Carbohydrate-hydrolyzing Enzymes Research Articles

A study towards drug discovery for the management of type 2 diabetes mellitus through inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by chalcone derivatives.

The inhibition of carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, is one of the major therapeutic strategies for the treatment of type 2 diabetes mellitus. Chalcones have been recognized for their multiple biological activities, including antidiabetic properties, through unclear mechanisms. In the present work, a panel of chalcones bearing hydroxy, methoxy, methyl, nitro, chloro, fluoro and bromo substituents were evaluated against α-amylase and α-glucosidase activities, most of them for the first time. The results showed that the substitution patterns and the type of substituents of chalcones influence their inhibitory activity. The presence of hydroxy groups at C-2'- and C-4' of the A ring and at C-3 and C-4 of the B ring favors the intended effect. Chalcones holding nitro groups and chloro substituents, together with a hydroxy group in the chalcone scaffold, showed strong inhibition of the α-glucosidase activity. The present study provides related scaffolds that may serve as the basis for the design and synthesis of new structures in order to obtain the ideal antidiabetic chalcone.

Postprandial glycaemia-lowering effect of a green tea cultivar Sunrouge and cultivar-specific metabolic profiling for determining bioactivity-related ingredients

Although the major green tea catechins can inhibit the activity of carbohydrate-hydrolyzing enzymes, there is a paucity of information describing the potential of other green tea ingredients and numerous green tea cultivars. Herein, we reveled that a green tea cultivar Sunrouge significantly suppressed the postprandial blood glucose level in mice. Unlike the most representative Japanese green tea cultivar, Yabukita, the suppression by Sunrouge was observed clearly during the initial period after oral dosing of starch. Sunrouge also strongly inhibited the carbohydrate-hydrolyzing enzymes α-glucosidase and α-amylase when compared with that of Yabukita and many other cultivars. Liquid chromatography–mass spectrometry (LC–MS)-based metabolic profiling (MP) of 42 Japanese green tea cultivars was performed. Multivariate statistical analysis enabled visualization of the differences among cultivars with respect to their ability to inhibit carbohydrate-hydrolyzing activities. Analysis of metabolites, contributing to the discrimination and prediction of the bioactivity of cultivars, showed that O-methylated catechins, epicatechin-3-O-(3-O-methyl) gallate (ECG3”Me) and epigallocatechin-3-O-(3-O-methyl) gallate (EGCG3”Me), were newly identified α-glucosidase inhibitors. Such ability was also observed in epigallocatechin-3-O-gallate (EGCG), epicatechin-3-O-gallate (ECG), delphinidin-3-O-glucoside and myricetin-3-O-glucoside. The amounts of these compounds in Sunrouge were higher than that in many other cultivars. These results suggest that Sunrouge has high potential for suppressing the elevation of the postprandial blood glucose level, and an MP approach may become a valuable strategy for evaluating the anti-hyperglycemic activity of green tea and for screening its active ingredients.

Calabrian extra-virgin olive oil from Frantoio cultivar: chemical composition and health properties

Extra virgin olive oil (EVOO) plays a crucial role in the Mediterranean diet. Recently, attention has been focused on presence in EVOO of phenolic compounds, phytochemicals characterized by a series of healthy properties. This paper analyzed the phenolic profile, the inhibitory activity against carbohydrate hydrolising enzyme as well as the radical scavenging activity of EVOO obtained from Olea europea L. cv. Frantoio. Samples derived from fruits collected in four different areas: Cariati, Vaccarizzo Albanese, Montalto Uffugo, and Praia a Mare. The phenolic profile obtained by HPLC revealed the presence of hydroxytyrosol (3,4-DHPEA, between 1.2 and 5.3 mg/kg) and p-hydroxyphenylethanol or tyrosol (p-HPEA, between 1.1 and 5.4 mg/kg), as the main components. Secoiridoids and their derivatives were also found in high concentrations (3,4-DHPEA-EDA 50.3-98.4 mg/kg, p-HPEA-EDA 34.6-52.9 mg/kg). All samples showed carbohydrate-hydrolyzing enzymes inhibition. The most promising activity was observed with EVOO from Vaccarizzo Albanese (IC50 of 65.5 and 57.7 µg/ml against α-glucosidase and α-amylase, respectively). The same sample showed the highest antioxidant activity of 45.3 and 56.3 µg/ml against DPPH and ABTS radicals, respectively. This sample was richest in phenols. In conclusion, EVOO has high-level bioactive compounds and a promising antioxidant and hypoglycemic activity.

