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.     

Effects of micronisation on the characteristics and physicochemical properties of insoluble fibres

The effects of micronisation on the characteristics and physicochemical properties of (a) an insoluble fibre‐rich fraction (IFRF) prepared from orange peel and (b) cellulose were studied and compared. The results showed that micronisation techniques such as ball milling, jet milling and high‐pressure micronisation could effectively (P < 0.05) reduce particle sizes to microscale, decrease the bulk density and improve the physicochemical properties (water‐holding capacity, swelling capacity, oil‐holding capacity, cation exchange capacity and glucose adsorption capacity) of IFRF and cellulose to different extents (up to 25‐fold). After micronisation the inhibitory effects of these insoluble fibres towards α‐amylase and pancreatic lipase were significantly increased (up to 5.8‐ and 7.8‐fold respectively) and a redistribution of some fibre components from insoluble to soluble fractions was observed. It was concluded that these micronisation treatments, especially high‐pressure micronisation, could effectively improve the functionalities of IFRF and cellulose, which might then be used as potential fibre‐rich ingredients in functional food applications. Copyright © 2006 Society of Chemical Industry     

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.     

Tiliroside, a glycosidic flavonoid, inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract

Scope Recent studies have reported that tiliroside, a glycosidic flavonoid, possesses anti‐diabetic activities. In the present study, we investigated the effects of tiliroside on carbohydrate digestion and absorption in the gastrointestinal tract. Methods and results This study showed that tiliroside inhibits pancreatic α‐amylase (IC₅₀ = 0.28 mM) in vitro. Tiliroside was found as a noncompetitive inhibitor of α‐amylase with K_i values of 84.2 μM. In male ICR mice, the increase in postprandial plasma glucose levels was significantly suppressed in the tiliroside‐administered group. Tiliroside treatment also suppressed hyperinsulinemia after starch administration. Tiliroside administration inhibited the increase of plasma glucose levels in an oral glucose tolerance test, but not in an intraperitoneal glucose tolerance test. In human intestinal Caco‐2 cells, the addition of tiliroside caused a significant dose‐dependent inhibition of glucose uptake. The inhibitory effects of both sodium‐dependent glucose transporter 1 (SGLT1) and glucose transporter 2 (GLUT2) inhibitors (phlorizin and phloretin, respectively) on glucose uptake were significantly inhibited in the presence of tiliroside, suggesting that tiliroside inhibited glucose uptake mediated by both SGLT1 and GLUT2. Conclusion These findings indicate that the anti‐diabetic effects of tiliroside are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract.     

Improvement of the functionality of a potential fruit insoluble fibre by micron technology

An insoluble food fibre was micronised to different microsizes (6.77–29.5 μm) by three different micron technologies using optimised conditions. The effects of different micronisation treatments and particle sizes on the characteristics and various physicochemical properties of this insoluble fibre were studied. As particle size decreased, the bulk density of the insoluble fibre was significantly (P < 0.05) decreased. A redistribution of fibre components from insoluble to soluble fractions was observed. The treatments, especially the high‐pressure micronisation, effectively (P < 0.05) increased the physicochemical properties (e.g. water‐holding capacity, swelling capacity, oil‐holding capacity, cation‐exchange capacity and glucose‐adsorption capacity) and also the inhibitory activity towards α‐amylase and pancreatic lipase of the insoluble fibre to different extent (from several up to c. fifteenfold). Our results suggested that micronisation treatments would provide an opportunity to improve the functionality of the insoluble fibre and exploit its potential applications as a functional ingredient in fibre‐rich products.     

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.     

