Plasma-Induced Oxidation Products of (-)-Epigallocatechin Gallate with Digestive Enzymes Inhibitory Effects.

(-)-Epigallocatechin gallate (EGCG), the chief dietary constituent in green tea (Camellia sinensis), is relatively unstable under oxidative conditions. This study evaluated the use of non-thermal dielectric barrier discharge (DBD) plasma to improve the anti-digestive enzyme capacities of EGCG oxidation products. Pure EGCG was dissolved in an aqueous solution and irradiated with DBD plasma for 20, 40, and 60 min. The reactant, irradiated for 60 min, exhibited improved inhibitory properties against α-glucosidase and α-amylase compared with the parent EGCG. The chemical structures of these oxidation products 1-3 from the EGCG, irradiated with the plasma for 60 min, were characterized using spectroscopic methods. Among the oxidation products, EGCG quinone dimer A (1) showed the most potent inhibitory effects toward α-glucosidase and α-amylase with IC50 values of 15.9 ± 0.3 and 18.7 ± 0.3 µM, respectively. These values were significantly higher than that of the positive control, acarbose. Compound 1, which was the most active, was the most abundant in the plasma-irradiated reactant for 60 min according to quantitative high-performance liquid chromatography analysis. These results suggest that the increased biological capacity of EGCG can be attributed to the structural changes to EGCG in H2O, induced by cold plasma irradiation.

Structurally diverse biflavonoids from the fruits of Citrus medica L. var. sarcodactylis Swingle and their hypolipidemic and immunosuppressive activities.

The fruit of Citrus medica L. var. sarcodactylis Swingle is not only used as a traditional medicinal plant, but also served as a delicious food. Six new (3'→7″)-biflavonoids (1-6), and twelve known biflavonoid derivatives (7-18) were isolated and characterized from the fruits of C. medica L. var. sarcodactylis Swingle for the first time. Their structures were determined by extensive and comprehensive analyzing NMR, HR-ESI-MS, UV, and IR spectral data coupled with the data described in the literature. Compounds (1-18) were evaluated for their hypolipidemic activities with Orlistat as the positive control, and assayed for their immunosuppressive activities with Dexamethasone as the positive control, respectively. Among them, compounds (1-3) exhibited moderate inhibition of pancreatic lipase activity by inhibiting 68.56 ± 1.40%, 56.18 ± 1.57%, 53.51 ± 1.59% of pancreatic lipase activities at the concentration of 100 µM, respectively. Compounds (4-6) and 8 showed potent immunosuppressive activities with the IC50 values from 16.83 ± 1.32 to 50.90 ± 1.79 µM. The plausible biogenetic pathway and preliminary structure activity relationship of the selected compounds were scientifically summarized and discussed in this study.

Inhibitory Action of Date Palm (Phoenix dactylifera L.) Leaf Extract on Pancreatic Lipase and α-Amylase Activities.

<b>Background and Objective:</b> Cardiovascular Diseases (CVDs) remain the main cause of mortality globally. High cholesterol levels (hypercholesterolemia) and high blood glucose (diabetes) are among the factors that increase the risk for CVDs. Application of inhibitors for the digestive enzymes accountable for the macronutrient hydrolysis, such as carbohydrates and fats, is one of the prevalent approaches in the development of medications against CVDs. The present study was performed to examine, <i>in vitro</i>, the lipase and amylase inhibitory potential of phenolic rich extract of leaves of four date palm cultivars. <b>Materials and Methods:</b> In the current study, the research investigated the potentiality of phytochemicals extracted from leaves of four date palm cultivars (Rawthan, Rabeaa, Barny and Ajwa), collected from Al-Madinah Governorate as lipase and amylase inhibitors and as antioxidants. Moreover, the total contents of flavonoids and phenolics were assessed. <b>Results:</b> The results revealed that all the tested cultivars showed promising lipase and amylase inhibition and antioxidants capacities. However, Rawthan and Ajwa were the most powerful cultivars. <b>Conclusion:</b> Therefore, the results presented herein suggest as the earliest report, the potential use of date palm leaves as a potential source for lipase and amylase inhibitors as an approach to decrease the risk for CVDs.

Evaluation on Antidiabetic Properties of Medicinal Plants from Myanmar.

