Α-amylase Inhibition Research Articles

Phytochemical Analysis and Evaluation of Antioxidant, Antidiabetic, and Anti-inflammatory Properties of Aegle marmelos and Its Validation in an In-Vitro Cell Model.

Persistent hyperglycemia significantly increases oxidative stress and inflammation resulting in multiple cellular and molecular alterations which further exacerbate the diabetes associated complications.Aegle marmelos (L.) Corrêais a medicinal plant used in the Indian system of medicine for treating various disorders including diabetes. However, studies on phytoconstituents and their pharmacological activity of this plant are limited. Therefore, we aimed to determine the phytochemical components, evaluate the antidiabetic activity, anti-inflammatory activity, and antioxidant activity ofA. marmelosleaf extract, and validate its mechanistic effects in an in vitro cell model. The qualitative and quantitative analysis of the different phytoconstituents in the extract was determined using standardized protocols. The antioxidant activity of the extract was evaluated by 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assay and ferric reducing antioxidant power (FRAP) assay. The antidiabetic activity of the extract was evaluated by α-amylase inhibition and α-glucosidase inhibition assay. The anti-inflammatory activity was studied using an albumin denaturation assay. In addition, the pharmacological effect(s) of leaf extract was checked in the normal rat kidney fibroblast cells (NRK-49F) under high glucose conditions. Intracellular reactive oxygen species (ROS) generation was measured by fluorometry using fluorescence probe 2',7'-dichlorodihydrofluorescin diacetate (DCF-DA). mRNA expression of inflammatory markers including inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha (TNF-α) was studied using real-time quantitative polymerase chain reaction (RT-qPCR). Cell migration was studied using cell scratch assay. Statistical analysis was performed using GraphPad Prism version 8.0. The phytochemical analysis ofA. marmelosleaf extract revealed the presence of alkaloids, phenols, flavonoids, and saponins. The extract showed higher antioxidant activity in the DPPH (IC50=258.21 µg/mL) and FRAP assay (IC50=293.83 µg/mL). The extract exhibited prominent antidiabetic activity by inhibiting enzymes α-Amylase (IC50=73.2 µg/mL) and α-glucosidase (IC50=43.9 µg/mL). In addition, the extract showed effective anti-inflammatory activity by significantly inhibiting the denaturation of egg albumin (IC50=102.8 µg/mL). Further, the leaf extract significantly decreased the high glucose-induced ROS generation as well as inflammatory markers in rat fibroblast cell lines in a dose-dependent manner. Additionally, high glucose-induced cell migration as the measure of cell injury was effectively reduced by the extract treatment. A. marmelosleafextract was quantified to possess a substantial amount of important phytoconstituents that have promising pharmacological properties. Besides showing antidiabetic activity, the extract significantly combats the high glucose-induced ROS generation, inflammatory markers expressions, and cell migration. Further, in-depth studies and clinical trials are warranted so as to position these traditional remedies for the treatment of metabolic disorders.

A promising α-glucosidase and α-amylase inhibitors based on benzimidazole-oxadiazole hybrid analogues: Evidence based in vitro and in silico studies

The present study reports the design and synthesis of new benzimidazole-oxadiazole compounds as potent inhibitors of α-glucosidase and α-amylase. The synthesized molecules were characterized through different techniques such as 1HNMR, 13CNMR, HREI-MS and evaluated for their in vitro inhibitory activities against these enzymes. Among the compounds screened, compound 8 demonstrated the highest inhibitory activity against both α-glucosidase (IC50 = 11.60 µM) and α-amylase (IC50 = 6.20 µM). Molecular docking analyses were conducted to investigate the binding modes and interactions of the active compounds within the enzyme active sites. The results demonstrate that several benzimidazole-oxadiazole hybrids exhibited potent inhibitory effects on both α-glucosidase and α-amylase, suggesting their promise as antidiabetic agents.

Gamma Irradiation and Exogenous Proline Enhanced the Growth, 2AP Content, and Inhibitory Effects of Selected Bioactive Compounds against α-Glucosidase and α-Amylase in Thai Rice.

