Α-amylase Enzyme Inhibition Research Articles

Impact assessment of different electric fields on the quality parameters of blueberry flavored dairy desserts processed by Ohmic Heating

The effect of ohmic heating (OH) (1.82, 3.64, 5.45, 7.30, 9.1 V cm−1, 90 °C/3 min) and conventional pasteurization in the parameters of quality of dairy desserts with blueberry flavor was investigated. Processes performances (heating rate, thermal load and energy consumption), physicochemical characteristics (fatty acids profile, volatile compounds, rheological assay and color parameters) and bioactive compounds (total phenolics, anthocyanins, antioxidant activity, inhibition of α-glycosidase, α-amylase, and angiotensin-converting enzymes) were evaluated. OH technology proportionated decreased heat generation, energy consumption and heat rate compared to conventional process. OH-treated dairy desserts subjected to higher electric field strength greater inhibition of α-glucosidase and ACE enzymes, without difference in fatty acid profile; however negative effects were observed in color parameters, volatiles profiling and rheological behavior. Overall, the results suggest the influence of ohmic heating on blueberry dairy processing is multidimensional, being the conditions of operation should be carefully chosen to keep the functional and structural aspects of the product.

Extraction and characterization of phycocyanin from Spirulina platensis and evaluation of its anticancer, antidiabetic and antiinflammatory effect

The phycocyanin was purified by Sephadex- G-100 and RP-HPLC and protein content was found to be 52.82% and the high purity fraction was collected and RP-HPLC analysis of fractionated phycocyanin, the α-subunit and β-subunit were detected in 4.9 and 11.1(mAU). The frequency of peak 1456.26 cm−1 has showed the CH2 bending vibration and the protein amide II band was detected at 1539.20 cm−1 (CO stretching) and 2358.94 cm−1. In 1H NMR analysis, 14 chemical shifts (δ) were observed and signals confirmed namely alkyl halide, alkene, aldehyde proton and carboxylic acid. The in vivo anticancer effect was assessed by MTT assay against HepG-2 cell lines and in vivo antidiabetic effect was carried out through α-amylase and β-glucosidase enzyme inhibition methods. The promising anticancer effect 68% was noticed at the concentration of 500 μg/ml and lower anticancer effect was noticed at the concentration of 100 μg/ml against Hep-G2 cell lines. The α-amylase and β-glucosidase enzyme inhibition of phycocyanin showed dose dependent and maximum inhibition effect at 250 μg/ml. Phycocyanin anti-inflammatory effect such as inhibition of albumin denaturation, antiproteinase, hypotonicity-induced haemolysis and anti-lipoxygenase activities have been recorded maximum level at 500 μg/ml. Phycocyanin have complex structure and high molecular weight with more biomedical applications for drug development.

Pharmacological activities of differential parts of selected Essential Indian Spices

The role of plants in human health has extensively revealed due to the emergence of numerous advancements in the medicine and nutrition disciplines. The awareness of the benefits of plants in food as wealthy additives poses researchers to pursue for discovering the influence of such ingredients to the health of the human beings. Spices and herbs are well known food ingredients, which enhances the flavour and aroma of the supplemented foods. Botanically, spices are one class of the aromatic plants; they are mainly present in the tropical provinces. Spices play an important role as flavouring agents in the diet and are used throughout the world. Spices refers to dried part of plant that contains volatiles oils or aromatic flavours such as buds (cloves), bark (cinnamon), root (ginger), berries (black pepper), seeds (cumin, coriander). Spices can be used as medicine because they are natural products easily absorbed by our bodies and generally do not have any adverse effects. Herbal remedies are an important source for the discovery of new antibiotics. Highest phenolic content was observed for ethanol extract of Bunium bulbocastanum (374.28±0.22 µg/mg GAE) and highest flavonoid content was observed for ethanol extract of Piper nigrum (123.58±0.32 µg/mg QE). Cuminum cyminum possessed effective inhibition against gram negative bacteria (Escherichia coli and Proteus vulgaris) and the zone of inhibition were found to be 23 mm at 100 µg/mL concentration respectively. The DPPH˙ radical scavenging activity was found to be higher for Syzygium aromaticum among the tested spices with 75.37±0.48% at 120 µg/mL concentration and the IC50 value was 53.54 µg/mL concentration respectively. The Fe3+ reduction was found to be higher for Syzygium aromaticum among the tested spices with 99.14±0.26% at 120 µg/mL concentration and the RC50 value was 12.81 µg/mL concentration respectively. The α-amylase enzyme inhibition was found to be higher for Piper nigrum among the tested spices with 67.47±0.40% at 120 µg/mL concentration and the IC50 value was 44.69 µg/mL concentration respectively.