OBJECTIVES: To explore the effective and safe medicines for treating diabetes. METHODS: Hydroalcoholic extracts of 130 medicinal plants belonging to 66 families were evaluated using porcine pancreatic lipase (PPL) inhibition and glucose uptake methods together with a literature review. RESULTS: The extracts of 22 species showed the PPL inhibition activity; 18 extracts of 15 species stimulated glucose uptake in 3T3-L1 adipocytes. Among them, Mansonia gagei J.R. Drumm., Mesua ferrea L., and Centella asiatica (L.) Urb. exhibited both activities. The extracts of Caladium lindenii (André) Madison rhizomes and Azadirachta indica A. Juss. leaves presented the utmost lipase inhibitory activity with IC50 of 6.86 ± 0.25 and 11.46 ± 0.06 µg/mL, respectively. The extracts of Coptis teeta Wall. rhizomes and Croton tiglium L. seeds stimulated the maximum glucose uptake. Ten species are reported to have antidiabetic activity for the first time. Flavonoids and triterpenoids are the dominant antidiabetic compounds in selected medicinal plants from Myanmar. CONCLUSIONS: P. zeylanica, L. cubeba, H. crenulate, M. gagei, C. teeta, and M. ferrea are worthy to advance further study according to their strong antidiabetic activities and limited research on effects in in vivo animal studies, unclear chemical constitutes, and safety.

Chemical Composition Analysis Using HPLC-UV/GC-MS and Inhibitory Activity of Different Nigella sativa Fractions on Pancreatic α-Amylase and Intestinal Glucose Absorption.

Nigella sativa (NS) is a well-known plant for its various benefits and multiuse in traditional medicine. This study is aimed at investigating the chemical composition of the different NS fractions by using GC-MS for the esterified fatty acids or HPLC-UV for organic fraction and at evaluating the inhibitory effect on pancreatic α-amylase (in vitro, in vivo) and intestinal glucose absorption. Among all the investigated fractions, it was shown that they are rich with different molecules of great interest. The n-hexane fraction was characterized by the presence of linoleic acid (44.65%), palmitic acid (16.32%), stearic acid (14.60%), and thymoquinone (8.7%), while among the identified peaks in EtOH fraction we found catechin (89.03 mg/100 g DW), rutin (6.46 mg/100 g DW), and kaempferol (0.032 mg/100 g DW). The MeOH fraction was distinguished with the presence of gallic acid (19.91 mg/100 g DW), catechin (13.79 mg/100 g DW), and rutin (21.07 mg/100 g DW). Finally, the aqueous fraction was marked by the existence of different molecules; among them, we mention salicylic acid (32.26 mg/100 g DW), rutin (21.46 mg/100 g DW), and vanillic acid (3.81 mg/100 g DW). Concerning the inhibitory effect on pancreatic α-amylase, it was found that in the in vitro study, the best IC50 registered were those of EtOH (0.25 mg/ml), MeOH (0.10 mg/ml), aqueous (0.031 mg/ml), and n-hexane fraction (0.76 mg/ml), while in the in vivo study an important inhibition of α-amylase in normal and diabetic rats was observed. Finally, the percentage of intestinal glucose absorption was evaluated for all tested extracts and it was ranging from 24.82 to 60.12%. The results of the present study showed that the NS seed fractions exert an interesting inhibitory effect of α-amylase and intestinal glucose absorption activity which could be associated with the existent bioactive compounds. Indeed, these compounds can be used as antidiabetic agents because of their nontoxic effect and high efficacy.

Proteinous pancreatic lipase inhibitor is responsible for the antiobesity effect of young barley (Hordeum vulgare L.) leaf extract.

Young barley leaves (Hordeum vulgare L.) have various health effects and are employed as an ingredient in the production of health-promoting foods. Promoting antiobesity is one such health effect; however, the mechanism and bioactive compounds are unclear. In this research, young barley leaf extract (YB) was demonstrated to possess pancreatic lipase inhibitory activity. The addition of YB to a high-fat diet in mice increased fecal lipid content, indicating reduced absorption of lipids as the mechanism underlying antiobesity effect. The investigation of bioactive compounds in YB resulted in the identification of fructose-bisphosphate aldolase as a proteinous lipase inhibitor. Maximum inhibition of the protein was 45%, but inhibition was displayed at a concentration as low as 16 ng/mL, which is a characteristic inhibition compared with other reported proteinous lipase inhibitors.