Exogenous proline can improve the growth, aroma intensities, and bioactive compounds of rice. This study evaluated the effects of gamma irradiation under proline conditions on the 2-acetyl-1-pyrroline (2AP), phenolic, and flavonoid contents of rice. Moreover, the bioactive compounds of gamma-irradiated rice under proline conditions that inhibited α-glucosidase and α-amylase were evaluated by in silico study. A low gamma dose (40 Gy) induced the highest rice growth under 5 mM proline concentration. The highest 2AP content was stimulated at a gamma dose of 5－100 Gy under 10 mM proline concentration. At 500 and 1,000 Gy gamma dose, the highest flavonoid and phenolic contents of rice were stimulated. 1-(2-Hydroxy-5-methylphenyl)-ethanone, which had the highest binding affinity (-7.9 kcal/mol) against α-glucosidase, was obtained at 500 and 1,000 Gy gamma dose under 5 and 10 mM proline concentrations. Meanwhile, 6-amino-1,3,5-triazine-2,4(1H,3H)-dione, which had the highest binding affinity (-6.3 kcal/mol) against α-amylase, was obtained under 10 mM proline concentration in non-gamma-irradiated rice. The results indicate that using a combination of gamma irradiation and exogenous proline is suitable for producing new rice varieties. Moreover, the bioactive compounds that were obtained in new rice varieties exhibited health benefits, especially for diabetes mellitus treatment (inhibition of α-glucosidase and α-amylase).

Antidiabetic and Antigout Properties of the Ultrasound-Assisted Extraction of Total Biflavonoids from Selaginella doederleinii Revealed by In Vitro and In Silico Studies.

In this study, the extraction, purification and metabolic enzyme inhibition potential of Selaginella doederleinii were investigated. In order to extract the total biflavonoids from S. doederleinii (SDTBs), the optimum extraction process was obtained by optimizing the ultrasonic extraction parameters using response-surface methodology. This resulted in a total biflavonoid content of 22.26 ± 0.35 mg/g. Purification of the S. doederleinii extract was carried out using octadecylsilane (ODS), and the transfer rate of the SDTBs was 82.12 ± 3.48% under the optimum purification conditions. We determined the effect of the SDTBs on α-glucosidase (AG), α-amylase and xanthine oxidase (XOD) and found that the SDTBs had an extremely potent inhibitory effect on AG, with an IC50 value of 57.46 μg/mL, which was much lower than that of the positive control. Meanwhile, they also showed significant inhibition of XOD and α-amylase, with IC50 values of 289.67 μg/mL and 50.85 μg/mL, respectively. In addition, molecular docking studies were carried out to understand the nature of the action of the biflavonoids on AG and XOD. The results showed that robustaflavone had the lowest binding energy to AG (-11.33 kcal/mol) and XOD (-10.21 kcal/mol), while, on the other hand, amentoflavone showed a good binding affinity to AG (-10.40 kcal/mol) and XOD (-9.962 kcal/mol). Moreover, molecular dynamics simulations verified the above results.

Anti-diabetic effect of rice extract constituents through the molecular inhibition of α-amylase and α-glucosidase activity

Anti-diabetic effect of rice extract constituents through the molecular inhibition of α-amylase and α-glucosidase activity

Antioxidant and antiamylase activities of leaf and root extracts of Ziziphus mauritiana Lam

Ziziphus mauritiana Lam is a plant species widely used in Mali for its medical virtues to treat various diseases including Diabetes. The present study aims to examine the antioxidant and antidiabetic activities of leaf and root extracts of Z. mauritiana Lam collected in Bamako. Phytochemical screening and assay were carried out using conventional methods. The DPPH test was used to evaluate the anti-radical activity, and the antidiabetic potential of the extracts was estimated via the α-amylase inhibition test. Characterization tests revealed the presence of free tannins, flavonoids, coumarins, terpenoids, triterpenes, alkaloids, saponins and anthraquinones in all our extracts. The root extracts revealed higher contents of polyphenols (561.40±22.4 to 218.00±30.2 mg EAG/g) and flavonoids (54.26±4.9 to 132.56±6, 82 mg EQ/g) whatever the solvent, with the exception of Ethyl Acetate. Ethanol extracts showed the best anti-radical potentiel. The IC50was 58.13±1.85 µg/mL for roots and 85.19±0.415 µg/mL for leaves. The results provide a better understanding of the medicinal properties of Z. mauritiana Lam and pave the way for management strategies for diabetes and diseases associated with oxidative stress.

Influence of Harvesting Stage on Phytochemical Composition, Antioxidant, and Antidiabetic Activity of Immature Ceratonia siliqua L. Pulp from Béni Mellal-Khénifra Region, Morocco: In Silico, In Vitro, and In Vivo Approaches.