In vitro and in vivo inhibitory effects of Carica papaya seed on α-amylase and α-glucosidase enzymes

The present study was aimed to investigate the in vitro and in vivo inhibitory effects of Carica papaya seeds on α-amylase and α-glucosidase enzymes, as this is known to be an antidiabetic mechanism. Analysis of the extracts of the seeds for phytochemicals revealed the presence of a significant amount of saponins, alkaloids, flavonoids, phenols, terpenoids, and steroids. The seed extracts of Carica papaya exhibited good antioxidant capacity using 2, 2-diphenyl-1-picryl hydroxyl (DPPH), thiobarbituric reactive substance (TBARS) and ferric reducing antioxidant power (FRAP) method. The results of the inhibitory studies of the extracts revealed that the hexane extract followed by the ethyl acetate extract was the most potent inhibitor of α-amylase and α-glucosidase enzyme when compared to other extracts using their IC50 values. In the animal study, different doses (250, 500 and 1000 mg/kg/body weight) of the extracts of Carica papaya seed were administered orally for 120 min, to normal and streptozotocin-induced diabetic rats, and were compared with acarbose 100 mg/kg/body weight and control group for the effect on postprandial hyperglycemia. The extract of ethyl acetate (at doses of 250, 500 and 1000 mg/kg/body weight) significantly reduced postprandial glucose levels in these animals. The characterization of hexane and ethyl acetate extracts by GC-MS analysis revealed 20 bioactive compounds while the FTIR analysis confirmed the presence of this functional groups: -C=C, -C-Cl, -C-O, -O-H, -CH, -C=O, -C=C=C, -N=C=S, -O=C=O and -N-H in Carica papaya seed extracts. It was concluded that the inhibition of α-amylase and α-glucosidase enzymes and the prevention of oxidative stress in postprandial hyperglycemia could be some of the possible mechanisms by which they exert their anti-diabetic properties.

Efficient extraction of cucurbitacins from Diplocyclos palmatus (L.) C. Jeffrey: Optimization using response surface methodology, extraction methods and study of some important bioactivities

Diplocyclos palmatus (L.) C. Jeffrey is an important medicinal plant used in several reproductive medicines. It serves as a wide source of tetracyclic triterpens called cucurbitacins. Response surface methodology (RSM) with Box-Behnken design (BBD) was studied to optimize the production of cucurbitacins. RSM put forth the ideal conditions such as 1:30 SS ratio (g/mL), 80 rpm (mixing extraction speed), 150 µm mean particle size, 30 min extraction time and 50 °C using chloroform in continuous shaking extraction (CSE) and showed the highest cucurbitacin I (CUI) content (2.345 ± 0.1686 mg/g DW). Similarly, the highest yield of cucurbitacin B (CUB) (1.584 ± 0.15 mg/g DW) was recorded at ideal conditions (1:40 g/mL SS ratio and 60 min time and others similar to CUI). Among the tested extraction methods, the highest CUI, CUB, and CUI + B yield (1.437 ± 0.03, 0.782 ± 0.10, 2.17 ± 0.35 mg/g DW, respectively) as well as promising DPPH radical scavenging activity (25.06 ± 0.1 µgAAE/g DW) were recorded from the SBAE (steam bath assisted extraction). In addition, MAE and UAE revealed the highest inhibition of α-amylase (68.68%) and α-glucosidase (56.27%) enzymes, respectively. Fruit extracts showed potent anticancer activity against breast (MCF-7) and colon (HT-29) cancer cell lines (LC50 – 44.27 and 46.88 µg/mL, respectively). Our study proved that SS ratio, particle size and temperature were the most positively influencing variables and served to be the most efficient for the highest recovery of CUI and CUB. Based on the present study, the fruits of D. palmatus were revealed as a potent antioxidant, anti-diabetic and anticancer bio-resource that could be explored further to develop novel drug to manage diabetes, cancer and oxidative stress related disorders.

