Extraction,optimisation and characterisation of phenolics from Thymus vulgaris L.: phenolic content and profiles in relation to antioxidant,antidiabetic and antihypertensive properties

The objectives of this study were to examine varying extraction conditions of Thymus vulgaris L. as related to phenolic content and profiles of the extracts and their antioxidant, antihypertensive and antidiabetic properties. Phenolics were extracted under various conditions pertaining to free and bound phenolics, solvent type and combination of extraction time and temperature, and these extracts were evaluated in terms of their antioxidant activities and inhibitory activities of angiotensin‐converting enzyme (ACE), α‐glucosidase and α‐amylase. The acetone–water solvent mixture (1:1; v/v) produced the extract with the greatest phenolic content, antioxidant activity and inhibitory activities of ACE and α‐glucosidase. The optimal extraction temperature for maximum phenolic content and antioxidant activity associated with methanol extraction was 60 °C, whereas a lower temperature at 40 °C was required to maximise inhibitory activities for ACE, α‐glucosidase and α‐amylase. An inverse relationship was seen between antioxidant and glucosidase inhibitory activities vs. the ACE and α‐amylase inhibitory activities, which suggests the need for extractions to be directed to specific bioactivities of thyme extracts. Generally, the results indicate major differences in phenolic profiles among the tested extraction conditions with thymol as the predominant phenolic seen in most extractions, while gallic acid, rosmarinic acid or diosmin also predominated in other extracts. Extracts with the same predominant phenolic compound and similar phenolic content showed major disparities in their ACE, glucosidase and α‐amylase inhibitory activities, indicating that the major phenolic profiles of thyme extracts may not be necessarily related to the degree of inhibition of ACE, glucosidase and α‐amylase enzymes.     

ANTI-AMYLASE, ANTI-GLUCOSIDASE AND ANTI-ANGIOTENSIN I-CONVERTING ENZYME POTENTIAL OF SELECTED FOODS

α‐Amylase and α‐glucosidase have been targeted as potential avenues for modulation of postprandial hyperglycemia through mild inhibition of the enzymatic breakdown of complex carbohydrates to decrease meal‐derived glucose absorption. Water‐soluble extracts with optimized phenolic content of selected American and Asian foods were investigated for inhibitory activity against α‐amylase and α‐glucosidase, as well as angiotensin I‐converting enzyme (ACE), which has been linked to hyperglycemia‐associated hypertension. Porcine pancreatic α‐amylase (PPA) was allowed to react with each phenolic‐optimized food extract, and the derivatized enzyme–phytochemical mixtures obtained were characterized for residual amylase activity. The α‐glucosidase and ACE activities were determined in the presence of each phenolic‐optimized food extract. The amylase activity was inhibited more than the glucosidase activity in the presence of these phytochemical extracts, and more so by Asian foods than by American foods. The Asian spice ginger was found to possess strong ACE inhibitory activity in addition to significant anti‐amylase activity. The α‐amylase enzyme inhibition was positively associated with extract antioxidant activity and negatively with extract protein content. The significance of food‐grade, plant‐based amylase inhibitors for modulation of carbohydrate breakdown and control of glycemic index of foods in the context of preventing hyperglycemia and diabetes mellitus complications in the long term and ACE inhibitors for modulation of associated hypertension is hypothesized and discussed.     

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.     

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.     

INHIBITORY POTENTIAL OF WINE AND TEA AGAINST α-AMYLASE AND α-GLUCOSIDASE FOR MANAGEMENT OF HYPERGLYCEMIA LINKED TO TYPE 2 DIABETES

ABSTRACT

Natural α‐amylase and α‐glucosidase inhibitors from food‐grade plants offer an attractive strategy to manage postprandial hyperglycemia for type 2 diabetes management via control of starch breakdown and intestinal glucose absorption. In this study, four random sources of red and white wines as well as four types of teas were investigated for α‐amylase and α‐glucosidase inhibitory potential. Water extracts of black tea had the highest α‐glucosidase inhibitory activity, followed by white tea and oolong tea. All the randomly selected red wines had significant α‐glucosidase inhibitory activity compared to white wine. The α‐glucosidase inhibitory activity of the tea and wines correlated to the phenolic content, antioxidant activity and phenolic profile of the extracts. Further, these extracts had less or no α‐amylase inhibitory activity, indicating potential to overcome the side effects of undigested starch. This research has relevance for managing hyperglycemia and related oxidation‐linked dysfunction and concurrently reducing problems of undigested starch.

