The inhibitory effects of ethanol extracts from sorghum,foxtail millet and proso millet on α-glucosidase and α-amylase activities

Cereal crops have recently experienced increased interest due to their potential health benefits. It has been suggested that the intake of whole grain foods is beneficial to the prevention and management of diabetes mellitus. In this study, we investigated the inhibitory effect of 70% EtOH extracts from different cultivars of sorghum, foxtail millet and proso millet on α-glucosidase and α-amylase. Among the six sorghum cultivars, Mongdang-susu(SS-1), Me-susu(SS-2), Susongsaengi-susu(SS-3) and Sikyung-susu(SS-4) extracts exhibited higher inhibitory activities against α-glucosidase (IC₅₀ = 1.1–1.4 μg/ml) than acarbose, reference inhibitor (IC₅₀ = 2.1 μg/ml). In addition, these extracts strongly inhibited degradation of starch by pancreatic and salivary α-amylase, whereas extracts from foxtail and proso millets exhibited no visible or detectible inhibitory effect on α-amylase or on α-glucosidase activity. These in vitro studies indicate the potential of sorghum in the development of effective anti-diabetic agents.     

The α-amylase and α-glucosidase inhibitory effects of Irish seaweed extracts

To date, numerous studies have reported on the antidiabetic properties of various plant extracts through inhibition of carbohydrate-hydrolysing enzymes. The objective of this research was to evaluate extracts of seaweeds for α-amylase and α-glucosidase inhibitory effects. Cold water and ethanol extracts of 15 seaweeds were initially screened and from this, five brown seaweed species were chosen. The cold water and ethanol extracts of Ascophyllum nodosum had the strongest α-amylase inhibitory effect with IC₅₀ values of 53.6 and 44.7 μg/ml, respectively. Moreover, the extracts of Fucus vesiculosus Linnaeus were found to be potent inhibitors of α-glucosidase with IC₅₀ values of 0.32 and 0.49 μg/ml. The observed effects were associated with the phenolic content and antioxidant activity of the extracts, and the concentrations used were below cytotoxic levels. Overall, our findings suggest that brown seaweed extracts may limit the release of simple sugars from the gut and thereby alleviate postprandial hyperglycaemia.     

Rhus verniciflua Stokes flavonoid extracts have anti-oxidant,anti-microbial and α-glucosidase inhibitory effect

We isolated four compounds, fustin, gallic acid, 3′,4′,7-trihydroxyflavone, and fisetin from Rhus verniciflua. These compounds showed electron donation ability (87–94%) that was stronger than butylated hydroxyanisole (52%). Gallic acid (OD₇₀₀ = 1.98) showed the highest reducing power, and the other isolated compounds (OD₇₀₀ = 0.66–1.31) showed stronger activity than α-tocopherol (OD₇₀₀ = 0.21). The ethyl-acetate fraction had the highest phenolic content (723 mg GAE/g), followed by the 80% ethanolic extract (597 mg GAE/g). For Gram-negative bacteria, fisetin had the most potent anti-bacterial activity (MIC = 8 μg/ml) against Escherichia coli. 3′,4′,7-Trihydroxyflavone (106%), the 80% ethanolic extract (101%), and ethyl-acetate (98%) had the most powerful α-glucosidase inhibitory effect at 50 μg/ml. R. verniciflua extracts have potential as functional food additives.     

Inhibitory potential of trilobatin from Lithocarpus polystachyus Rehd against α-glucosidase and α-amylase linked to type 2 diabetes

The chemical structure of the sweet compound from Lithocarpuspolystachyus Rehd was identified as trilobatin on the basis of HPLC, EIS-MS and NMR analyses. The inhibitory activities of trilobatin against α-glucosidase and α-amylase were evaluated, and the inhibition mechanism was analysed with Lineweaver–Burk plots. Also the antioxidant activity evaluation of trilobatin was conducted by DPPH radical scavenging assay. Comparing with acarbose, trilobatin showed a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase. The Lineweaver–Burk plots analysis elucidated that trilobatin inhibited the enzyme non-competitively. DPPH scavenging activity of trilobatin (IC₅₀ = 0.57 mg/ml) was higher than rutin (IC₅₀ = 0.72 mg/ml), which indicated that trilobatin had a moderate antioxidant potential. These results suggest that trilobatin is a potential effective α-glucosidase inhibitor for management of postprandial hyperglycemia with less side effect, and provide strong rationale for further animal and clinical studies.     

