has many beneficial properties. Two critical exoacting glycoside hydrolase enzymes (glucosidases) involved in carbohydrate digestion are α‐glucosidase and α‐amylase. We investigated the properties of PPGs from L. purpurascens for inhibiting α‐amylase and α‐glucosidase activity in vitro and found IC₅₀ values of 1.02 and 0.73 mg mL^?1, respectively. The patterns of inhibiting both α‐amylase and α‐glucosidase were mixed‐inhibition type. Multispectroscopy and molecular docking studies indicated that the interaction between PPGs and α‐amylase and α‐glucosidase altered the conformation of enzymes, with binding at the site close to the active site of enzymes resulting in changed enzyme activity. Our studies may help in the further health use of small‐leaved kudingcha.     

Polyphenolic composition,antioxidant and antiproliferative effects of wild and cultivated blackberries (Rubus fruticosus L.) pomace

The content of total polyphenolics, antioxidative capacity and antiproliferative activity were tested in wild and cultivated blackberry pomace. Wild blackberry pomace extract Tw2 showed the highest following contents: total polyphenolics (50.16 mg GAE g⁻¹ dw), flavonoids (7.73 mg Qc g⁻¹ dw), flavonols (6.63 mg Qc g⁻¹ dw) and total monomeric anthocyanins (13.40 mg Cy g⁻¹). Tw2 extract significantly inhibited free radicals: IC₅₀^DPPH = 127.76 μg mL⁻¹, IC₅₀^ABTS = 26.53 μg mL⁻¹ and IC₅₀ ^{˙ OH} = 168.62 μg mL⁻¹, and the growth of breast adenocarcinoma IC₅₀^MCF7 = 306.68 μg mL⁻¹ and cervix epitheloid carcinoma cell lines IC₅₀^HeLa = 315.49 μg mL⁻¹. Wild blackberry varieties had higher extraction yields, higher total polyphenolic contents and possessed stronger biological effects compared to cultivated blackberries (P < 0.05). All blackberry extracts showed high biological potential that could be attributed to high total polyphenols and flavonoids content and could be utilised as value-added functional food.     

The influence of heat treatment of chickpea seeds on antioxidant and fibroblast growth‐stimulating activity of peptide fractions obtained from proteins digested under simulated gastrointestinal conditions

This study presents the effect of heat treatment of chickpea seeds on biological activity of peptides obtained by in vitro gastrointestinal digestion. The most significant antiradical activity against ABTS^+? expressed as IC₅₀ value was observed for 3.5‐ to 7‐kDa peptide fraction from TC hydrolysate (41.01 μg mL^?1). In turn, peptide fraction of 3.5–7.0 kDa obtained from raw chickpea seeds hydrolysate showed the highest antiradical activity against DPPH^? and Fe²⁺ chelating activity with IC₅₀ value of 20.94 and 52.53 μg mL^?1, respectively. The highest Cu²⁺ chelating activity was observed for peptides obtained from TC hydrolysate (IC₅₀ = 56.60 μg mL^?1). Peptide fraction <3.5 kDa from TC hydrolysate demonstrated the most significant reducing power (0.362 A₇₀₀/μg mL^?1). The peptide fraction of 3.5–7 kDa from TC hydrolysate also showed the highest fibroblast growth‐stimulating activity. These results indicated that the heat treatment process has no significant effect on antiradical activity against DPPH^? and Fe²⁺ chelating ability of peptides.     

α-Glucosidase- and α-amylase-inhibitory activities of phlorotannins from Eisenia bicyclis

BACKGROUND: In an effort to develop alternative therapeutic agents, strong inhibitory activity against α‐glucosidase and α‐amylase was detected in Eisenia bicyclis methanolic extract. RESULTS: In this study, two phlorotannins were isolated from E. bicyclis and characterised by chromatography and nuclear magnetic resonance. The active substances were identified as fucofuroeckol A (FF) and dioxinodehydroeckol (DD). To the authors' knowledge, this is the first report of the identification of these substances in E. bicyclis. However, to date, no antidiabetic activity of FF and DD has been reported. Both phlorotannins demonstrated significant inhibitory activity against α‐glucosidase and α‐amylase. FF showed potent antidiabetic activity, with IC₅₀ values of 131.34 nmol L^?1 against α‐glucosidase and 42.91 µmol L^?1 against α‐amylase. The corresponding IC₅₀ values of DD were 93.33 nmol L^?1 and 472.7 µmol L^?1. Furthermore, kinetic analysis revealed that FF and DD exhibited non‐competitive inhibitory activity against α‐glucosidase. CONCLUSION: These results suggest that FF and DD may be candidates for the development of an antidiabetic pharmaceutical agent or food additive. Copyright © 2012 Society of Chemical Industry     