Screening grape seeds recovered from winemaking by‐products as sources of reducing agents and mammalian α‐glucosidase and α‐amylase inhibitors

Grape seeds collected from vinification of various grape varieties were extracted by supercritical CO₂ for oil recovery. The defatted residues thus obtained were considered as a re‐utilisable co‐product and assessed for phenolic content, reducing capacity and inhibitory activities against mammalian α‐amylase and α‐glucosidase enzymes. Supercritical CO₂ treatment led to higher recovery of anthocyanins. Reducing capacity of phenolic extracts reached up to ~2200 mmolFe(II) kg^?1, much higher than that of various natural phenolic sources. The anthocyanin‐rich extracts showed the highest inhibitory effectiveness towards α‐glucosidase (I₅₀ value equal to ~40 μg gallic acid equivalents (GAE)/mL ~ half than acarbose). Inhibitory effectiveness towards α‐amylase activity was similar among grape varieties, with I₅₀ values comparable to that of acarbose and correlated with proanthocyanidin contents. These results could pave the way for an efficient processing of grapes, including cascade processes, namely: winemaking, oil extraction from recovered grape seeds and phenolic extraction from defatted grape seeds as potential cost‐effective nutraceuticals.     

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.     

Isolation of a Recombinant Bacillus sp. TS‐23 α‐Amylase by Adsorption‐Elution on Raw Starch

A Bacillus sp. TS‐23 α‐amylase produced by recombinant Escherichia coli was adsorbed onto raw starch and the adsorbed enzyme was eluted with maltose or maltodextrin in 50 mM Tris/HCl buffer (pH 8.5). The adsorption‐elution procedure resulted in a yield of 53% α‐amylase activity and sodium dodecyl sulfate‐polyacrylamide gel electrophoresis (SDS/PAGE) analysis showed that the eluted α‐amylase had a molecular mass of approximately 64 kDa. Raw starch could be used repeatedly in the adsorption‐ elution cycle with good reproducibility. Scanning electron microscopy of the isolated corn starch exhibited a smooth appearance of the granules before adsorption and only a small change in appearance after three adsorption‐elution cycles. These results suggest that the raw starch adsorption‐elution technique has a great potential in the isolation of Bacillus sp. TS‐23 α‐amylase from the culture broth of recombinant E. coli.     

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.     

Water‐holding capacity of insoluble fibre decreases free water and elevates digesta viscosity in the rat

BACKGROUND: The relationships between possible physiological properties of insoluble fibre and the viscosity of digesta are poorly understood. The aim of this study was to investigate the effect of insoluble fibres with different water‐holding capacity, swelling, oil‐holding capacity and cation exchange capacity on gastric, small intestinal and caecal contents in rats fed a semi‐purified diet containing either no fibre (control), 50 g kg^?1 tossa jute fibre or 50 g kg^?1 shiitake fibre. RESULTS: The water‐holding capacity, swelling, oil‐holding capacity and cation exchange capacity of insoluble fibres of tossa jute were higher than those of shiitake (P < 0.001). The order of the viscosities of digesta was control group < shiitake fibre group < tossa jute fibre group in gastric, small intestinal and caecal contents (P < 0.05). The digesta viscosity at a shear rate of 40 s^?1 was strongly correlated with the free water content of digesta (r = ? 0.89; P < 0.01). The free water content of digesta depended on the water‐holding capacity of insoluble fibres represented as a linear function with negative slope (P < 0.001). CONCLUSION: The viscosity of digesta depends on the free water content, and this is reduced by fibre that holds water and can swell. Copyright © 2008 Society of Chemical Industry     

Three Citrus flavonoids retard the digestion of starch and its working mechanisms

In this work, the effects of three Citrus flavonoids (naringin, neohesperidin and hesperidin) on α‐amylase catalysed starch digestion were investigated. An inhibitory kinetics experiment demonstrated that they noncompetitively inhibit the activity of α‐amylase with Ki values of, respectively, 25.21 μm , 40.26 μm , 40.69 μm . Surface plasmon resonance assay showed three Citrus flavonoids can bind with starch with K_D values of, respectively, 3.98 ± 0.20 mm , 4.92 ± 0.15 mm and 5.07 ± 0.17 mm . Scanning electron microscopy indicated they can delay the retrogradation of starch. The results of 1, 1‐diphenyl‐2‐picryl hydrazyl radical assay indicate that the antioxidant activities of three Citrus flavonoids are significantly decreased by interacting with starch. These results illustrated three Citrus flavonoids that retard the digestion of starch not only through interaction with α‐amylase, but also through interaction with starch.     