PRACTICAL APPLICATIONS

In this study anti‐diabetic‐relevant potential of wines and teas were confirmed in four types of red and white wines as well as four types of commonly available teas using in vitro enzyme assays for alpha‐glucosidase and alpha‐amylase inhibitory activities. In vitro inhibitory activities of these enzymes provide a strong biochemical rationale for further in vivo studies and dietary management strategy for type 2 diabetes through the control of glucose absorption. Further this phenolic antioxidant‐enriched dietary strategy using specific beverage combinations can generate a whole food profile that has the potential to reduce hyperglycemia‐induced pathogenesis and also associated complications linked to cellular oxidation stress.     

EVALUATION OF PEPPER (CAPSICUM ANNUUM) FOR MANAGEMENT OF DIABETES AND HYPERTENSION

Natural α‐amylase and α‐glucosidase inhibitors from food‐grade plants offer an attractive strategy to control postprandial hyperglycemia for type 2 diabetes management. Concurrently associated macrovascular complication of hypertension can be managed by similar extracts by inhibition of angiotensin I‐converting enzyme (ACE ). In this study, nine types of pepper were investigated for inhibitory activity against said enzymes. Several pepper extracts had high α‐glucosidase inhibitory activity, which was not correlated to total phenolic content and free radical scavenging‐linked antioxidant activity. Select extracts such as Green pepper and Long hot pepper had less or no inhibitory effect on the α‐amylase activity, which indicates the potential for reduced side effects. Among various water extracts, Yellow, Cubanelle and Red pepper had the highest ACE inhibitory activity. Therefore, combinations of pepper could be screened for dietary management of type 2 diabetes, associated hypertension and microvascular complications linked to oxidative dysfunction, and provide the basis for clinical studies.     

Molecular Weight Affected Antioxidant,Hypoglycemic and Hypotensive Activities of Cold Water Extract from Pleurotus citrinopileatus

Cold water extract of P. citrinopileatus (CWEPC) was fractioned into 4 fractions, PC‐I (<1 kDa), PC‐II (1‐3.5 kDa), PC‐III (3.5‐10 kDa), and PC‐IV (>10 kDa), by ultrafiltration. The antioxidant activities, the inhibition of pancreatic α‐amylase, intestinal α‐glucosidase, and hypertension‐linked angiotensin converting enzyme (ACE), as well as the contents of polysaccharides, protein, and phenolic compounds of 4 fractions were determined. The results showed that lower MW fractions exerted a higher antioxidant activity, which was correlated to phenolic contents. The high molecular fraction (PC‐IV) exhibited significantly higher inhibitory activity on α‐amylase, α‐glucosidase, and ACE compared to CWEPC and the other 3 lower MW fractions (<10 kDa), which was more related to protein contents. The inhibition capability of CWEPC and PC‐IV on α‐amylase activity was 1/13.4 to 1/2.7 relative to that of acarbose, respectively. Kinetic data revealed that PC‐IV fraction followed a noncompetitive inhibition pattern on α‐glucosidase activity. The study demonstrated that various MW fractions and types of components contribute to different biological functions of P. citrinopileatus and it is protein constituents but not peptides responsible for the hypoglycemic potential of CWEPC.     

Antioxidant properties of various solvent extracts of potato peel,sugar beet pulp and sesame cake

BACKGROUND: Growing interest in the replacement of synthetic food antioxidants by natural ones has fostered research on vegetable sources and screening of raw materials to identify new antioxidants. The food‐processing industry generates substantial quantities of phenolic‐rich by‐products that could be valuable natural sources of antioxidants. In this study the antioxidant properties and total phenolic, flavonoid and flavonol contents of three industrial by‐products, sugar beet pulp, sesame cake and potato peel, extracted with various solvents were examined. Since different antioxidant compounds have different mechanisms of action, several methods were used to assess the antioxidant efficacy of extracts. RESULTS: Among the six solvents tested, methanol gave the highest extract yield of potato peel and sugar beet pulp, while diethyl ether gave the highest extract yield of sesame cake. Methanol exhibited the highest extraction ability for phenolic compounds, with total phenolics amounting to 2.91, 1.79 and 0.81 mg gallic acid equivalent g^?1 dry weight in potato peel, sugar beet pulp and sesame cake extracts respectively, and also showed the strongest antioxidant capacity in the three assays used. All three methods proved that potato peel extract had the highest antioxidant activity owing to its high content of phenolic compounds and flavonoids. CONCLUSION: On the basis of the results obtained, potato peel, sugar beet pulp and sesame cake extracts could serve as natural antioxidants owing to their significant antioxidant activity. Therefore they could be used as preservative ingredients in the food and/or pharmaceutical industries. Copyright © 2009 Society of Chemical Industry     

Inhibitory Effects of Pomegranate Extracts on Recombinant Human Maltase–Glucoamylase