Ceratonia siliqua L. is a medicinal plant that has long been used in traditional Moroccan medicine to treat many diseases. This study aimed to assess the impact of the stages of the immature phase of carob pulp (M1, M2, M3, M4, and M5) on phytochemical composition, antioxidant activity, and antidiabetic activity of Ceratonia siliqua L. The identification of the phenolic profile by HPLC-UV/MS-MS and the study of the antidiabetic effect by in silico, in vitro, and in vivo studies were carried out for extracts with high contents of phenolic compounds from immature wild carob pulp from the communes of Timoulit (TM), Bin Elouidane (AW), and Ouaouizerth (TG) in the province of Azilal in the Béni Mellal-Khénifra region. The results revealed a gradual increase in total sugar content over the pulp's ripening period, reaching a value of 2134 ± 56.23 mg GE/100 g fresh weight (FW) for TG. The three locations showed peak values for total polyphenol content (TPC), total flavonoid content (TFC), and total condensed tannin (TCT) at the M2 stage. AW had the highest concentrations of TPC (3819 ± 226.4 mg GAE/100 g FM), TFC (1034 ± 57.08 mg QE/100 g FM), and TCT (1472 ± 28.46 mg CE/100 g FM). The DPPH assay (7892 ± 296.1 mg TE/100 g FM) and the FRAP assay (278.2 ± 7.85 mg TE/100 g FM) both demonstrated that the TG zone is a highly potent antioxidant zone. In contrast, the AW site exhibited a markedly elevated value of 725.4 ± 103.6 mg TE/100 g FM in the ABTS assay. HPLC-UV-MS/MS analysis showed that the methanolic extracts of immature carob pulp (MEICP) from the three areas contained several different chemical compounds. The most prevalent were 3-O-p-coumaroyl-5-O-caffeoylquinic acid, quercetin 3-methyl ether, gallic acid, and galloylquinic acid. Immature carob pulp extract (ICPE) from AW showed the strongest in vitro inhibition of pancreatic α-amylase (IC50 = 0.405 µg/mL) and TG extracts were most potent against intestinal α-glucosidase (IC50 = 0.063 µg/mL). In vivo, AW, TG, and TM extracts significantly reduced postprandial glycemia in rats, with AW having the greatest effect. These results highlight the antidiabetic potential of ICPE. The 3-O-p-Coumaroyl-5-O-caffeoylquinic acid showed better affinity for α-amylase compared to acarbose and interacted significantly with several amino acid residues of the enzyme. Similarly, this molecule and 3,4-Dicaffeoylquinic acid demonstrated a strong affinity for α-glucosidase, suggesting their potential as natural inhibitors of enzymes involved in carbohydrate metabolism. Most of the compounds are not substrates of P-glycoprotein and exhibited high intestinal absorption. Furthermore, the majority of these compounds did not act as inhibitors or substrates of CYP450 enzymes, reinforcing their suitability for development as oral medications. These results underscore the potential of immature carob pulp as a promising antidiabetic agent.

Integrative bioinformatic and experimental analysis of benzoylbenzodioxol derivatives: hypoglycemic potential in diabetic mice.

We investigated the hypoglycemic activity and pharmacokinetic study of two synthesized benzoyl benzodioxol derivatives, compound I (methyl 2-(6-(2-bromobenzoyl)benzo[d][1,3]dioxol-5-yl)acetate), and compound II, 2-(6-benzoylbenzo[d][1,3]dioxol-5-yl)acetic acid, which showed very strong α-amylase inhibiting activity in our previous study. Then, diabetes was induced by the injection of streptozotocin to mice. The molecular docking simulations and analyses of density functional theory analyses were conducted to study the binding interactions with human pancreatic alpha-amylase, and their pharmacokinetic properties were further evaluated by ADMET profiling. Compound I showed the most important hypoglycemic effect, decreasing the blood glucose by 32.4%, higher than that of compound II by 14.8% and even the positive control acarbose by 22.9%. Histopathological examination revealed that diabetic livers showed portal inflammation with some apoptotic hepatocytes due to streptozotocin treatment, whereas controls without any treatment maintained normal liver architecture. Molecular docking studies gave results for the best binding affinity of the compound I, through its strong water bridges and π-π interactions, and also through analysis with density functional theory, was more stable and reactive when compared to compound II. Further ADMET analysis showed that both compounds shared a promising pharmacokinetic profile, and compound I had the potential for CNS penetration. Thus, compound I was selected as the best candidate for developing new hypoglycemic agents with potent efficacy, good binding interactions, and excellent pharmacokinetic properties.