Identification of Bioactive Compound from <i>Citrus maxima</i> Fruit against Carbohydrate-Hydrolysing Enzymes

The aim of this study was to identify the bioactive compound of Citrus maxima fruit that targets the enzymes responsible for hyperglycaemia. Preliminary in vitro screening of extracts of fruit parts revealed that juicy segments (ethanol, methanol and aqueous) showed the highest inhibition towards the carbohydrate- hydrolysing enzymes. Further, juicy segment extracts were subjected to preparative HPLC for separation and isolation of compounds. After a series of separations, in vitro analysis and characterization, naringin was identified to be the bioactive compound that is responsible for inhibiting carbohydrate-hydrolysing enzyme activities. Further application, such as developing food formulations from C. maxima will benefit diabetic populations.

Update on Marine Carbohydrate Hydrolyzing Enzymes: Biotechnological Applications.

After generating much interest in the past as an aid in solving structural problems for complex molecules such as polysaccharides, carbohydrate-hydrolyzing enzymes of marine origin still appear as interesting biocatalysts for a range of useful applications in strong interdisciplinary fields such as green chemistry and similar domains. The multifaceted fields in which these enzymes are of interest and the scarce number of original articles in literature prompted us to provide the specialized analysis here reported. General considerations from modern (2016–2017 interval time) review articles are at start of this manuscript; then it is subsequently organized in sections according to particular biopolymers and original research articles are discussed. Literature sources like the Science Direct database with an optimized W/in search, and the Espacenet patent database were used.

Portulaca oleracea L. (Purslane) extracts display antioxidant and hypoglycaemic effects

Purslane (Portulaca oleracea L.) is a member of the family Portulacaceae. Due to its many health benefits, it is listed in a World Health Organization database. The aim of this work is to investigate the purslane extracts for their chemical profile and bioactivity.In this study, two different solvents (MeOH/H2O and EtOH) were applied to fresh and dried leaves. The extracts were analysed using HPLC-DAD. Phenolic acids (caffeic acid, p-coumaric acid and ferulic acid) and flavonoids (apigenin, kaempferol, luteolin, quercetin, isorhamnetin, kaempferol-3-O-glucoside and rutin) were identified in all samples. Quercetin and p-coumaric acid were the most abundant compounds. Total antioxidant activity was measured by using the ABTS and DPPH tests, and the ferric reducing antioxidant power (FRAP) assay. Hypoglycaemic properties were investigated via the inhibition of carbohydrate-hydrolysing enzymes, α-amylase and α-glucosidase.Fresh hydroalcoholic purslane extract exhibited the highest radical scavenging potential in both ABTS and DPPH test (IC50 values of 52.86 and 66.98 μg/mL, respectively), whereas dried hydroalcoholic purslane extract showed the highest α-glucosidase inhibitory potential (IC50 value of 45.05 μg/mL). Collectively these data show the health properties of this widely consumed salad plant.

Cytotoxic, kinetics of inhibition of carbohydrate-hydrolysing enzymes and oxidative stress mitigation by flavonoids roots extract of Dicoma anomala (Sond.)

Objective: To investigate the free radical scavenging, antidiabetic, kinetics and cytotoxic potentials of flavonoids extract of Dicoma anomala root by using standard methods. Methods: Antioxidant activity of the flavonoids was investigated at scavenging free radicals such as 1,1- diphenyl-2-picrylhydrazyl, nitric oxide, hydroxyl radical, reducing capabilities, 2,2-azino- bis (3-ethylbenzothiazoline-6) sulfonic acid as well as metal chelating capability at different concentrations (0.125-1.000 mg/mL) while the antidiabetic activity was evaluated via the inhibition and kinetics of carbohydrate digestive enzymes including, alpha glucosidase, sucrase and maltase. Brine shrimp lethality assay was also employed to examine the cytotoxic effects of the extract by using different range of concentrations (0.125-2.000 mg/mL). Results: The study revealed the best antioxidant activity of the extract in 1,1-diphenyl-2-picrylhydrazyl, 2,2-azino-bis (3-ethylbenzothiazoline-6) sulfonic acid and nitric oxide having IC50 values of (386.90±4.91), (736.00±38.12), (629.30±9.62) μg/mL respectively compared with quercetin (standard) with IC50 [(522.20±12.38), (1 021.00±15.61) and (1 075.00±29.35) μg/mL] respective values while it was insignificantly (P>0.05) at par with quercetin for reducing power. Similarly, the extract exhibited a moderate inhibition of alpha glucosidase (43.1%), sucrase (33.4%) and maltase (29.9%) activities which were significantly (P