Inhibition of α-glucosidase, pancreatic lipase, and antioxidant property of Myrcia hatschbachii D. Legrand containing gallic and ellagic acids / Inhibición de la α-glucosidasa, la lipasa pancreática y la propiedad antioxidante de Myrcia hatschbachii D. Legrand que contiene ácidos gálico y elágico

Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 µg/mL) and FFA (IC50: 1.14 µg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 µg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 µg/mL for EBF and 532.68 µg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.

Varias especies del género Myrcia se han utilizado en la medicina popular para tratar la diabetes. Por lo tanto, el objetivo de este trabajo fue investigar la actividad inhibitoria de la α-glucosidasa y la lipasa pancreática en el extracto crudo (EBF) y en la fracción de acetato de etilo (FFA) de Myrcia hatschbachii, así como identificar compuestos fenólicos aislados y evaluar la propiedad antioxidante y toxicidad in vitro preliminar contra Artemia salina. EBF (IC50: 3.21 µg/mL) y FFA (IC50: 1.14 µg/mL) mostraron una actividad inhibitoria superior a la acarbosa (IC50: 193.65 µg/mL). Además, mostraron efectos inhibitorios de la lipasa pancreática (IC50: 556.58 µg/mL para EBF y 532.68 µg/mL para FFA), potencial antioxidante, ausencia de toxicidad preliminar y presencia de ácidos gálico y elágico en FFA. Los resultados relevantes en la inhibición de la α-glucosidasa y la lipasa pancreática motivan nuevos estudios para el desarrollo de medicamentos a base de hierbas que ayudan en el tratamiento de pacientes diabéticos.

Chemical Constituents of the Bulbs of Scilla peruviana and Their Pancreatic Lipase Inhibitory Activity.

Scilla species are used as medicinal plants and contain lanosterol-type triterpene glycosides. The phytochemical investigation of the bulbs of Scilla peruviana led to the isolation of 17 compounds, including three new rearranged pentacyclic-lanosterol glycosides (1-3) and two new homoisoflavanone glycosides (12 and 13). The structures of the undescribed compounds were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Among the triterpene glycosides, 2, 3, and 6 showed significant pancreatic lipase inhibitory activity in a concentration-dependent manner in vitro. The oral administration of scillascilloside D-2 (6) reduced serum triglyceride levels in a dose-dependent manner in soybean oil-loaded mice.

In-vitro functional efficacy of extracts from Phyllanthus emblica, Eucalyptus globulus, Tinospora cordifolia as pancreatic lipase inhibitor and source of anti-oxidant in goat meat nuggets.

The present study was aimed to evaluate the functional efficacy of plant extracts as a source of pancreatic lipase inhibitor and antioxidant in goat meat nuggets to address the fat paradox issue of red meat. The PPLIA, antioxidant potential, and resistance against fat digestion were in the order ofPhyllanthus emblica > Eucalyptus globulus > Tinospora cordifolia.PPL inhibition activities of water and ethanolic extracts fromPhyllanthus emblicausing DNPB and Triolein as substrate were 63.76, 67.94 and 56.17 and 64.36 percent respectively whereas, TPC, DPPH RSA, FRPA were 40.82 and 59.52 (mgGAE/g), 54.89 and 59.84 (percent), 1.26 and 1.61 (OD) respectively. The average diameter of fat globules in digest was maximum (8.91 µm) withPhyllanthus emblicafruits extracts whereas; TBARs (0.347 mg MDA/Kg) and FFA (4.47 µg/g) values were lowest. This study showed that extracts from plants can act as a promising natural alternative in the development of healthy meat products.

The hydrolysis of saponin-rich extracts from fenugreek and quinoa improves their pancreatic lipase inhibitory activity and hypocholesterolemic effect.