Therapeutic Efficacy of Nyctanthes arbor-tristis Flowers to Inhibit Proliferation of Acute and Chronic Primary Human Leukemia Cells, with Adipocyte Differentiation and in Silico Analysis of Interactions between Survivin Protein and Selected Secondary Metabolites

Although the antidiabetic efficacy of Nyctanthes arbor-tristis flowers has been reported, antiproliferative and anti-obesity activities are yet to be explored. We examined the anti-obesity and antiproliferative potentials of different fractions (hexane, chloroform, ethyl acetate, methanol) of N. abor-tristis flower extract for the first time using 3T3-L1 cells, primary peripheral blood mononuclear cells (PBMC) isolated from healthy and adult acute myeloid (AML) and chronic lymphocytic leukemia (CLL) patients, recombinant Jurkat T cells, and MCF7 cell lines. The in vitro hypoglycemic activity was evaluated using the inhibition of α-amylase enzyme and glucose uptake by yeast cells. The percentage glucose uptake and α-amylase inhibitory activity increased in a dose-dependent manner in the crude and the tested fractions (hexane and ethyl acetate). Inhibition of the 3T3-L1 cells’ differentiation was observed in the ethyl acetate and chloroform fractions, followed by the hexane fraction. Antiproliferative analyses revealed that Nyctanthes exerted a high specific activity against anti-AML and anti-CLL PBMC cells, especially by the hexane and ethyl acetate fractions. The gas chromatography/mass spectrometry analysis indicated the presence of 1-heptacosanol (hexane fraction), 1-octadecene (hexane and chloroform fractions), and other organic compounds. Molecular docking demonstrated that phenol,2,5-bis(1,1-dimethylethyl) and 4-hydroxypyridine 1-oxide compounds showed specificity toward survivin protein, indicating the feasibility of N. abor-tristis in developing new drug leads against leukemia.

Anti-Diabetic Potential of Anti-Oxidant Compounds "Riboflavin, Flavin Mononucleotide and Flavin Adenine Dinucleotide" with High Therapeutic Potency through Inhibition of α-Amylase and α-Glucosidase Enzymes at Sub-Micromolar Concentrations

Diabetes is a group of metabolic disorders characterized by a high blood sugar level over a prolonged period of time. Inhibition of carbohydrate hydrolyzing enzymes leads to decrease in the absorption of glucose which is considered as one of the effective managements of diabetes mellitus. Vegetable, fruit, milk, and fish are good sources of riboflavin (RF) and vitamin B5 with versatile health benefits. The well-adapted structural features of these compounds for the inhibition/activation of enzymes include several available hydrogen bond (H-bond) acceptors and donors, flexible backbone, and hydrophobic nature. The substrates of α-amylase (α-Amy) and α-glucosidase (α-Glu), known as key absorbing enzymes, have functional groups (OH groups) resembling RF and vitamin B5. Therefore, the present study was conducted to evaluate the inhibitory properties of fliavin, RF, flavin mononucleotide (FMN), flavin adenine dinucleotide (FAD) and vitamin B5 against α-Amy and α-Glu. The median inhibition concentration (IC50) values for α-Glu in the presence of RF, FMN and FAD were determined 136.7±4.8, 235.4±5.2 and 78.9±3.4, respectively. The IC50 values α-Amy in the presence of RF, FMN and FAD were determined 165.6±7.1, 253.6±5.5 and 131.2±6.3, respectively. Moreover, the Ki values of RF were calculated as 14.2±1.8 and 18.6±1.7 µM for α-Glu and α-Amy in a mixed-mode. In addition, to communicate with the active site of α-Glu and α-Amy respectively, RF presented a binding energy of -8.1 and -7.3 kcal/mol, FMN -7.1 and -6.8, and FAD -10.3 and -7.8 kcal/mol. These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index, but also to limit the activity of the major reactive oxygen species (ROS) producing pathways. Key words: Riboflavin, hydrolyzing enzymes, enzyme inhibition, hyperglycemia Introduction