α‐Glucosidase inhibitors are currently used in the treatment of type 2 diabetes. In this study, we investigated the inhibitory activities of aril and pericarp extracts from pomegranates obtained various regions against recombinant human maltase–glucoamylase (MGAM). The inhibitory activities of the aril extracts tended to be stronger than those of the pericarp extracts. The Iranian aril extract was the most effective inhibitor. We investigated the polyphenol content of the pomegranate extracts using the Folin–Ciocalteu method. Among the aril extracts, the Iranian aril extract showed the highest polyphenol content. We further evaluated inhibitory activity against α‐glucosidase from the rat small intestine. Pomegranate extract used in this study showed slightly different inhibitory activities according to α‐glucosidase origin. Iranian aril extract was the most effective inhibitor of α‐glucosidases, especially recombinant human MGAM. Bioassay‐guided fractionation of the pomegranate arils led to identification of punicalagin and oenothein B as potent inhibitors of α‐glucosidase. Oenothein B showed inhibitory activity with a half‐maximal inhibitory concentration (IC₅₀) value of 174 μM. Its potency was comparable to that of the α‐glucosidase inhibitor acarbose with an IC₅₀ value of 170 μM. Dixon plot kinetic analysis of oenothein B showed a noncompetitive inhibition with a K_i value of 102 μM. These results suggest that pomegranate arils would be useful for suppressing postprandial hyperglycemia.     

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.     

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.     

Inhibitory activities of kaempferol,galangin, carnosic acid and polydatin against glycation and α‐amylase and α‐glucosidase enzymes

The activities of four natural phenolics, kaempferol, galangin, carnosic acid and polydatin in scavenging free radicals, inhibiting advanced glycation end‐product (AGE) formation, α‐amylase and α‐glucosidase and trapping methylglyoxal (MGO), were evaluated in this study. Carnosic acid and galangin had the highest activity in scavenging free radicals. Kaempferol and galangin had the greatest activity in preventing bovine serum albumin (BSA) against glycation and reducing glycated proteins. Polydatin had the greatest performance in trapping MGO to reduce glycation reaction. However, there was no significant difference for kaempferol, galangin and carnosic acid in inhibiting AGE formation by BSA‐MGO reaction. Kaempferol, galangin and carnosic acid were the competitive inhibitors for α‐amylase, while kaempferol and carnosic acid were noncompetitive inhibitors for α‐glucosidase. However, polydatin showed as a mixed noncompetitive inhibitor for both α‐amylase and α‐glucosidase. The results indicated that the four natural phenolics have potential in inhibiting AGE production and the digestive enzymatic activity with different mechanisms.     

大叶紫薇叶提取物抗氧化性能的研究

采用不同溶剂对大叶紫薇叶进行浸泡提取,计算提取率,并用FolinCiocalteu方法测定总酚含量;采用DPPH分析法和FRAP分析法评估了不同溶剂提取物的抗氧化活性,选出抗氧化活性最高的提取物添加到猪肉中,于4℃光照下贮存12d,通过测定贮存期间猪肉的TBARS值、pH值和亨特L、a、b值,评估了提取物抗脂质氧化、防腐保鲜和护色作用,并与BHT、VE、茶多酚比较。结果表明,不同溶剂提取物显示出不同的抗氧化活性,其中甲醇提取物抗氧化活性最高(高于BHT),其提取率和总酚含量也最高。大叶紫薇叶甲醇提取物在生猪肉中具有明显的抗脂质氧化和防腐保鲜的作用,且随着提取物含量的增大,抗氧化的效果增强,有明显的量效关系。     

Effect of different solvents on the chemical composition,antioxidant activity and alpha‐glucosidase inhibitory activity of hawthorn extracts

The aim was to investigate chemical composition of different extracts prepared from hawthorn fruit using 80% ethanol, 80% methanol, 80% acetone and pure deionised water, and evaluate their antioxidant and anti‐alpha‐glucosidase activities. The highest alpha‐glucosidase inhibitory activity was determined in 80% acetone extract, while the highest DPPH scavenge capacity and ferric reducing power both exhibited in deionised water extract. In the correlation analysis, polyphenols, triterpenoids, protocatechuic acid and epicatechin all contribute to the alpha‐glucosidase inhibitory activity, while flavonoids, polyphenols, vanillic acid, gallic acid, catechin and chlorogenic acid all contribute to the antioxidant activity. By HPLC‐MS, thirty six compounds were identified, and fifteen of them were found from hawthorn fruits for the first time. Our results would provide a good reference for the further study on the antidiabetes activity of hawthorn, and also support that deionised water extract has the potential to be used as ingredients of functional food products.     