Phenolic compounds in cowpea and horse gram flours in comparison to chickpea flour: Evaluation of their antioxidant and enzyme inhibitory properties associated with hyperglycemia and hypertension

Evaluation of phenolic contents and their in vitro bioactive functional properties of cowpea and horse gram flours in comparison to chickpea flour revealed that horse gram flour, which contain highest concentrations of total phenolics and total flavonoids was found to be the most active 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenger. Hydrogen peroxide scavenging capacity, reducing power and metal chelating abilities were significantly higher in cowpea and horse gram than chickpea flour. Phenolic extracts from flours showed distinct variations in the inhibition of enzymes associated with hyperglycemia and hypertension. Although, α-glucosidase inhibitory activity was superior in cowpea (IC₅₀ 52.8 μg/ml), α-amylase (IC₅₀ 96.4 μg/ml) and angiotensin-I converting enzyme (IC₅₀ 32.8 μg/ml) inhibitory activities were predominant in horse gram. These results provided useful information for effective utilisation of legume flours as ingredients in composite flours and for the development of food products with health promoting functions.     

Syzygium aqueum leaf extract and its bioactive compounds enhances pre-adipocyte differentiation and 2-NBDG uptake in 3T3-L1 cells

The insulin-like and/or insulin-sensitising effects of Syzygium aqueum leaf extract and its six bioactive compounds; 4-hydroxybenzaldehyde, myricetin-3-O-rhamnoside, europetin-3-O-rhamnoside, phloretin, myrigalone-G and myrigalone-B were investigated in 3T3-L1 adipocytes. We observed that, S. aqueum leaf extract (0.04–5 μg/ml) and its six bioactive compounds (0.08–10 μM) at non-cytotoxic concentrations were effectively enhance adipogenesis, stimulate glucose uptake and increase adiponectin secretion in 3T3-L1 adipocytes. Clearly, the compounds myricetin-3-O-rhamnoside and europetin-3-O-rhamnoside showed insulin-like and insulin-sensitising effects on adipocytes from a concentration of 0.08 μM. These compounds were far better than rosiglitazone and the other isolated compounds in enhancing adipogenesis, stimulating 2-NBDG uptake and increasing adiponectin secretion at all the concentrations tested. These suggest the antidiabetic potential of S. aqueum leaf extract and its six bioactive compounds. However, further molecular interaction studies to explain the mechanisms of action are highly warranted.     

α-Glucosidase inhibitors from Chinese Yam (Dioscoreaopposita Thunb.)

The inhibitory activities of crude extracts and purified constituents from the fresh tuberous rhizomes of Chinese Yam (Dioscorea opposita Thunb.), which is commonly called Huai Shan Yao in Chinese, were evaluated against yeast α-glucosidase in order to search for the active principals for treatment of diabetes. Bioassay-guiding isolation gave four compounds: trans-N-p-coumaroyltyramine (1) (IC₅₀ = 0.40 μM), 1,7-bis(4-hydroxyphenyl)heptane-3,5-diol (2) (IC₅₀ = 0.38 mM), 6-hydroxy-2,4,7-trimethoxyphenanthrene (3) (IC₅₀ = 0.77 mM) as α-glucosidase inhibitors, and cis-N-p-coumaroyltyramine (4), an isomer of compound 1, which showed no inhibitory activity against α-glucosidase. Furthermore, the separation and purification of compound 3 from Chinese Yam (Huai Shan Yao) was conducted by high-speed counter-current chromatography (HSCCC) using hexane–ethyl acetate–methanol–water (1:1:1:1, v/v/v/v). Compound 1, 2 and 4 were isolated from or detected in the Dioscoreaceae family for the first time.     

Glycosidase inhibitory phenolic compounds from the seed of Psoralea corylifolia

The seeds of Psoralea corylifolia were extracted into five different polar solvents: chloroform, 50% ethanol in water, ethanol, methanol and water. All extracts were evaluated for glycosidase inhibitory activity. The chloroform extract (CE) showed the lowest IC₅₀ values against α-glucosidase (82.9 μg/ml) and α-mannosidase (132 μg/ml). Chromatography of CE yielded nine phenolic compounds which were identified as isovabachalcone (1), 4′-O-methylbavachalcone (2), isobavachromene (3), corylifolin (4), bavachinin (5), psoralidin (6), neobavaisoflavone (7), corylifol A (8), and bakuchiol (9). All isolated compounds, apart from compound 5, possessed α-glucosidase inhibitory activities. Among them, compounds 6–8 exhibited potent inhibition with IC₅₀s of 13.7, 27.7 and 11.3 μM, respectively. Furthermore, compounds 2 and 6 showed α-mannosidase inhibitory activity. Mechanistic analysis of their inhibition modes against α-glucosidase showed that compounds (6 and 7) were noncompetitive, whereas compound 8 was mixed. Furthermore, the most active glycosidase inhibitors (2, 6–8) were proven to be present in the native seed in high quantities by an HPLC chromatogram.     