Saponins are promising compounds for ameliorating hyperlipidemia but scarce information exists about sapogenins, the hydrolyzed forms of saponins. Saponin-rich extracts and their hydrolysates from fenugreek (FE, HFE) and quinoa (QE, HQE), and saponin and sapogenin standards, were assessed on the inhibition of pancreatic lipase and interference on the bioaccessibility of cholesterol by in vitro digestion models. All extracts inhibited pancreatic lipase (IC50 between 1.15 and 0.59 mg/mL), although the hydrolysis enhanced the bioactivity of HQE (p = 0.014). The IC50 value significantly correlated to the saponin content (r = -0.82; p = 0.001). Only the hydrolyzed extracts showed a reduction of bioaccessible cholesterol (p < 0.001) higher than that of phytosterols (35% reduction). Sapogenin standards exhibited no bioactivities, protodioscin and hederacoside C slightly inhibited the lipase (around 10%) and protodioscin reduced the bioaccessible cholesterol (23% reduction, p = 0.035). The hydrolysis process of saponin-rich extracts enhances the bioactivity and allows developing multibioactive products against pancreatic lipase and cholesterol absorption simultaneously.

Antiamylase, Antilipase, Antimicrobial, and Cytotoxic Activity of Nonea obtusifolia (Willd.) DC. from Palestine.

BACKGROUND: Medicinal plants are widely used in many cultures, traditions, and civilizations worldwide. Plants with high contents of the valuable biological compounds can efficiently cure many diseases. This study is aimed at assessing, for the first time, the anti-α-amylase, antilipase, antimicrobial, and cytotoxic activities of Nonea obtusifolia (Willd.) DC. of five extracts from Palestine. METHODS: The antimicrobial activity was estimated using well diffusion method for N. obtusifolia plant of five extracts against eight ATCC (American Type Culture Collection) and clinical isolates. The cytotoxic effects for these extracts were evaluated against HeLa (cervical) carcinoma cells using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Moreover, the lipase and α-amylase inhibitory properties were determined using standard biomedical assays. RESULTS: The acetone extract of N. obtusifolia plant showed a more potent α-amylase inhibitory compared with acarbose with IC50 values of 25.7 ± 0.08 and 28.18 ± 1.22 µg/ml, respectively. Additionally, the acetone and methanol extracts revealed moderate antilipase activity compared to orlistat with IC50 values of 30.19 ± 0.11, 33.11 ± 0.13, and 12.3 ± 0.35 µg/ml, respectively. The methylene chloride extract was found to inhibit the growth of all the tested bacterial and fungal strains and also found to have potential cytotoxic effect against HeLa cancer cell line. CONCLUSION: This research work reports for the first time the biological activity of N. obtusifolia from Palestine, and the results were promising indicating that N. obtusifolia extracts contain valuable bioactive molecules that have a potential anti-α-amylase, antilipase, antibacterial, and antifungal cytotoxic potentials. Therefore, N. obtusifolia could have a medical significance in the future.

POCU1b, the n-Butanol Soluble Fraction of Polygoni Cuspidati Rhizoma et Radix, Attenuates Obesity, Non-Alcoholic Fatty Liver, and Insulin Resistance via Inhibitions of Pancreatic Lipase, cAMP-Dependent PDE Activity, AMPK Activation, and SOCS-3 Suppression.

This study investigated the effects of the n-BuOH soluble fraction of Polygoni Cuspidati 80% ethanol extract (POCU1b) on high-fat diet (HFD)-induced obesity, non-alcoholic fatty liver (NAFL), and insulin resistance (IR) to find a safe and more effective agent. HPLC profiling of POCU1b identified seven marker compounds. POCU1b increased glycerol release, cyclic adenosine monophosphate (cAMP) level, and inhibited phosphodiesterase (PDE) activity. Seven weeks of POCU1b treatment decreased body weight gain, weight and adipocyte size in fat tissues, serum lipids, and triglyceride and lipid droplets in the livers of HFD-fed rats. POCU1b improved blood glucose, insulin sensitivity, and impaired insulin secretion in the pancreas. Further, POCU1b ameliorated adiponectin, leptin, IL-6 and TNF-α levels, increased AMPK and p-ACC expression, activated CPT-1 activity, and suppressed FAS mRNA, SOCS-3 protein expression, and NF-κB DNA-binding activity. When compared with the Xenical®-treated group, a positive group, the action of POCU1b on body weight was more effective than that of Xenical. POCU1b did not show side effects, such as oily spotting and loss of appetite. These results suggest that POCU1b possesses therapeutic or preventive potential for obesity, NAFL and IR via inhibitions of pancreatic lipase and cAMP-dependent PDE activity, AMPK activation, and SOCS-3 suppression, without oily spotting and loss of appetite.