Changes in the phenolic compounds and antioxidant activities of mustard leaf (<Emphasis Type="Italic">Brassica juncea</Emphasis>) kimchi extracts during different fermentation periods

This study was conducted to investigate the changes in the total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activities of 80% methanol and water extracts from mustard leaf kimchi during different fermentation periods. The methanol extract exhibited higher TPC and TFC than the water extract. Both extracts from kimchi fermented for two months showed the highest antioxidant effects against the scavenging activities of 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radicals and 2,2-azino-bis diammonium salt (ABTS) radicals. Moreover, the methanol extract from kimchi fermented for two months showed the highest nitrite scavenging activity. The highest metal (Fe²⁺) chelating effect of the methanol extract and water extract was observed after three months and one month, respectively. Caffeic acid showed the highest increase with fermentation. These findings suggest that the antioxidant activities of kimchi depend on the fermentation period. Accordingly, this study provides basic data for improving the antioxidant activity of mustard leaf kimchi through the establishment of their fermentation period.     

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

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

SOLID-STATE BIOCONVERSION OF PHENOLIC ANTIOXIDANTS FROM DEFATTED SOYBEAN POWDERS BY RHIZOPUS OLIGOSPORUS: ROLE OF CARBOHYDRATE-CLEAVING ENZYMES

Consumption of soybeans has been linked to a reduction in risk of numerous chronic diseases. The health benefits of soybean consumption have been linked to nutritionally functional phenolic compounds known as isoflavones. As the majority of plant phenolics exist naturally as glucoside‐bound moieties, we investigated the efficacy of increasing phenolic content in defatted soybean powder by fermentation with a glucosidase‐excreting fungus, Rhizopus oligosporus, and further investigated the involvement of carbohydrate‐cleaving enzymes (α‐amylase, α‐/β‐glucosidase) in phenolic antioxidant mobilization. Phenolic content increased 41% in water extracts and 255% in ethanol extracts after 10 days of fermentation, and associated with β‐glucosidase activity. The results suggest that solid‐state fermentation with R. oligosporus is an excellent strategy for increasing phenolic content in defatted soybean powder and that β‐glucosidase is the main carbohydrate‐cleaving enzyme that is required for efficient phenolic mobilization from powdered soybean. The results have potential importance for the commercial development of enzymatic strategies for utilizing the maximal phenolic potential of soybean substrates for use as nutritionally functional food ingredients.     

POTENTIAL OF SELECT YOGURTS FOR DIABETES AND HYPERTENSION MANAGEMENT

Select brands of dairy and soy yogurt, enriched with strawberry, blueberry and peach, were screened for total phenolic content, antioxidant activity and inhibition of α‐glucosidase, pancreatic α‐amylase inhibition and the angiotensin converting enzyme‐I (ACE‐I). Blueberry yogurt had the highest phenolic content in all selected brands (A, 104 µg/mL; B, 91 µg/mL; C, 105 µg/mL; D, 79 µg/mL). Blueberry yogurt also had the highest activity in terms of 1,1‐diphenyl‐2‐picrylhydrazyl scavenging activity (A, 93%; B, 82%; C, 93%; D, 80%) and α?glucosidase inhibition (A, 58%; B, 78%; C, 90%; D, 83%), which correlated to phenolic content. The α?amylase inhibitory activity was not correlated to any specific type of yogurt, whether it was plain, soy based or fruit enriched. α‐Amylase inhibition ranged from 48 to 69% in brands that were plain or soy based and/or fruit enriched. However, with ACE‐I inhibition, the highest activity was found in soy‐based and fruit‐enriched yogurts.     

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.     

α‐Glucosidase Inhibitory Activities of Fatty Acids Purified from the Internal Organ of Sea Cucumber Stichopus japonicas

α‐Glucosidase inhibitory activities of the various solvent fractions (n‐hexane, CHCl₃, EtOAc, BuOH, and water) of sea cucumber internal organ were investigated. 1,3‐Dipalmitolein (1) and cis‐9‐octadecenoic acid (2) with potent α‐glucosidase inhibitory activity were purified from the n‐hexane fraction of sea cucumber internal organ. IC₅₀ values of compounds 1 and 2 were 4.45 and 14.87 μM against Saccharomyces cerevisiae α‐glucosidase. These compounds mildly inhibited rat‐intestinal α‐glucosidase. In addition, both compounds showed a mixed competitive inhibition against S. cerevisiae α‐glucosidase and were very stable at pH 2 up to 60 min. The K_I values of compounds 1 and 2 were 0.48 and 1.24 μM, respectively. Therefore, the internal organ of sea cucumber might be a potential new source of α‐glucosidase inhibitors suitably used for prevention of obesity and diabetes mellitus.