Antioxidant and hepatoprotective activity of ethanolic extract of leaves of Solidago microglossa containing polyphenolic compounds

The antioxidative and hepatoprotective potential of Solidago microglossa D.C, a widely used medicinal plant from Brazil was investigated. The leaf extract showed inhibition against thiobarbituric acid reactive species (TBARS) induced by different prooxidants (10 μM FeSO₄ and 5 μM sodium nitroprusside SNP) in rat liver, brain and phospholipid homogenates from egg yolk. Moreover, the free radical scavenging activities of the extract was evaluated by the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC_50, 3.8 ± 0.5 μg/ml) and hydroxyl radical on benzoic acid hydroxylation (IC_50, 32.3 ± 1.3 μg/ml) and deoxyribose (IC_50, 39.1 ± 2.4 μg/ml) assays. The ethanolic extract showed significant hepatoprotective activity against paracetamol (250 mg/kg) induced liver damage in mice in a dose dependent manner. The phenolic composition and their quantification by high performance liquid chromatography (HPLC) resulted in the identification of gallic acid and flavonoids: quercetrin (quercetin-3-O-rhamnoside), rutin (quercetin-3-O-rutinoside) and quercetin.     

Rambutan rind in the management of hyperglycemia

Plant extracts have been suggested as a rich as yet unexplored source of potentially useful anti-diabetic drugs. Recent scientific investigations have confirmed the efficacy of many of these preparations, as effective antioxidants; able to regenerate functional pancreatic beta cells and has a hypoglycemic potential. In this study, the exotic rambutan (Nephelium lappaceum L.) fruit's rind has been shown to be effective in inhibiting the carbohydrate hydrolyzing enzymes, alpha glucosidase (EC₅₀ = 2.7 ??g/mL) and alpha amylase (EC₅₀ = 70.8 ??g/mL), at a much more significant level than the drug acarbose (EC₅₀ = 3500 ??g/mL; alpha glucosidase; EC₅₀ = 12 ??g/mL; alpha amylase). In addition, the geraniin-enriched ethanolic extracts were able to inhibit the key enzyme in the polyol pathway, aldol reductase (EC₅₀ = 0.04 ??g/mL) and prevent the formation of advanced glycation end-products (AGE) by 43%. These findings indicate that the geraniin-standardized N. lappaceum rind may be a potential source of an anti-hyperglycemic agent.     

Isolation and characterisation of an α-glucosidase inhibitory substance from fructose–tyrosine Maillard reaction products

An α-glucosidase inhibitory substance was isolated and characterised from fructose–tyrosine Maillard reaction products (MRPs) and the inhibition mode of the active substance determined. The ethyl acetate fraction of fructose–tyrosine MRPs showed strong α-glucosidase inhibitory activity; this fraction was isolated and purified using silica gel column chromatography and semi-preparative RP-HPLC. The structure of the purified compound was determined using spectroscopic methods. The isolated compound was identified as 2,4-bis (p-hydroxyphenyl)-2-butenal (C₁₆H₁₄O₃, HPB242). This is the first report of baker’s yeast α-glucosidase inhibitory activity of HPB242 isolated from fructose–tyrosine MRPs. The IC₅₀ value of HPB242 on α-glucosidase inhibition was 4.00 ± 0.09 μg/ml. Kinetic data revealed that HPB242 inhibits the p-NPG hydrolysing activity of baker’s yeast α-glucosidase noncompetitively with a K_i value of 0.870 mM.     