Impact of α‐amylase and maltodextrin on physicochemical,functional and antioxidant capacity of spray‐dried purple sweet potato flour

BACKGROUND: Purple sweet potato flour could be used to enhance food products through colour, flavour and nutrients. Purple sweet potato flour has not yet been prepared with maltodextrin and amylase treatment using spray drying. Thus, the investigation was to evaluate the effect of various levels of maltodextrin (30 and 50 g kg^?1 w/v), amylase (3 and 7 g kg^?1 puree) and combined with maltodextrin and amylase on the physicochemical, functional and antioxidant capacity of spray dried purple sweet potato flours. RESULTS: Amylase and amylase with maltodextrin‐treated flours had a higher anthocyanin and total phenolic content than the control and maltodextrin‐treated flours. However, the antioxidant capacity was higher in the control and maltodextrin‐treated flours compared to the amylase and amylase with maltodextrin‐treated flours. The control had a higher water absorption index and lower water solubility index compared to the maltodextrin and combined with amylase and maltodextrin‐treated flours. On the other hand, maltodextrin increased whereas α‐amylase decreased the glass transition temperature. With respect to morphology, the particles of amylase‐treated flours were smaller than the control and maltodextrin‐treated flours. CONCLUSION: The results showed that good quality flour could be prepared by combining 30 g kg^?1 maltodextrin and 7 g kg^?1 amylase treatment. Copyright © 2009 Society of Chemical Industry     

Extrusion improved the physical and chemical properties of dietary fibre from bamboo shoot by-products

Bamboo shoot by-products are regarded as waste and environmental pollutant. This study aimed to improve the functional properties of dietary fibre from bamboo shoot by-products. After CO₂ extrusion, the particle size of CO₂-extruded bamboo fibre was 17.6% lower than that of the control, and its specific surface area was 2.85 times that of the control. The soluble dietary fibre content was significantly increased from 5.64 g/100 g to 11.05 g/100 g (P < 0.05), and the capacities for water holding, swelling and oil holding were remarkably improved. The cholesterol adsorption of CO₂-extruded bamboo fibre was increased from 96.54 μg g⁻¹ to 174.65 μg g⁻¹ (pH 7.0), and its nitrite ion adsorption capacity was increased from 503.33 μg g⁻¹ to 657.27 μg g⁻¹ (pH 2.0). In summary, the structural changes of bamboo fibre such as internal porosity, surface roughening and low crystallinity indicated that its functional properties were improved after CO₂ extrusion.     

Phytochemicals content,antioxidant and hypoglycaemic activities of commercial nutmeg mace (Myristica fragrans L.) and pimento (Pimenta dioica (L.) Merr.)

Commercially dried powder of nutmeg mace (Myristica fragrans) and pimento (Pimenta dioica) spices was investigated for their high performance liquid chromatography phenolic profile and their antioxidant and hypoglycaemic properties by α‐amylase and α‐glucosidase inhibition tests. Generally, mace showed the most promising activity. An interesting protection of lipid peroxidation with an IC₅₀ value of 7.7 μg mL^?1 was found. A significant result was also obtained in ferric reducing ability power assay if compared to the positive control butylated hydroxytoluene (IC₅₀ value of 68.7 μg mL^?1 vs. 63.2 μg mL^?1, respectively). Mace also exhibited the highest carbohydrate‐hydrolysing enzyme inhibitory activity with IC₅₀ values of 62.1 and 75.7 μg mL^?1 against α‐amylase and α‐glucosidase, respectively. Overall, these results support the use of these spices not only as flavouring agent but also as food preservative and functional ingredients.     