Effects of physicochemical factors and in vitro gastrointestinal digestion on antioxidant activity of R‐phycoerythrin from red algae Bangia fusco‐purpurea

R‐phycoerythrin (R‐PE) was purified from the red algae Bangia fusco‐purpurea after 35–50% ammonium sulphate fractionation followed by ion‐exchange column chromatography on DEAE‐Sepharose, resulting in a purity (A₅₆₅/A₂₈₀) ratio of 5.1. The circular dichroism spectroscopy results suggested that the structure of R‐PE is predominately helical. The antioxidant activity of R‐PE was studied and revealed changes in conformation and antioxidant activity at different temperatures and pH values. After in vitro‐simulated gastrointestinal (GI) digestion of R‐PE, the scavenging activity of ABTS radical (EC₅₀, 769.9 μg mL^?1), DPPH radical (EC₅₀, 421.9 μg mL^?1), hydroxyl radical (EC₅₀, 32.4 μg mL^?1) and reducing power (A₇₀₀ = 0.5, 625.8 μg mL^?1) were measured. Gel filtration chromatography analysis showed that the molecular weight distribution of the final GI digest that still contained high antioxidant activity was <3 kDa. Our present results indicate that digestion‐resistant antioxidant peptides of R‐PE may be obtained by in vitro GI proteinases degradation.     

Comparative study of the essential oils of three Beilschmiedia species and their biological activities

This study was designed to examine the chemical compositions of the essential oils from three Beilschmiedia species and antioxidant, antimicrobial, antityrosinase, acetylcholinesterase and anti‐inflammatory activities. The essential oils of B. kunstleri, B. maingayi, B. penangiana gave β‐caryophyllene (10.6–12.1%), β‐eudesmol (17.5–24.1%) and δ‐cadinene (17.5–28.7%) as the most abundant components respectively. The bark oil of B. maingayi showed the highest activity in β‐carotene/linoleic acid (125.9%) and phenolic content (288.2 mg GA g^?1), while B. penangiana bark oil was found to have strong activity in DPPH (IC₅₀ 84.7 μg mL^?1) and ABTS (IC₅₀ 108.3 μg mL^?1). The essential oils of B. penangiana showed the best activity against Candida glabrata with MIC value 31.3 μg mL^?1. The bark oil of B. penangiana gave 82.5% tyrosinase inhibiton. The leaf oil of B. maingayi gave the highest inhibition in AChE (66.6%) and lipoxygenase (77.0%) assay. Our findings demonstrate that the essential oils have great potential for applications in pharmaceutical and food industries.     

Assessment of chemically characterised Rosmarinus officinalis L. essential oil and its major compounds as plant‐based preservative in food system based on their efficacy against food‐borne moulds and aflatoxin secretion and as antioxidant

The study explores antifungal, anti‐aflatoxigenic and antioxidant efficacy of Rosmarinus officinalis essential oil (ROEO) and its major compounds. In addition, the mode of action of ROEO and its practical efficacy as preservative have been assessed. GC‐MS analysis of ROEO identified 16 compounds; α‐pinene, 1,8‐cineole and camphor being the major compounds. The minimum concentration for inhibition of growth and aflatoxin B₁ secretion against A. flavus (LHP‐6) was found to be 1.5, >5.0, 4.0 and 3.0 μL mL^?1 and 1.25, >5.0, 3.5 and 3.0 μL mL^?1 for ROEO, α‐pinene, 1,8‐cineole and camphor, respectively. The IC₅₀ value through DPPH analysis and percentage inhibition of linoleic acid peroxidation of ROEO were 0.042 μL mL^?1 and 71.05%, respectively. The targeted site of antifungal action of ROEO was confirmed as plasma membrane through ergosterol measurement and TEM analysis. Moreover, ROEO significantly protected Piper nigrum fruits against mould infestation upto 6 months in in vivo trial.     