α-Glucosidase inhibitors from the bulb of Eleutherine americana

One effective way to treat diabetes is by suppressing carbohydrate digestion due to the utilisation of α-glucosidase inhibitors (AGIs). The determination of prospective herbs, done in vitro by using enzyme assay, resulted in the finding of Eleutherine americana, which showed a potent inhibitory activity. A 50% aqueous methanol-soluble extract of bulbs of E. americana was chromatographed successively and the active fractions were further purified with preparative high performance liquid chromatography (HPLC) to isolate active compounds against α-glucosidase. Structure determination by mass and NMR analysis revealed that these isolated compounds were eleutherol (1), eleutherinoside A (2), and eleuthoside B (3) based on comparisons with the reference data. Considering the amount and the inhibitory activity of each naphthalene in the whole extracts, the bulb of E. americana inhibitory activity against α-glucosidase might be a result of compound 2 (IC₅₀ = 0.5 mM, yield = 5 mg/50 g plant sample, with a characteristic structure which has never been found in other AGIs. AGIs play an important role for the treatment of diabetes, therefore these results may suggest novel alternatives for diabetes treatment management.     

Inhibitory effect of raspberries on starch digestive enzyme and their antioxidant properties and phenolic composition

Seven primocane fall-bearing raspberry (Rubus idaeus L.) cultivars, Nova (red), Dinkum (red), Heritage (red), Autumn Britten (red), Josephine, Anne (yellow), Fall Gold (yellow) were analysed for potential health promoting properties including their inhibitory effect on starch and fat digestive enzymes, antioxidant activities, and phenolic composition. The tested raspberry extracts showed no detectable inhibition of pancreatic α-amylase and lipase. However, all the extracts exhibited potent inhibition of α-glucosidase with IC₅₀ from 16.8 to 34.2 μg/mL. Four phenolic compounds, ellagic acid, cyanidin-diglucoside, pelargonidin-3-rutinoside, and catechin were identified as the active α-glucosidase inhibitors. The raspberry extracts also possessed significant antioxidant activities with oxygen radical absorbance capacities (ORAC) ranging from 136.7 to 205.2 μmol Trolox equivalents (TE)/g dry weight fruit and DPPH radical scavenging activities from 305 to 351 μmol TE/g. The total phenolic content of raspberry cultivars varied significantly from 40.9 to 98.5 mg of gallic acid equivalents/g dry weight. The anthocyanin content varied widely from 0.1 to 9.5 mg cyanidin 3-glucoside equivalents/g. Nine phenolic acids were quantified in raspberries and their total amounts varied from 157.3 to 713.5 μg/g. The enzyme inhibition and antioxidant properties of raspberry cultivars were not correlated with their total phenolic, anthocyanin, and phenolic acid content. Overall, ‘Dinkum’ and ‘Josephine’ raspberry varieties possess higher total phenolic content, ORAC, DPPH radical scavenging activity, and α-glucosidase inhibitory activity than other five cultivars.     

α-Glucosidase and α-amylase inhibitory activities of guava leaves

The 75% ethanol extract from guava (Psidium guajava Linn.) leaves was extracted further, in turn, with CH₂Cl₂, EtOAc and n-BuOH to afford four fractions, CH₂Cl₂-soluble, EtOAc-soluble, n-BuOH-soluble and residual extract fractions. Both the n-BuOH-soluble and EtOAc-soluble fractions showed high inhibitory activity against α-glucosidase and α-amylase. Seven pure flavonoid compounds, quercetin (1), kaempferol (2), guaijaverin (3), avicularin (4), myricetin (5), hyperin (6) and apigenin (7), were isolated (using enzyme assay-guide fractionation method) from the n-BuOH-soluble and EtOAc-soluble fractions. The structures of these pure compounds were determined on the basis of MS and NMR data and the activities of these compounds were evaluated. Compounds 1, 2 and 5 showed high inhibitory activities, with IC₅₀ values of 3.5 mM, 5.2 mM and 3.0 mM against sucrase, with IC₅₀ values of 4.8 mM, 5.6 mM and 4.1 mM against maltase and with IC₅₀ values of 4.8 mM, 5.3 mM and 4.3 mM against α-amylase, respectively. We found that myricetin showed the most powerful activity among these compounds with a 70% inhibition against sucrase at a concentration of 1.5 mg/ml. The hydroxyl group at the 3-position on the A-ring and a number of hydroxyl groups attached to the C-ring played important roles in the inhibition activity. There was an obvious synergistic effect (the mixing action of two compounds) against α-glucosidase, but against α-amylase this was not found. This is the first study of the active compositions of guava leaves and the biological activity of the active compositions against α-glucosidase and α-amylase.     

α-Glucosidase and α-amylase inhibitory activities of Nepalese medicinal herb Pakhanbhed (Bergenia ciliata, Haw.)