Enhanced Glucose Uptake in Human Liver Cells and Inhibition of Carbohydrate Hydrolyzing Enzymes by Nordic Berry Extracts

A Western lifestyle with low physical activity and a diet rich in sugar, fat and processed food contribute to higher incidences of diabetes and obesity. Enhanced glucose uptake in human liver cells was observed after treatment with phenolic extracts from different Nordic berries. All berry extracts showed higher inhibition against α-amylase and α-glucosidase than the anti-diabetic agent acarbose. Total phenolic content and phenolic profiles in addition to antioxidant activities, were also investigated. The berries were extracted with 80% methanol on an accelerated solvent extraction system (ASE) and then purified by C-18 solid phase extraction (SPE). Among the ASE methanol extracts, black chokeberry, crowberry and elderberry extracts showed high stimulation of glucose uptake in HepG2 cells and also considerable inhibitory effect towards carbohydrate hydrolyzing enzymes. SPE extracts with higher concentrations of phenolics, resulted in increased glucose uptake and enhanced inhibition of α-amylase and α-glucosidase compared to the ASE extracts. Crowberry and cloudberry were the most potent 15-lipoxygenase inhibitors, while bog whortleberry and lingonberry were the most active xanthine oxidase inhibitors. These results increase the value of these berries as a component of a healthy Nordic diet and have a potential benefit against diabetes.

Enzymatic action mechanism of phenolic mobilization in oats (Avena sativa L.) during solid-state fermentation with Monascus anka

This work aims to investigate the effects of carbohydrate-hydrolysing enzymes on the release of phenolics in oat fermentation with Monascus anka. There were good correlations between phenolic content and α-amylase, xylanase and FPase activities. A high level of α-amylase activity (141.07 U/g) was observed, while xylanase (2.40 U/g), total cellulase (0.52 U/g) and β-glucosidase activities (0.028 U/g) were relatively low in the fermentation system. The phenolic content of oat powder treated with crude enzyme from fermented oats significantly increased, especially that of the ferulic acid in the insoluble fraction and the vanillic acid in the soluble fraction. The surface SEM morphology of the oats showed that the cell wall structure was damaged by the crude enzyme treatment, which led to the release of phenolics. This study could provide metabolic understanding for optimization of phenolic compounds which could more efficiently increase the nutrition of oat intended for functional food ingredients.

Polyphenols from guaraná after in vitro digestion: Evaluation of bioacessibility and inhibition of activity of carbohydrate-hydrolyzing enzymes

Guaraná (Paullinia cupana) is a typical product from Amazon biota that exerts antioxidant capacity due to the presence of phenolic compounds, such as catechin, epicatechin and proanthocyanidins. The objective of this study was to evaluate the potential inhibitory activity of guaraná extracts, after digestion in vitro, on carbohydrates-metabolism enzymes and to assess the bioacessibility of guaraná polyphenols. The guaraná samples before and after enzymatic digestion, were compared for total phenolic content and phenolic profile. Furthermore, we investigated the uptake of polyphenols from guarana, using Caco-2 cells, and the effect of digested guaraná on carbohydrate metabolism enzymes. The amount of total phenolic compounds extracted from guaraná decreased after digestion in vitro, and native phenolics were not identified after cell permeation. On the other hand, polyphenols from guaraná were able to inhibit α-glucosidase and α-amylase activities. In conclusion, guaraná can be considered as a dietary source with anti-hyperglycemic potential.

Effect of clarified Brazilian native fruit juices on postprandial glycemia in healthy subjects

Brazilian native fruits have been shown as excellent sources of polyphenols which are associated with multiple biological activities including inhibition of carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase. Postmeal blood glucose elevations and high glycemic index diets can play a major role in the development of type 2 diabetes, therefore alternative approaches to reduce postprandial hyperglycemia are of growing interest in order to reduce diabetes risk. Here we investigated the effect of six Brazilian native clarified fruit juices from Amazon, Savannah and Atlantic Forest biomes on postprandial glycemia after consumption of a carbohydrate meal. For this, 23 healthy subjects were selected to consume seven meal tests, with a 1-week interval among them, consisting in 50g white bread plus 300mL of water (control) or cambuci, cagaita, maracujá-alho, cupuaçu, camu-camu and jaboticaba clarified fruit juices. The results showed that serum glucose concentrations were significantly lower after consumption of cambuci, cagaita, camu-camu and jaboticaba juices, whereas maracujá-alho and cupuaçu juices did not decrease the amount of glucose absorbed, compared to control (p<0.05). In addition, cagaita, cambuci, cupuaçu and jaboticaba juices increased the oxygen radical absorbance capacity in plasma, whereas all juices augmented the ferric reducing ability of plasma, except for cambuci (p<0.05). These results indicate that juices from Brazilian native fruits may be considered as adjuvant treatment for reduction of postprandial glycemia in healthy subjects.