A new nanofibrillated and hydrophobic grafted dietary fibre derived from bamboo leaves: enhanced physicochemical properties and real adsorption capacity of oil

Dietary fibre (DF) has been used for enhancing health benefits for centuries. In this study, an innovative nanofibrillated cellulose (NFC) was obtained by the combined application of high‐density steam flash‐explosion and enzymatic hydrolysis of bamboo leaves. The NFC prepared in this study was characterised by long, well‐defined and distinct NFC fibres, exhibiting excellent functional properties (water retention capacity: 20 g water g^?1, swelling capacity: 97 mL g^?1, oil‐holding capacity: 13 g oil g^?1, and higher adsorption of bile acids and cholesterol). Octenyl succinic anhydride (OSA) was further successfully grafted onto the NFC to improve its hydrophobicity. Thus, the oil‐holding capacity of the NFC reached 18.5 g oil g^?1 and the adsorption of bile acids and cholesterol increased twofold. A gastrointestinal digestion experiment further showed that the nanofibrillated and hydrophobic grafted dietary fibre represented a high‐quality dietary supplement providing enhanced health benefits, highlighted by the strong ability to absorb oil. These results indicate that the OSA‐NFC has a great potential for use as a functional ingredient in food products.     

Effects of pretreatment and drying methods on molecular structure,functional properties and thermal stability of fibre powder exhibiting colour from Centella asiatica L.

Effects of pretreatment and drying methods and particle size on characteristics of fibre powder from Centella asiatica L. leaves were investigated. Thermal stability of oil‐based colour solutions was also assessed. Steaming and combined steaming and alkaline soaking resulted in the powder with more greenness and higher chlorophylls contents, while combined steaming and acid soaking yielded dark yellow powder with lower chlorophylls contents. Chemical soaking led to the powder with decreased water holding capacity and solubility. Vacuum‐drying reduced chlorophylls degradation, hence retention of the greenness of the powder. Increased particle size resulted in decreased lightness of the powder, but in increased lightness of the solutions; water and oil holding capacities of the powder increased with the particle size. Fourier transform infrared (FTIR) spectra and X‐ray diffraction (XRD) patterns of the powder corresponded to its colour and functional property changes. Colour of the solutions changed only slightly upon heating at 80 and 180 °C for 1 h.     

Drying characteristics and quality of taegeuk ginseng (Panax ginseng C.A. Meyer) using far‐infrared rays

The purpose of this study is to investigate the drying characteristics of taegeuk ginseng using a far‐infrared dryer. The dryer used for this experiment can control the drying parameters such as far‐infrared heater temperature and air velocity. The far‐infrared drying tests of taegeuk ginseng were performed using large, medium and small ginseng at an air velocity of 0.6 m s^?1, and drying chamber temperatures of 45, 55 and 65 °C. The results were compared with those of the hot‐air drying method. The drying characteristics were analysed based on factors such as drying rate, colour changes, internal tissue structure of ginseng, saponin contents and antioxidant activities, and energy consumption. In general, the hot‐air drying time was 3–3.5 days longer than that of far‐infrared drying under the same conditions. The colour changes of far‐infrared drying were also smaller than that of hot‐air drying. Far‐infrared dryer required less energy consumption about 9.67–14.8% less than that required by hot‐air drying. At the same time, the saponin and polyphenol contents of taegeuk ginseng subjected to far‐infrared drying were 1.01 mg g^?1, 7.81 mg/100 g higher than that subjected to hot‐air drying, respectively. The results showed that the far‐infrared drying increases the capacity and quality of taegeuk ginseng.     

In vitro regulation of enzymatic release of glucose and its uptake by Fenugreek microgreen and Mint leaf extract

Fenugreek microgreen and mint leaf displayed antidiabetic potential during in vitro assays including cell line‐based analysis. Aqueous fenugreek microgreen extract (FME) (2 mg mL^?1) inhibited α‐amylase by 70%. It also enhanced glucose uptake in L6 cells by 25% at 10 mg mL^?1 which further improved to 44% in the presence of insulin. On the other hand, fresh mint leaf extract (MLE) inhibited α‐glucosidase up to 90% and increased glucose uptake by 15% in HepG2 cells. Besides, both these extracts also inhibited nonenzymatic glycation of protein. FME and MLE were also found to have high levels of total phenolics, flavonoids and antioxidants which could play a possible role in the observed antidiabetic activity. As blood glucose levels in diabetes can be regulated by inhibition of enzymes regulating carbohydrate metabolism and improving glucose uptake in cells, the findings indicate a complimentary therapeutic role of these two dietary herbs in diabetes.     

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