Anti-diabetic properties of Synsepalum dulcificum and its potential inclusion in functional yogurt

There has been an enormous interest in the development of alternative medicines for type-2 diabetes, specifically screening for phythochemicals with the ability to delay or prevent glucose absorption. The goals of the present study were to provide in vitro evidence for potential inhibition of α-amylase and α-glucosidase enzymes, followed by inclusion of the extracts of Synsepalum dulcificum in yogurt to enhance the therapeutic properties of the yogurt. The screening results of seed, leaf and pulp of S. dulcificum showed that pulp extracts contained significantly (P<0.05) higher anti-diabetic activities than the other plant parts. More interestingly, S. dulcificum pulp also has stronger anti-diabetic properties than the standard drug, acarbose and hence it was chosen to be incorporated into yogurt. S. dulcificum yogurt had higher (P<0.05) anti-diabetic activities than the plain yogurt throughout the storage period with the highest α-glucosidase and α-amylase inhibitory activities were shown on day 7 of storage. Therefore, S. dulcificum pulp can be developed as functional factor with anti-diabetic activities in food application.

Comparison Between the Potential of Tempe Flour Made from Germinated and Nongerminated Soybeans in Preventing Diabetes Mellitus

This study was aimed to compare the chemical characteristics of tempe flour made from nongerminated soybean (NST) and germinated soybean (GST), especially on their capacity in preventing diabetes mellitus (DM). Soybeans were germinated for 20 hours in the dark until 2.5-5.0 mm of the radicle emerged. The ungerminated soybeans and the germinated soybeans were then processed into tempe and tempe flour. The two types of tempe flour were subjected to proximate analysis, amino acid profiling, antioxidant capacity, total phenol content, isoflavone content, and α-amylase and α-glucosidase enzyme inhibition analyses. GST was superior in preventing DM in the protein content and antioxidant parameters, as these were significantly higher (p&lt;0.05) than in NST. On the other hand, NST was superior in preventing diabetes in the isoflavon (daidzein, genistein, and total isoflavone) and α-amylase inhibition IC50 parameters which were significantly better (p&lt;0.05) than in GST. On the contrary, the diabetes-preventing parameters total phenols, α-glucosidase inhibition IC50, and insulinotropic amino acids (arginine, alanine, phenilalanine, isoleucine, leucine, and lysine) were not different (p&gt;0.05). Therefore, GST and NST both have potential in preventing diabetes through different mechanisms.

UHPLC-QTOF-MS/MS metabolites profiling and antioxidant/antidiabetic attributes of Cuscuta reflexa grown on Casearia tomentosa: exploring phytochemicals role via molecular docking