Herbal medicine has been used for many years by different cultures around the world for the treatment of diabetes. The Nepalese herb Pakhanbhed, is one of the traditional remedies used for diabetes since prehistoric times. In this study, we examined the anti-diabetic activity using an in vitro model and isolated the active compounds from Pakhanbhed. Extraction and fractionation of the extract lead to the isolation of two active compounds, (−)-3-O-galloylepicatechin and (−)-3-O-galloylcatechin and these are reported from this plant species for the first time. These isolated compounds demonstrated significant dose dependent enzyme inhibitory activities against rat intestinal α-glucosidase and porcine pancreatic α-amylase. IC₅₀ value for sucrose, maltase and α-amylase were 560, 334 and 739 μM, respectively for [(−)-3-O-galloylepicatechin] and 297, 150 and 401 μM, respectively for [(−)-3-O-galloylcatechin]. Our study, for the first time, revealed the anti-diabetic potential of Pakhanbhed and this study could be helpful to develop medicinal preparations or nutraceutical and functional foods for diabetes and related symptoms.     

Novel α-glucosidase inhibitors from Macaranga tanarius leaves

One of the hyperglycaemic remedies is glucose absorption reduction by suppressing carbohydrate digestion due to utilisation of α-glucosidase inhibitors (AGIs). Determination of prospecting herbs done in vitro by using enzyme assay resulted in the finding of Macaranga tanarius, which showed a potent inhibitory activity. An EtOAc-soluble extract of M. tanarius leaves was chromatographed by a Diaion HP-20 column and the active fractions were further purified with high performance liquid chromatography (HPLC) to isolate active principles against α-glucosidase. Five ellagitannins were successfully isolated and identified. Structure determination revealed that these isolated compounds were mallotinic acid (IC₅₀ > 5.00 mM), corilagin (IC₅₀ = 2.63 mM), chebulagic acid (IC₅₀ = 1.00 mM), and two novel compounds named macatannins A (IC₅₀ = 0.80 mM) and B (IC₅₀ = 0.55 mM). AGIs play an important role for the treatment of diabetes, therefore this research results may suggest novel alternatives for diabetes treatment management.     

In vitro determination of antioxidant activity of proteins from jellyfish Rhopilema esculentum

In this study, the antioxidant activity of proteins isolated from jellyfish, Rhopilema esculentum Kishinouye (R. esculentum), was determined by various antioxidant assays, including superoxide anion radical-scavenging, hydroxyl radical-scavenging, total antioxidant activity, reducing power and metal chelating activity. Butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), α-tocopherol, vitamin C and mannitol were used as standards in those various antioxidant activities. The crude protein (CP) and the protein fractions isolated by Sephadex chromatography, first peak (FP) and second peak (SP), had very low reductive power and metal chelating abilities compared to EDTA, but they showed strong scavenging effects on the superoxide anion radical, hydroxyl radical and varying total antioxidant activity. FP and SP exhibited stronger scavenging effects on the superoxide anion radical than BHA, BHT or α-tocopherol. The EC₅₀ values of FP and SP were 6.12 and 0.88 μg/ml, respectively, while values EC₅₀ of BHA, BHT and α-tocopherol were 31, 61 and 88 μg/ml, respectively. CP, FP and SP showed far higher hydroxyl radical-scavenging activities than did vitamin C or mannitol. The EC₅₀ values of CP, FP and SP were 48.76, 45.42 and 1.52 μg/ml, but EC₅₀ values of vitamin C and mannitol were 1907 and 4536 μg/ml, respectively. In a β-carotene–linoleate system, SP and CP showed antioxidant activity, but lower than BHA. Of the three samples, SP had the strongest antioxidant activity. So, SP may have a use as a possible supplement in the food and pharmaceutical industries.     

Antioxidant and free radical scavenging activities of wild bitter melon (Momordica charantia Linn. var. abbreviata Ser.) in Taiwan