Anti-Obesity Attributes; UHPLC-QTOF-MS/MS-Based Metabolite Profiling and Molecular Docking Insights of Taraxacum officinale.

The naturopathic treatment of obesity is a matter of keen interest to develop efficient natural pharmacological routes for disease management with low or negligible toxicity and side effects. For this purpose, optimized ultrasonicated hydroethanolic extracts of Taraxacum officinale were evaluated for antiobesity attributes. The 2,2-diphenyl-1-picrylhydrazyl method was adopted to evaluate antioxidant potential. Porcine pancreatic lipase inhibitory assay was conducted to assess the in vitro antiobesity property. Ultra-high performance chromatography equipped with a mass spectrometer was utilized to profile the secondary metabolites in the most potent extract. The 60% ethanolic extract exhibited highest extract yield (25.05 ± 0.07%), total phenolic contents (123.42 ± 0.007 mg GAE/g DE), total flavonoid contents (55.81 ± 0.004 RE/g DE), DPPH-radical-scavenging activity (IC50 = 81.05 ± 0.96 µg/mL) and pancreatic lipase inhibitory properties (IC50 = 146.49 ± 4.24 µg/mL). The targeted metabolite fingerprinting highlighted the presence of high-value secondary metabolites. Molecular-binding energies computed by docking tool revealed the possible contribution towards pancreatic lipase inhibitory properties of secondary metabolites including myricetin, isomangiferin, icariside B4, kaempferol and luteolin derivatives when compared to the standard drug orlistat. In vivo investigations revealed a positive impact on the lipid profile and obesity biomarkers of obese mice. The study presents Taraxacum officinale as a potent source of functional bioactive ingredients to impart new insights into the existing pool of knowledge of naturopathic approaches towards obesity management.

Discovery of anthocyanins from cranberry extract as pancreatic lipase inhibitors using a combined approach of ultrafiltration, molecular simulation and spectroscopy.

Obesity is a chronic disease that has been causing serious problems all over the world. However, there is a lack of available therapeutic approaches to treat obesity. The FDA-approved drug orlistat has severe side effects, such as abdominal pain, flatulence and oily stool. As the therapeutic target of orlistat is pancreatic lipase, there is an urgent need for discovery of new pancreatic lipase inhibitors from natural sources that have reduced side effects compared with orlistat. In this study, ultrafiltration in combination with molecular simulation and spectroscopy was reported as an effective approach for identifying new pancreatic lipase inhibitors from anthocyanin-rich berry sources. Using this approach, four monomeric anthocyanins cyanidin-3-O-arabinoside (C3A), cyanidin-3-O-galactoside (C3Ga), peonidin-3-O-arabinoside (Pn3A) and peonidin-3-O-galactoside (Pn3Ga) from cranberries were discovered as potent pancreatic lipase inhibitors. These four cranberry anthocyanins were shown to form hydrophobic interactions and hydrogen bonds with pocket amino acid residues in molecular docking and molecular dynamics simulations. C3A showed greater impact on secondary structures of the enzyme and showed higher binding capacity with the enzyme compared with C3Ga, Pn3A and Pn3Ga as observed by CD and fluorescence spectroscopy. The structure-activity relationships were then investigated and summarized as both the structures of the B ring and glycosyl group were related to the inhibitory activities of anthocyanins. In short, our results suggested that cranberry anthocyanins could be developed as food supplements to facilitate the prevention and treatment of obesity.

Anti-Obesity Effect of DKB-117 through the Inhibition of Pancreatic Lipase and α-Amylase Activity.