ABSTRACT Present study reports metabolites profiling, antioxidant, and antidiabetic effects of Cuscuta reflexa grown on Casearia tomentosa. The UHPLC-QTOF-MS/MS method was used to characterize phytochemicals in most potent extract. Thirteen bioactive compounds/metabolites including (2S)-3-(β-D-galactopyranosyloxy)-2-(hexanoyloxy)propyl nonanoate, 4-O-β-D-glucosyl-4-coumaric acid, isorhamnetin-3-O-glucoside, 7-(α-D-glucopyranosyloxy)-2,3,4,5,6-pentahydroxyheptanoic acid, 13S-hydroxyoctadecadienoic acid, astragaloside derivative, salicylic acid, oleanolic acid, citric acid, pinellic acid, quinic acid, caffeic acid derivative and caffeic acid-3-glucoside were detected in 80% hydroethanolic (HE) extract. Among different extracts (aqueous, 20–80% HE and pure ethanolic), 80% HE extract showed maximum TPC (186.19 ± 2.15 mg GAE/g DE) and TFC (106.50 ± 1.68 mg RE/g DE). A strong correlation was observed between TPC, TFC, DPPH radical scavenging (IC50 = 60.64 ± 1.74 µg/mL) and TAP activity (235.96 ± 1.33 mg AAE/g DE) of 80% HE extract among others. The same extract also depicted highest α-amylase and α-glucosidase enzyme inhibition with IC50 of 71.84 ± 1.06 and 57.25 ± 1.40 µg/mL, respectively. Molecular docking was performed to explore possible role of identified phytochemicals. Binding affinity data as well as interaction patterns have revealed possible interaction of the identified bioactives against α-glucosidase and α-amylase. Moreover, intra-molecular charge transfer, energies of the FMOs, HOMO-LUMO-Egaps, MEP and IP were also explained. The present findings suggested that, C. reflexa is a promising natural antioxidant and antidiabetic agent, thus supporting the use of this plant for designing related functional foods and nutra-pharmaceuticals.

Evaluation of In Vivo Antidiabetic, In Vitro α-Amylase Inhibitory, and In Vitro Antioxidant Activity of Leaves Crude Extract and Solvent Fractions of Bersama abyssinica Fresen (Melianthaceae).

Background.The leaves of Bersama abyssinica are used for the treatment of diabetes mellitus in folk medicine system of Ethiopia. The present study was done based on the traditional claim of B abyssinica for the treatment of diabetes mellitus.Methods.The α-amylase inhibition and antioxidant activities of B abyssinica extracts were evaluated by using 3,5-dinitrosalicylic acid method and diphenyl-2-picrylhydrazyl assay model, respectively. Blood glucose lowering activity of the extracts was studied in 4 animal models; normoglycemic, oral glucose loaded, and streptozotocin-induced diabetic mice models.Results.Among the extracts, the crude extract showed the highest α-amylase enzyme inhibition activity with an IC50 of 6.57 μg/mL. The water fraction showed the strongest antioxidant activity with an IC50 of 3.43 μg/mL. The crude extract at doses of 200, and 400 mg/kg showed significant (P < .05) hypoglycemic activity in normoglycemic mice. All doses of the crude extract significantly (P < .05) reduced blood glucose levels of oral glucose-loaded mice. In streptozotocin-induced diabetic mice models, both the crude and solvent fractions showed a significant (P < .05) blood glucose lowering effect as compared with the negative control group post 8 hour treatment.Conclusion.The results demonstrated the beneficial biochemical effects of B abyssinica extract by inhibiting α-amylase and scavenging the free radicals. The crude extract and solvent fractions of B abyssinica had significant blood glucose lowering effect in all animal models.

Molecular Modelling and in Vitro Hypoglycemic Examination of Polysubstituted Quinoline Derivatives

In the present work in-silico molecular simulations were carried out to find out the binding affinities of synthesized polysubstituted quinolines towards PPARγ protein (2XKW). The results obtained from docking analysis showed that the synthesized polysubstituted quinoline derivatives 1a-g are having stronger binding interactions which was on par to that of standards rosiglitazone and pioglitazone. In addition to this in-vitro hypoglycemic studies were studied through α-amylase and α-glucosidase enzyme inhibition assays. The results showed that compounds 1c and 1d possess good hypoglycemic efficacy with percentage inhibition of 87.94 ± 0.25, 85.90 ± 0.56 towards α-glucosidase and 84.55 ± 1.02, 82.14 ± 0.26 percent inhibition towards α-amylase which was greater than standard rosiglitazone and comparable to standard pioglitazone

Alpha-Amylase and Alpha-Glucosidase Enzyme Inhibition and Antioxidant Potential of 3-Oxolupenal and Katononic Acid Isolated from Nuxia oppositifolia.