Effect of Extracts of Bilberries (Vaccinium myrtillus L.) on Amyloglucosidase and α-Glucosidase Activity.

Vaccinium myrtillus L. is a species belonging to the genus Vaccinium of the family Ericaceae. Bilberries have drawn attention due to the multiple benefits for the human health, including antioxidant, anti-inflammatory, anticancer, anti-neurodegenerative, and cardioprotective effects. Recently, bilberries were shown to inhibit the activity of carbohydrate-hydrolysing enzymes that can help reduce the intensity of the metabolic syndrome and prevent type 2 diabetes. In this study, we investigated the α-glucosidase and amyloglucosidase inhibitory activities of polyphenol-rich extracts from fruit of Vaccinium myrtillus L. from different regions in Bulgaria. The total phenolic content was determined spectrophotometrically using the Folin-Ciocalteu method. With HPLC analysis, phenolic acid composition of extracts was assessed. Enzymatic inhibitory activities were determined according to the methodology by Borooah et al. (1961), and Dewi et al. (2007). Amyloglucosidase assay and α-glucosidase assay were used to measure the inhibition potential of bilberries' extracts. Phenolic compound content ranged from 1299.60 mg to 510.88 mg GAE/100 g for organic extracts and from 453.63 mg to 290.83 mg GAE/100 g for aqueous extracts. Based on qualitative HPLC analyses, gallic acid and chlorogenic acid were found to be among the major phenolic acids present in bilberries. Methanol and aqueous extracts there were found to be effective inhibitors of α-glucosidase with an IC50 value of 20 μg GAE/ml and 55 μg GAE/ml, respectively. The inhibitory activity of bilberries' extracts towards α-glucosidase offers the patients with type 2 diabetes the opportunity to manage their own glycaemic levels with a diet.

Ruta chalepensis L. (Rutaceae) leaf extract: chemical composition, antioxidant and hypoglicaemic activities

Ruta chalepensis L. (Rutaceae) leaf extract was investigated for its chemical profile and antioxidant and hypoglycaemic properties. The antioxidant effects were investigated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), β-carotene bleaching, and metal chelating activity assays. The carbohydrate-hydrolysing enzymes inhibition assay was used to test the hypoglycaemic potential. R. chalepensis showed a high content of hesperidin and rutin with values of 591.9 and 266.7 mg/g dry extract, respectively. The extract exhibited a promising protection of lipid peroxidation (IC50 value of 16.9 μg/mL) and inhibited both α-amylase and α-glucosidase enzymes in a concentration-dependent manner. The highest activity was found against α-amylase (IC50 value of 69.0 μg/mL). The obtained results support the use of R. chalepensis leaves as healthy food ingredients.

α-Glucosidase inhibitor produced by an endophytic fungus, Xylariaceae sp. QGS 01 from Quercus gilva Blume

Xylariaceae sp. QGS 01, an endophytic fungus isolated from the stem of Quercus gilva Blume showed high α-glucosidase inhibitory activity. α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to postpone absorption of glucose in the digestive organs. The α-glucosidase inhibitor constituents were isolated from the ethyl acetate extract of the mycellium of endophytic fungi Xylariaceae sp. QGS 01 using a bioassay-guided fractionation technique. Further separation and purification of the active fraction led to the isolation of constituents with strong inhibitory activities against α-glucosidase: 8-hydroxy-6,7-dimethoxy-3-methylisocoumarine (1) with inhibitory concentration (IC50) values against α-glucosidase from Saccharomyces cerevisiae of 41.75μg/mL, while quercetin as the standard had an IC50 value of 4.80μg/mL. The results of the present study showed that the endophytic fungus Xylariaceae sp. QGS 01 is potentially a rich source of antidiabetic medicine.