Momordica charantia Linn. var. abbreviata Ser. (Cucurbitaceae), also known as “Shan Ku Gua”, is a wild variety of bitter melon (BM) in Taiwan. The size of its fruits is only about one-fifth of the commonly seen BM. It is commonly consumed as vegetable and also used as a popular folk medicine. In this study, the antioxidant and free radical scavenging activities of BM aqueous (BM-H₂O) and ethanol (BM-EtOH) extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH), metal chelation, cytochrome c and xanthine oxidase inhibition (XOI) assays, as well as FeCl₂-ascorbic acid induced lipid peroxidation (thiobarbituric acid reactive substances, TBARS) assay in rat liver homogenates in vitro. Total flavonoid and phenol contents of BM extracts were also analyzed. Results showed that both BM-H₂O (IC₅₀=129.94 μg/ml) and BM-EtOH (IC₅₀=156.78 μg/ml) possess potent DPPH radical scavenging activity, which was better than vitamin E (IC₅₀=172.21 μg/ml). These extracts also showed better iron chelating activity than vitamin E. However, they were weaker than vitamin E in free radical scavenging, xanthine oxidase inhibitory and anti-lipid peroxidation activities. With the exception of XOI activity [IC₅₀=7.90 μg/ml (BM-H₂O) vs. 7.69 μg/ml (BM-EtOH)], BM-H₂O showed a lower IC₅₀ value in free radical scavenging [IC₅₀=6.15 μg/ml (BM-H₂O) vs. 7.08 μg/ml (BM-EtOH)] and anti-lipid peroxidation [IC₅₀=53.72 μg/ml (BM-H₂O) vs. 88.51 μg/ml (BM-EtOH) for liver; 82.53 μg/ml (BM-H₂O) vs. 91.83 μg/ml (BM-EtOH) for brain] activities than BM-EtOH. Both BM extracts showed a weak anti-lipid peroxidation activity in plasma. BM-H₂O (62.0 mg/g) possessed a significant higher concentration of total flavonoids than BM-EtOH (44.0 mg/g), but was lower in the total phenol content (BM-H₂O: 51.6 mg/g vs. BM-EtOH: 68.8 mg/g). In conclusion, BM extracts possess potent antioxidant and free radical scavenging activities. These antioxidant activities could have contributed, at least partly, to the therapeutic benefits of the certain traditional claims of wild BM.     

The influence of fruit ripening on the phytochemical content and biological activity of Capsicum chinense Jacq. cv Habanero

During the past decade, it has been reported that the consumption of certain foods and spices such as pepper may have a positive effect on health. The present study evaluates the influence of fruit ripening on total phenols, flavonoids, carotenoids and capsaicinoids content and antioxidant, hypoglycaemic and anticholinesterase activities of Capsicum chinense Jacq. cv Habanero. The chemical investigation showed a different composition between the two stages of ripening (immature and mature). Generally, the concentration of carotenoids and capsaicinoids increased as the peppers reached maturity, whereas the concentration of phenols declined. The immature fruits showed the highest radical scavenging activity (IC₅₀ of 97.14 μg/ml). On the contrary, the antioxidant activity evaluated by the β-carotene bleaching test showed a significant activity for mature peppers (IC₅₀ value of 4.57 μg/ml after 30 min of incubation). Mature peppers inhibited α-amylase with an IC₅₀ of 130.67 μg/ml. The lipophilic fractions of both mature and immature peppers exhibited an interesting and selective inhibitory activity against α-amylase with IC₅₀ values of 29.58 and 9.88 μg/ml, respectively. Both total extracts of mature and immature peppers inhibited butyrylcholinesterase selectively. The obtained results underline the potential health benefits as a result of consuming C. chinense Habanero and suggest that it could be used as new valuable flavour with functional properties for food or nutriceutical products on the basis of the high content of phytochemicals and found biological properties.     

Rapid isolation of geraniin from Nephelium lappaceum rind waste and its anti-hyperglycemic activity

Recently we confirmed the ability of ethanolic Nephelium lappaceum L. rind extract to act as anti-hyperglycemic agent. Geraniin, an ellagitannin, was identified as the major bioactive compound isolated from the ethanolic Nephelium lappaceum L. rind extract. In this study, we describe the rapid isolation of geraniin from the above plant. In addition to its extremely high anti-oxidant activity and low pro-oxidant capability, geraniin is seen to possess in vitro hypoglycemic activity (alpha-glucosidase inhibition: IC₅₀ = 0.92 μg/ml and alpha-amylase inhibition: IC₅₀ = 0.93 μg/ml), aldol reductase inhibition activity (IC₅₀ = 7 μg/ml) and has the ability to prevent the formation of advanced glycation end-products (AGE). Geraniin was observed to exhibit these properties at more significant levels compared to the positive controls acarbose (carbohydrate hydrolysis inhibitor), quercetin (aldol reductase inhibitor) and green tea (AGE inhibitor). Geraniin therefore, has the potential to be developed into an anti-hyperglycemic agent. Our findings also strongly support the use of a geraniin-standardised N. lappaceum extract in the management of hyperglycemia.