Nuxia oppositifolia is traditionally used in diabetes treatment in many Arabian countries; however, scientific evidence is lacking. Hence, the present study explored the antidiabetic and antioxidant activities of the plant extracts and their purified compounds. The methanolic crude extract of N. oppositifolia was partitioned using a two-solvent system. The n-hexane fraction was purified by silica gel column chromatography to yield several compounds including katononic acid and 3-oxolupenal. Antidiabetic activities were assessed by α-amylase and α-glucosidase enzyme inhibition. Antioxidant capacities were examined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) scavenging assays. Further, the interaction between enzymes (α-amylase and α-glucosidase) and ligands (3-oxolupenal and katononic acid) was followed by fluorescence quenching and molecular docking studies. 3-oxolupenal and katononic acid showed IC50 values of 46.2 μg/mL (101.6 µM) and 52.4 μg/mL (119.3 µM), respectively against the amylase inhibition. 3-oxolupenal (62.3 µg/mL or 141.9 μM) exhibited more potent inhibition against α-glucosidases compared to katononic acid (88.6 µg/mL or 194.8 μM). In terms of antioxidant activity, the relatively polar crude extract and n-butanol fraction showed the greatest DPPH and ABTS scavenging activity. However, the antioxidant activities of the purified compounds were in the low to moderate range. Molecular docking studies confirmed that 3-oxolupenal and katononic acid interacted strongly with the active site residues of both α-amylase and α-glucosidase. Fluorescence quenching results also suggest that 3-oxolupenal and katononic acid have a good affinity towards both α-amylase and α-glucosidase enzymes. This study provides preliminary data for the plant’s use in the treatment of type 2 diabetes mellitus.

In Silico Pharmacokinetics and Molecular Docking of Novel Bioactive Compound (11-Methoxy-2-Methyltridecane-4-Ol) for Inhibiting Carbohydrates Hydrolyzing Enzyme

The inhibition of α-amylase enzyme involved in the digestion of carbohydrates can significantly reduce the post prandial hyperglycemia. The bioactive compound, 11-methoxy-2-methyltridecane- 4-ol extracted from marine macro alga Gracilaria edulis showed antidiabetic activity. In the present study, in silico pharmacokinetics and molecular interaction properties of novel bioactive compound 11-methoxy-2-methyltridecane-4-ol for inhibiting α-amylase enzyme activity in carbohydrates digestion is investigated and reported. The ADME properties of bioactive compound and its absorption such as solubility (-3.151 log mol/L), Caco-2 permeability (1.73 log papp in 10-6 cm/s), intestinal absorption (96.127 % absorbed), skin permeability (- 1.986 log kp) were evaluated. The distribution of VDss (-0.025 log L/kg), fraction unbound (0.322 FU), BBB permeability (0.556 BB), CNS permeability (-1.763 PS) and the Excretion of Total clearance is 0.67 log ml/min/kg were also proved. The metabolic changes of the compound 11-methoxy-2-methyltridecane-4-ol are not observed. With regard to toxicity of the bioactive compound observed concentration is as follows, in max tolerated dose of 0.343 log mg/kg/day, in oral rat acute toxicity (LD50) 1.526 mol/kg, in oral rat chronic toxicity (LOAEL) (1.972 log mg/kg_bw/day), in T. pyriformis toxicity, 1.839 log ug/L, and in minnow toxicity 1.225 log nM. The molecular interaction properties predicted on the biding energy of this compound is -5.56 kcal/ mol and the H-bond interaction of the amino acid is ILE 235 and HIS 101. Results of present study on 11-methoxy-2-methyltridecane-4-ol suggest that it could be developed as a novel α-amylase inhibitor for the treatment of diabetes mellitus.