This study sought to evaluate the effects of Phaseolus multiflorus var. albus Bailey extract (PM extract) and Pleurotus eryngii var. ferulae extract (PF extract) on the inhibition of digestive enzymes and to confirm the anti-obesity effect of DKB-117 (a mixture of PM extract and PF extract) in digestive enzyme inhibition in a mouse model of obesity induced by a high-fat diet. In in vitro studies, PM extract and PF extract have increased dose-dependent inhibitory activity on α-amylase (Inhibitory concentration (IC50 value: 6.13 mg/mL)) and pancreatic lipase (IC50 value; 1.68 mg/mL), respectively. High-fat diet-induced obese mice were orally administered DKB-117 extracts at concentrations of 100, 200, and 300 mg/kg/day, while a positive control group was given orlistat (pancreatic lipase inhibitor) and Garcinia cambogia (inhibiting the enzymes needed to synthesize carbohydrates into fat) at concentrations of 40 and 200 mg/kg/day, respectively, for eight weeks. As a result, body weight, fat mass (total fat mass, abdominal fat, and subcutaneous fat) detected with microcomputed tomography, fat mass (abdominal fat and inguinal fat) after an autopsy, and liver triglyceride levels were decreased significantly in the DKB-117 (300 mg/kg/day) group compared to those in the HFD control group. Additionally, we obtained results indicating that the presence of carbohydrates was found more in the DKB-117-300 (300 mg/kg/day) group than in the HFD control group. These data clearly show that DKB-117 extracts are expected to have an anti-obesity effect through a complex mechanism that promotes carbohydrate release through the inhibition of carbohydrate-degrading enzymes while blocking lipid absorption through lipase inhibition.

Activity-guided isolation of α-amylase, α-glucosidase, and pancreatic lipase inhibitory compounds from Rhus coriaria L.

The leaves and fruits of Rhus coriaria are traditionally used in Turkey for the treatment of diabetes. The aim of the present study is to determine α-amylase, α-glucosidase, and pancreatic lipase inhibitory activities of R. coriaria leaf and fruit ethanol extracts (80%), and to isolate active compounds against these enzymes. As a result of the activity-guided isolation, the active compounds were determined as the amentoflavone, agathisflavone, and 1,2,3,4,6-penta-O-galloyl-ß-glucopyranose. Agathisflavone, amentoflavone, and penta-O-galloyl-ß-glucopyranose inhibited α-glucosidase with 11.4 ± 0.9, 11.3 ± 0.7, and 4.1 ± 0.1 µM IC50 values, respectively. Furthermore, penta-O-galloyl-ß-glucopyranose inhibited α-amylase with 6.32 ± 0.18 µM IC50 . These three compounds also significantly inhibited (P < 0.05) pancreatic lipase. The results of high-performance liquid chromatography analysis showed that penta-O-galloyl-ß-D-glycopyranose was one of the main compounds in both fruit and leaf extracts. Therefore, it may be considered that R. coriaria fruit and leaf extracts can be standardized on this substance and used in the development of both medicinal products and functional food for diabetes. PRACTICAL APPLICATION: Rhus coriaria (Sumac) is one of the plants that is well known and used around the world as a spice. It is also used against diabetes traditionally. The determination of effective compounds can lead to the standardization and development of both medicinal products and functional foods for diabetes. While the fruits of the plant are used as a spice all around the world, the leaves are generally throw away; therefore, the usage of the leaves to the food and medical industry can lead to beneficial effects on the economy.

Effect of thermal processing for rutin preservation on the properties of phenolics & starch in Tartary buckwheat achenes.

The endogenous rutin-degrading enzymes (RDEs) in Tartary buckwheat (TB) considerably limit the development of TB functional foods. In this study, three thermal treatments, including superheated steam (SS), saturated steam (ST), and far-infrared drying (FID), were used to inactivate RDEs in TB. Results showed that SS and ST could efficiently inactivate RDEs, whereas FID could not. The extractable rutin contents in TB were increased by 52.3% and 12.3% by SS and ST, respectively, with 90 s of treatment time. Furthermore, the properties of phenolics and starch were used to evaluate the influence of thermal inactivation on TB. Results showed that the soluble phenolic compounds contents in TB were significantly improved (p < 0.05) by SS. The bound phenolic compounds contents were decreased after SS and ST treatments. The change in antioxidant properties was consistent with that of phenolics and flavonoids. Besides, the starch in SS- and ST-treated TB achenes had higher relative crystallinity, setback, transition temperatures, rapidly digestible starch, and slowly digestible starch contents, but a lower ratio of 1047 cm-1/1022 cm-1, peak viscosity, breakdown, gelatinization enthalpy, and resistant starch contents, than native TB starch. In conclusion, SS was a better method for the inactivation of RDEs than ST.

Chain conformation of an acidic polysaccharide from green tea and related mechanism of α-amylase inhibitory activity.