Antioxidative and anti‐inflammatory potential of phenolics from purple basil (Ocimum basilicum L.) leaves induced by jasmonic,arachidonic and β‐aminobutyric acid elicitation

The study presents changes in the phenolic levels, antioxidant and anti‐inflammatory potential of purple basil leaves caused by different chemical elicitors: arachidonic acid (AA), jasmonic acid (JA) and β‐aminobutyric acid (BABA). The application of the all tested elicitors increased the concentration of phenolic compounds, including flavonoids and phenolic acids; especially, in comparison with control (457.62 μg g^?1 FW), the rosmarinic acid level significantly increased after AA and JA treatment ‐ 705.0 and 596.5 μg g^?1 FW, respectively. Phenolics from AA‐elicited plants showed the highest anti‐inflammatory activities designated as lipoxygenase (EC₅₀ = 1.67 mg FW mL^?1) and cyclooxygenase inhibition (EC₅₀ = 0.31 mg FW mL^?1). Elicitors' treatments (especially AA and JA) may be a very useful biochemical tool for improving the production of phenolic compounds in purple basil leaves.     

Screening culinary herbs for antioxidant and α‐glucosidase inhibitory activities

Twelve commonly consumed culinary herbs were assessed for their potential effect in mitigating oxidative stress and postprandial hyperglycaemia: River Mint, Vietnamese Mint, Fish Mint, Spearmint, Sweet Basil, Thai Basil, Coriander, Lemon Verbena, Vietnamese Perilla, Rice Patty, Sawtooth and Rosemary. The radical scavenging and reducing antioxidant activity of the herbs were quite variable ranging from 31–652 mg Trolox Equivalent to 35–512 mg Ferrous Equivalent per gram dried leaves, respectively. The herbs were largely inactive against pancreatic α‐amylase, but showed strong inhibitions against yeast α‐glucosidase at 100 μg Gallic Acid Equivalent (GAE) per millilitre. Vietnamese Mint is the most potent herbs with the concentration required for 50% inhibition of activity of 6.9 μg Dried Leaves per millilitre. In addition, Vietnamese Mint was the only herb that produced significant inhibition of rat intestinal α‐glucosidases, reducing activity to 29.6% at 100 μg GAE mL^?1 compared with control.     

Efficacy of Acorus calamus L. essential oil as a safe plant‐based antioxidant,Aflatoxin B1 suppressor and broad spectrum antimicrobial against food‐infesting fungi

The study explores the efficacy of Acorus calamus L. essential oil (EO) as a safe plant‐based broad spectrum antifungal, antiaflatoxin, antioxidant food additive. The oil completely inhibited the growth and toxin production of the toxigenic strain of Aspergillus flavus at 0.4 and 0.25 μL mL^?1, respectively. EO exhibited pronounced antifungal activity against sixteen food‐infesting fungal species at 0.5 μL mL^?1. The EO showed strong antioxidant efficacy (IC₅₀ 1.06 μL mL^?1) and nonphytotoxic nature on germination of chickpea seeds. The EO was found nonmammalian toxic showing high LD₅₀ (4877.4 μL kg^?1) for mice (oral, acute). The chemical profile of EO was determined through GC and GC–MS analysis. The findings strengthen the possibility of A. calamus EO as a plant‐based food additive in view of its favourable safety profile, antioxidant and antiaflatoxigenic efficacy and broad spectrum antimicrobial activity against food‐infesting fungi.     

Changes of porcine pancreas α‐amylase in activity and secondary conformations under inhibition of tea polyphenols

To investigate two‐sided functions of tea polyphenols (TP) in antinutrition and energy balance modulation, TP were extracted from Chinese green tea and used to complex porcine pancreas α‐amylase (PPA). Changes of PPA in activity and secondary conformations were analysed. Porcine pancreas α‐amylase was found sensitive to TP treatment. Tea polyphenols exhibited IC₅₀ at 0.41 mg mL^?1 against PPA and maximum inhibitory rate (98.17%) at 3.0 mg mL^?1. Tea polyphenols inhibition was concluded as noncompetitive pattern based on its unchanged Km value (0.98 mg mL^?1) for soluble starch substrate. Tea polyphenols inhibition arose from pH 1.5 to 10.14, covering gastric and intestinal environments inside body. Circular dichroism spectra analysis revealed regular changes of PPA in secondary conformations (increased proportions of α‐helix and β‐sheet) prior to its inactivation at low TP concentrations. Tea polyphenols‐inhibited PPA had distinct double‐negative peaks at 204 nm and 208 nm. Porcine pancreas α‐amylase was inactivated by TP in ways of complexation and modification of secondary conformations.     