Evaluation of phenolic bioactive-linked anti-hyperglycemic and Helicobacter pylori inhibitory activities of Asian Basil (Ocimum spp.) varieties

Basil (Ocimum spp.) is an important herb from the Lamiaceae family with a long history of use in traditional medicine and food applications. Thus, targeting basil varieties for developing herbal medicines against non-communicable chronic diseases (NCDs) such as type 2 diabetes has significant merit. The aim of this study was to screen Asian basil varieties with therapeutic potential for type 2 diabetes targeting relevant phenolic bioactive-linked antioxidant, anti-hyperglycemic, and antimicrobial properties and was compared with a high phenolic and high antioxidant mint species (Mentha arvensis). Aqueous and ethanol (12%) extracts of 8 different varieties of Asian basil were analyzed for total soluble phenolic (TSP) content, phenolic acid profiles, total antioxidant activity (TA), α-amylase, and α-glucosidase enzyme inhibitory activities and inhibition of ulcer-causing bacteria, Helicobacter pylori using in vitro assay models. The highest TSP content was observed in mint and all basil varieties were compared to this standard. High TA, and α-glucosidase enzyme inhibitory activity were observed in targeted varieties of Indian basils. Major phenolic acids found were rosmarinic, ellagic, benzoic, and gallic acids, which may potentially contribute to health benefits such as antioxidant and anti-hyperglycemic properties. Inhibitory activity against H. pylori was observed in response to high phenolic mint but not in Asian basil extracts. This in vitro study provides biochemical rationale on phenolic bioactive-linked antioxidant and anti-hyperglycemic potentials of Asian Basil varieties that need to be further validated with in vivo studies for therapeutic and herbal medicine related applications against type 2 diabetes and associated complications.

Hypoglycemic, Antiglycation, and Cytoprotective Properties of a Phenol-Rich Extract From Waste Peel of Punica granatum L. var. Dente di Cavallo DC2.

Pomegranate peel is a natural source of phenolics, claimed to possess healing properties, among which are antioxidant and antidiabetic. In the present study, an ethyl acetate extract, obtained by Soxhlet from the peel of Dente di Cavallo DC2 pomegranate (PGE) and characterized to contain 4% w/w of ellagic acid, has been evaluated for its hypoglycemic, antiglycation, and antioxidative cytoprotective properties, in order to provide possible evidence for future nutraceutical applications. The α-amylase and α-glucosidase enzyme inhibition, interference with advanced glycation end-products (AGE) formation, and metal chelating abilities were studied. Moreover, the possible antioxidant cytoprotective properties of PGE under hyperglycemic conditions were assayed. Phenolic profile of the extract was characterized by integrated chromatographic and spectrophotometric methods. PGE resulted able to strongly inhibit the tested enzymes, especially α-glucosidase, and exerted chelating and antiglycation properties. Also, it counteracted the intracellular oxidative stress under hyperglycemic conditions, by reducing the levels of reactive oxygen species and total glutathione. Among the identified phenolics, rutin was the most abundant flavonoid (about 4 % w/w). Present results suggest PGE to be a possible remedy for hyperglycemia management and encourage further studies to exploit its promising properties.

Synthesis of new indazole based dual inhibitors of α-glucosidase and α-amylase enzymes, their in vitro, in silico and kinetics studies.

The current study describes the discovery of novel inhibitors of α-glucosidase and α-amylase enzymes. For that purpose, new hybrid analogs of N-hydrazinecarbothioamide substituted indazoles 4-18 were synthesized and fully characterized by EI-MS, FAB-MS, HRFAB-MS, 1H-, and 13C NMR spectroscopic techniques. Stereochemistry of the imine double bond was established by NOESY measurements. All derivatives 4-18 with their intermediates 1-3, were evaluated for in vitro α-glucosidase and α-amylase enzyme inhibition. It is worth mentioning that all synthetic compounds showed good inhibition potential in the range of 1.54 ± 0.02-4.89 ± 0.02 µM for α-glucosidase and for α-amylase 1.42 ± 0.04-4.5 ± 0.18 µM in comparison with the standard acarbose (IC50 value of 1.36 ± 0.01 µM). In silico studies were carried out to rationalize the mode of binding interaction of ligands with the active site of enzymes. Moreover, enzyme inhibitory kinetic characterization was also performed to understand the mechanism of enzyme inhibition.