Chemical Composition, Antioxidant and α-Glucosidase-Inhibiting Activities of the Aqueous and Hydroethanolic Extracts of Vaccinium myrtillus Leaves.

Vaccinium myrtillus (bilberry) leaf is traditionally used in southeastern Europe for the treatment of diabetes. In the present study, the ability of bilberry leaf extracts to inhibit carbohydrate-hydrolyzing enzymes and restore glutathione concentration in Hep G2 cells subjected to glucose-induced oxidative stress was investigated. A comprehensive analysis of the antioxidant activity of two bilberry leaf extracts was performed. The aqueous extract showed excellent total antioxidant and chelating activity. Its antioxidant activity in the β-carotene-linoleic acid assay was very good, reaching the activity of the antioxidant standard BHA (93.4 ± 2.3% vs. 95.1 ± 2.4%, respectively). The hydroethanolic extract (ethanol/H2O, 8:2, v/v), on the other hand, was a better radical scavenger and Fe2+ reducing agent. Furthermore, the aqueous extract was able to efficiently increase glutathione concentration in Hep G2 cells subjected to glucose-induced oxidative stress and restore it to the levels observed in non-hyperglycaemic cells. The hydroethanolic extract strongly inhibited α-glucosidase, with the IC50 statistically equal to the antidiabetic drug acarbose (0.29 ± 0.02 mg/mL vs. 0.50 ± 0.01 mg/mL, respectively). Phytochemical analysis revealed the presence of quercetin and kaemferol derivatives, as well as chlorogenic and p-coumaric acid. The study results indicate that V. myrtillus leaf may have promising properties as a supporting therapy for diabetes.

Polyphenolic Compounds and Digestive Enzymes: In Vitro Non-Covalent Interactions.

The digestive enzymes–polyphenolic compounds (PCs) interactions behind the inhibition of these enzymes have not been completely studied. The existing studies have mainly analyzed polyphenolic extracts and reported inhibition percentages of catalytic activities determined by UV-Vis spectroscopy techniques. Recently, pure PCs and new methods such as isothermal titration calorimetry and circular dichroism have been applied to describe these interactions. The present review focuses on PCs structural characteristics behind the inhibition of digestive enzymes, and progress of the used methods. Some characteristics such as molecular weight, number and position of substitution, and glycosylation of flavonoids seem to be related to the inhibitory effect of PCs; also, this effect seems to be different for carbohydrate-hydrolyzing enzymes and proteases. The digestive enzyme–PCs molecular interactions have shown that non-covalent binding, mostly by van der Waals forces, hydrogen binding, hydrophobic binding, and other electrostatic forces regulate them. These interactions were mainly associated to non-competitive type inhibitions of the enzymatic activities. The present review emphasizes on the digestive enzymes such as α-glycosidase (AG), α-amylase (PA), lipase (PL), pepsin (PE), trypsin (TP), and chymotrypsin (CT). Existing studies conducted in vitro allow one to elucidate the characteristics of the structure–function relationships, where differences between the structures of PCs might be the reason for different in vivo effects.

Phenolic Elderberry Extracts, Anthocyanins, Procyanidins, and Metabolites Influence Glucose and Fatty Acid Uptake in Human Skeletal Muscle Cells.

Uptake of glucose and fatty acids in skeletal muscle is of interest for type 2 diabetes treatment. The aim was to study glucose and fatty acid uptake in skeletal muscle cells, antioxidant effects, and inhibition of carbohydrate-hydrolyzing enzymes by elderberries. Enhanced glucose and oleic acid uptake in human skeletal muscle cells were observed after treatment with phenolic elderberry extracts, anthocyanins, procyanidins, and their metabolites. The 96% EtOH and the acidified MeOH extracts were highly active. Of the isolated substances, cyanidin-3-glucoside and cyanidin-3-sambubioside showed highest stimulation of uptake. Phloroglucinol aldehyde was most active among the metabolites. Isolated anthocyanins and procyanidins are strong radical scavengers and are good inhibitors of 15-lipoxygenase and moderate inhibitors of xanthine oxidase. As α-amylase and α-glucosidase inhibitors, they are considerably better than the positive control acarbose. The antidiabetic property of elderberry phenolics increases the nutritional value of this plant and indicates potential as functional food against diabetes.

Fatty Acid Profiling and In Vitro Antihyperglycemic Effect of Leucas cephalotes (Roth) Spreng via Carbohydrate Hydrolyzing Enzyme Inhibition.