Interaction of aqueous extracts of two varieties of Yam tubers (Dioscorea spp) on some key enzymes linked to type 2 Diabetes in vitro

This study sought to assess the effect of processing of yam flour [from white yam (Dioscorea rotundata) and water yam (Dioscorea alata)] to paste, on the antioxidant properties and inhibition of key enzymes linked to type‐2 diabetes (α‐amylase and α‐glucosidase). The phenolic content (phenol and flavonoid), antioxidant properties, α‐amylase and α‐glucosidase inhibitory properties of the aqueous extracts of the yam products were determined. Processing into paste caused significant (P < 0.05) percentage decrease in their total phenol and flavonoid content of the yam varieties. However, significant increase (P < 0.05) in the antioxidant properties of the yam varieties was observed after processing. Furthermore, the yam extracts inhibited α‐amylase and α‐glucosidase activities in vitro in a dose‐dependent parttern (1–4 mg mL^?1), however, the pasting process caused significant (P < 0.05) decrease in the α‐amylase inhibitory and α‐glucosidase inhibitory activities. Therefore, processing the yam varieties into paste (browned) could potentially increase their antioxidant capacity as well as decreasing their α‐amylase and α‐glucosidase inhibitory properties.     

The effect of enzymatic hydrolysis on the biological properties of Oenothera biennis,Borago officinalis and Nigella sativa seedcake by‐products from oil pressing

The biological properties of ethanolic (50%, v/v) extracts from Oenothera biennis, Borago officinalis, Nigella sativa seedcake before and after enzymatic hydrolysis by alpha‐amylase (EC 3.2.1.1) from Aspergillus oryzae, beta‐glucosidase (EC 3.2.1.21) and beta‐glucanase (EC 3.2.1.6) from Aspergillus niger combinations in a ratio of 1:1:1 were investigated. Total phenolic, flavonoid and reducing sugar content for O. biennis extract after enzymatic hydrolysis was, respectively, 0.5, 1.5 and 2 times higher in comparison with nonhydrolysed extract. Iron‐chelating and radical‐scavenging activity of O. biennis seedcake extract after hydrolysis (IC₅₀ = 0.076 mg mL^?1 and IC₅₀ = 0.050 mg mL^?1) was at a similar level as that nonhydrolyeed (IC₅₀ = 0.070 mg mL^?1 and IC₅₀ = 0.065 mg mL^?1). The antioxidant activity was two times higher after hydrolysis than before enzymatic hydrolysis of O. biennis seedcake extract. Also strong elastase inhibition activity has been shown to O. biennis seedcake extract before (IC₅₀ = 0.095 mg mL^?1) and after enzymatic hydrolysis (IC₅₀ = 0.07 mg mL^?1), respectively. Oenothera biennis and B. officinalis seedcake extracts before and after hydrolysis have stronger antibacterial activity against Pseudomonas aeruginosa strain in comparison with N. sativa seedcake.     

Validation of analytical method for α‐dicarbonyl compounds using gas chromatography–nitrogen phosphorous detector and their levels in alcoholic beverages

This study aimed to establish an analytical method for α‐dicarbonyl compounds (α‐DCs) including glyoxal, methylglyoxal and diacetyl, to determine the content of α‐DCs in 101 various alcoholic beverages using gas chromatography–nitrogen phosphorous detector (GC‐NPD) and to perform exposure assessment. The limit of detection and limit of quantification for α‐DCs were 0.05–0.22 and 0.15–0.70 μg g^?1, respectively. The accuracy and precision were validated in five matrices. The raspberry fruit wine had the highest value at 139.74 μg g^?1 total α‐DCs. The lowest α‐DC concentration among the beverages was detected in rice wine (Makgeolli) at 1.59 μg g^?1. The levels of α‐DCs in various samples were detected as follows: 1.59–56.68 μg g^?1 in rice wine (Makgeolli), 2.73–16.77 μg g^?1 in beer, 8.22–139.74 μg g^?1 in fruit wine and 8.17–91.56 μg g^?1 in rice wine (Cheongju). The estimated daily intake of α‐DCs in the intake‐only group and population group was calculated as 4.22–97.94 μg kg^?1 bw day^?1 and 0.28–7.13 μg kg^?1 bw day^?1, respectively.