Evaluation of in vivo and in vitro biological activities of Gardenia latifolia Ait leaf

Gardenia latifolia Ait. belonging to the family Rubiaceae is a flowering plant with high ethnomedicinal practices in Bangladesh. The current study evaluates analgesic, antipyretic, α-amylase enzyme inhibition, membrane stabilizing, antioxidant effect and antimicrobial potentials of G. latifolia. The analgesic and antipyretic activity of ethanol extract of G. latifolia (EGL) leaves were evaluated by hot plate reaction model and brewers’ yeast-induced hyperthermia model in mice, respectively. The a-amylase inhibiting activity, membrane stabilizing activity, antioxidant activity and antimicrobial activity of EGL along with its hexane (HSGL) and chloroform (CSGL) soluble fractions were measured employing the starch-iodine method, hypotonic induced hemolysis assay, DPPH free radical scavenging assay and minimum inhibitory concentration (MIC) determination method, respectively. Here, EGL exhibited dose-dependent pain relieving activity in experimental mice. EGL also significantly (p

Antidiabetic potential and multi-biological activities of Trachystemon orientalis extracts

Due to the increase in exposure to chemical substances, the investigation of natural compounds with protective effects has become popular. So in this study the antimicrobial, antioxidant, antimutagenic activities and enzyme inhibitory effects of Trachystemon orientalis leaf and stem extracts were investigated. Antimicrobial effect was determined by disc diffusion method and the antimutagenic effect was investigated by Ames/Salmonella/microsomal test. Antioxidant properties of T. orientalis extracts were determined by investigating the phytochemical contents and 2,2-diphenyl-1-picrylhydrazyl (DPPH) removal activity. The antidiabetic activity of the extracts was investigated by α-amylase and α-glucosidase enzyme inhibition. It has been determined that all extracts exhibit antimicrobial activity at different ratios and the highest antimicrobial activity was obtained with a 21 ± 0.4 mm inhibition zone against Escherichia coli. The highest DPPH removal activity of leaf and stem extracts was determined to be 65.1 ± 2.4% and 59.4 ± 2.7%, respectively. In enzyme inhibitory analysis, it was determined that the α-glucosidase inhibitory effect of extracts was higher than the α-amylase inhibition effect. In antimutagenity test, the highest antimutagenic effects of leaf and stem extract were determined as 78.2 ± 1.1% and 67.2 ± 1.5%, respectively. As a result, T. orientalis leaf and stem extracts were determined as a potential natural antimicrobial, antimutagenic and antioxidant source with a moderately high antidiabetic activity.

Antidiabetic‎ Activity of Terfezia Claveryi; An In Vitro and In Vivo Study

The main objective of current study was to investigate the in vitro and in vivo antidiabetic activity of Terfezia claveryi methanol extract. In vitro antidiabetic assays such as inhibition of α-amylase enzyme and non-enzymatic glycosylation of hemoglobin were carried out. The results of α- amylase inhibition assay revealed that the inhibitory activity (IC50) of Terfezia claveryi methanol extract (‎38.7µg/ml) is stronger when compared with positive control (Acarbose IC50 value of ‎45.3‎ µg/ml). The inhibition of glycosylation of hemoglobin of Terfezia claveryi methanol extract showed almost the same IC50 (33.1µg/ml) when compared the positive control, alpha-tocopherol (‎35.4µg/ml‎). In vivo antidiabetic study revealed that Terfezia claveryi methanol extract ‎ possessed good activity at a dose of 200 mg/kg through reducing the fasting plasma glucose level (122.1‎±‎3.0 mg/dl) when compared with positive control (Glibenclamide of ‎79.4±1.4‎ mg/dl) (p &lt; 0.001). The results from this study indicated that Terfezia claveryi methanol extract exhibited considerable in vitro and in vivo antidiabetic activities. These possible activities could be useful to consider Terfezia claveryi ‎ as therapeutic antidiabetic candidate.