Background:Leucas cephalotes has been used by many tribes to treat variety of diseases and known to have many essential secondary metabolites. To the best of our knowledge, it is the first comparative analysis of total fatty acid (FA) composition and α-amylase inhibition activity of L. cephalotes.Objective:The present study is carried out to explore the antihyperglycemic activity and FA contents of all parts of L. cephalotes.Material and Method:Fruits, leaves, stems, and roots part of L. cephalotes have been extracted in ethanol. Simultaneously, all plant parts have been extracted in hexane with Soxhlet extraction. Ethanolic extracts have been evaluated for antihyperglycemic activity and hexane extract have been analyzed for FA identification.Result:The present study indicated that ethanolic extract of fruit and leaves have shown significant α-amylase inhibitory activity with IC50 value of 92.86 ± 0.89 and 98.09 ± 0.69 μg/mL, respectively. FA composition of all the parts of L. cephalotes was analyzed by GC/MS. Nineteen FAs have been identified in all parts of L. cephalotes in which palmitic acid, oleic acid, linolenic acid, and linoleic acid were major FAs.Conclusion:The study indicates that L. cephalotes has significant potential to inhibit α-amylase enzyme and it is a rich source of essential FAs.SUMMARY L. cephalotes has significant antidiabetic activity and will be beneficial for diabetic patients to reduce the starch breakdown and helps in reduction of postprandial hyperglycemia. It can be used in the formulation of diabetic drugs.L. cephalotes is rich source of essential FAs and may be used as a nutraceutical.Ethanol extract of fruits and leaves of L. cephalotes are showed the maximum α-amylase inhibition when compared with standard drug acarbose. Abbreviations used: DM: Diabetes Mellitus, FA: Fatty Acid, FFAs: Free Fatty Acids, FAME: Fatty Acid Methyl Ester, IC50: Inhibitor Concentration, GC-MS: Gas Chromatography- Mass Spectrophotometer

α-Glucosidase Inhibitory Activity of Selected Malaysian Plants.

Diabetes is a common metabolic disease indicated by unusually high plasma glucose level that can lead to major complications such as diabetic neuropathy, retinopathy, and cardiovascular diseases. One of the effective therapeutic managements of the disease is to reduce postprandial hyperglycemia through inhibition of α-glucosidase, a carbohydrate-hydrolyzing enzyme to retard overall glucose absorption. In recent years, a plenty of research works have been conducted looking for novel and effective α-glucosidase inhibitors (AGIs) from natural sources as alternatives for the synthetic AGI due to their unpleasant side effects. Plants and herbs are rich with secondary metabolites that have massive pharmaceutical potential. Besides, studies showed that phytochemicals such as flavonoids, alkaloids, terpenoids, anthocyanins, glycosides, and phenolic compounds possess significant inhibitory activity against α-glucosidase enzyme. Malaysia is a tropical country that is rich with medicinal herbs. In this review, we focus on eight Malaysian plants with the potential as AGI to develop a potential functional food or lead compounds against diabetes.

Functional Properties of Partially Characterized Polysaccharide from the Medicinal Mushroom Ganoderma neo-japonicum (Agaricomycetes).

This study was conducted to evaluate the mycochemical composition and antiglycemic and antioxidant activities of Ganoderma neo-japonicum hot aqueous extracts, prepared at different boiling durations, and polysaccharides isolated from them. Ground basidiocarps of G. neo-japonicum were double-boiled at 100°C for 0.5, 3, or 4 hours, and the antiglycemic activity was assessed by α-amylase and α-glucosidase enzyme inhibition assays. The antioxidant capacity of the crude hot aqueous extracts (AE-1, AE-2, AE-3) was assessed by DPPH and ABTS radical scavenging and ferric-reducing antioxidant power assays. The total phenolics, protein, and sugar in the crude extracts were also determined. The hot aqueous extract (AE-3) containing a significant amount of total sugar and having enhanced antiglycemic and antioxidant activities was selected for polysaccharide isolation. The isolated crude polysaccharide was separated and purified using diethylaminoethyl-cellulose-52 and Sepharose 6B column chromatography. Fourier transform infrared spectroscopy studies of the purified polysaccharide fraction (PF) showed the presence of typical bands corresponding to polysaccharides. The estimated β-glucan concentration in the PF was 39.26%. In general, the PF exhibited significantly lower antioxidant activity than AE-3. Nevertheless, its potency in inhibiting carbohydratehydrolyzing enzymes may have potential in the management of diabetes mellitus.