An acidic tea polysaccharide (TPSA) isolated from green tea was fractionated using a precipitation-fractionation method into seven fractions with different molecular weights. TPSA was characterized as a hyperbranched polysaccharide with a globular homogeneous conformation by analysis of solution parameters of each fraction using static light scattering and viscosity analyses. Observation by transmission electron microscopy confirmed that TPSA occurred as globular homogeneous particles with size in the range of 20-40 nm. To simulate the branched chain segments of TPSA, four model molecules were designed based on chemical structure of TPSA. Molecular docking analysis indicated that the branched chain segments of TPSA similar to the TPSA-4 model molecule showed preferential binding to α-amylase to form the TPSA/α-amylase complex through hydrogen bonding interactions. Circular dichroism spectroscopy showed that the structure of α-amylase was not significantly affected by TPSA. The mechanism of α-amylase inhibitory activity of TPSA was simulated by molecular docking analysis. The branched chain segments of TPSA similar to the TPSA-4 model molecule likely act as a potential competitor to the starch substrate to inhibit the activity of α-amylase.

Effects of a rhizome aqueous extract of Dioscorea batatas and its bioactive compound, allantoin in high fat diet and streptozotocin-induced diabetic mice and the regulation of liver, pancreas and skeletal muscle dysfunction.

ETHNOPHARMACOLOGICAL RELEVANCE: Dysfunction of glucose metabolism is associated with the occurrence of metabolic syndromes, including type 2 diabetes mellitus (T2DM). In this study, we investigated the anti-diabetic effects of yam aqueous extract and allantoin in high-fat-diet (HFD) and streptozotocin (STZ)-induced diabetic mice and the mechanism of action on the dysfunction of the liver, pancreas, and skeletal muscle. MATERIALS AND METHODS: Male C57BL/6 mice were induced into a diabetic condition by HFD for 16 weeks and a single injection of STZ (120 mg/kg) and then orally administered yam aqueous extract (500 and 1000 mg/kg) or allantoin (20 and 50 mg/kg) once daily for 4 weeks. The changes in physiological parameters, serological parameters, and morphology of tissues were investigated. The expression levels of antioxidant enzymes, biogenetic proteins, and myogenetic proteins were determined in the liver, pancreas and skeletal muscle tissues of mice. RESULTS: The administration of yam aqueous extract and allantoin at high doses in HFD/STZ-induced diabetic mice compared with the control group significantly decreased the increase in body weight, caloric intake, and water intake. Yam aqueous extract and allantoin significantly decreased high glucose and leptin, total cholesterol, triglyceride, low-density lipoprotein-cholesterol, aspartate transaminase, alanine aminotransferase levels and increased insulin and albumin levels in the plasma of mice. Yam aqueous extract and allantoin inhibited the structural damage of the liver with regard to fat accumulation, the pancreas with atrophy of Langerhans' islets, and skeletal muscle with regard to atrophy and significantly increased the expression of antioxidant enzymes and mitochondria-mediated biogenetic factors in the liver, pancreas, and muscle tissues. In addition, Yam aqueous extract and allantoin significantly increased the expression of myogenetic proteins in skeletal muscle tissues. CONCLUSION: Our results indicated that Yam aqueous extract and allantoin improve diabetic symptoms through the regulation of oxidation and glucose imbalance in liver, pancreas, and skeletal muscle tissues in mice. These findings suggest that Yam aqueous extract and allantoin can be used as antidiabetic factors in supplementary foods and medications for T2DM patients.

Antioxidant and pancreatic lipase inhibitory effects of flavonoids from different citrus peel extracts: An in vitro study.

Obesity and oxidative damage are two important risk factors associated closely with metabolic syndrome. Utilization of functional food ingredients is considered as a feasible way to tackle these challenges. In the present study, eight representative species of citrus peel extracts (CPEs) were evaluated and compared for their flavonoid profiles, antioxidant activities, and pancreatic lipase (PL) inhibitory capacities and mechanisms. Results indicated that hesperidin, naringin, neohesperidin, narirutin and eriocitrin were the five major flavonoids in CPEs, among which hesperidin was the main active PL inhibitor. Moreover, hesperidin could interact with PL by hydrogen bonds and van der Waals forces, and the interaction would not obviously change the secondary structure of PL. Overall, ponkan peel extract, having the strongest overall antioxidant activity, the highest content of hesperidin and total phenolic compounds among all tested CPEs, is a promising natural ingredient to scavenge free radicals and manage obesity.