Colchicine, serotobenine, and kinobeon A: novel therapeutic compounds in Carthamus tinctorius L. for the management of diabetes

Diabetes, a global health concern, poses increasing mortality risks. The pathogenesis of diabetes involves multiple mechanisms, with oxidative stress being one of the key contributors. As synthetic drugs have various side effects, which can be minimized by using herbal plants. This study focuses on the In vitro antioxidant potential, α-amylase inhibition potential, identification of bioactive compounds, and hub genes in diabetes treatment mechanism by using C. tinctorius Extraction of C. tinctorious lead and flower was performed using different solvents (Distilled water, methanol, chloroform, and Dimethyl ether). After extraction different concentrations range from 25–200 mg/mL) was made and checked against activities. The antioxidant potential was assessed using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), total phenolic contents (TPC), and total antioxidant capacity (TAC) assays, while antidiabetic activity was evaluated through α-amylase inhibition assay. Phytochemicals was identified by GC–MS analysis, followed by ADMET screening and network pharmacology analysis using Swiss Target Prediction, Gene Card, DesGeNet, DAVID, STRING, Cytoscape, and drug revitalization databases. Results revealed positive correlations with DPPH, TAC, and TPC. Methanol extract exhibited the highest inhibitory concentration. Screening of 46 compounds was performed by studying their pharmacokinetic properties which revealed 9 compounds effective against 204 diabetes targets. Moreover, their network analysis identified four hub genes, including AKT1, JUN, EGFR, and MMP9. These genes found highly associated with drugs like Colchicine and Serotobenine. Revitalization analysis also highlighted four genes (EGFR, PTGS2, AKT1, and MMP9) strongly correlated with FDA-approved drugs. The study suggests C. tinctorius methanol extract is a potential source for novel drugs.Graphical

Phenolic Compositions of Different Fractions from Coffee Silver Skin and Their Antioxidant Activities and Inhibition towards Carbohydrate-Digesting Enzymes.

Seeking food-derived antioxidants and inhibitors of α-glucosidase and α-amylase has been recognized as an effective way for managing diabetes. Coffee silver skin (CSS) is rich in phenolic compounds, which may be potential agents as antioxidants and for α-glucosidase and α-amylase inhibition. But whether phenolics in different forms show similar bioactivity remains unknown. In this study, phenolic compounds in CSS were extracted as free phenolics (FPs), esterified phenolics (EPs), and bound phenolics (BPs). The phenolic profiles and antioxidant activities of them were investigated. Their inhibitory effects on α-glucosidase and α-amylase were analyzed, and the inhibitory mechanisms were elucidated by molecular docking and molecular dynamic simulation. Results showed that FPs exhibited the best antioxidant ability and inhibitory effects on α-glucosidase and α-amylase. A total of 17 compounds were identified in FPs with 3-caffeoylquinic acid, 4-feruloylquinic acid, and dicaffeoylquinic acids as the dominant ones. Typical phenolics in FPs could bind to α-glucosidase and α-amylase through hydrogen bonds and form hydrophobic interaction with several key amino acid residues. In addition, 3,4-dicaffeoylquinic acid and 3-caffeoylquinic acid might be the principal components that account for the inhibitory effect of FPs on α-glucosidase. The results of this study may provide some scientific support for CSS utilization as a health-beneficial component in functional food development for type 2 diabetes mellitus management.

Design, Synthesis, Anticholinesterase and Antidiabetic Inhibitory Activities, and Molecular Docking of Novel Fluorinated Sulfonyl Hydrazones.

In this study, it was aimed to synthesize (E)-N'-(2-hydroxybenzylidene)-substituted benzenesulfonohydrazide (1-7) from the 2-hydroxybenzaldehyde reaction of different substituted fluorinated sulfonyl hydrazides. The structures of the synthesized molecules were characterized by elemental analysis, FTIR, 1H NMR, 13C NMR, 19F NMR, and 2D NMR (HMBC, correlation spectroscopy, and HQSC). The anticholinesterase (AChE and BChE) and antidiabetic (α-glucosidase, α-amylase) inhibition activities of the synthesized compounds were evaluated. According to biological activity test results, (E)-N'-(2-hydroxybenzylidene)-4-(trifluoromethoxy)benzenesulfonohydrazide (compound 7 among hydrazone derivatives 1-7) demonstrated better BChE inhibitor activity than galantamine in anticholinesterase inhibition; and in the α-glucosidase and α-amylase assay, it exhibited more antidiabetic inhibition activity than the reference standard.

The structure elucidation, anti-aging and hypoglycemic effects of an O-acetyl mannoglucan from the bulbs of Lanzhou lily

An O-acetyl mannoglucan (BHP-1) from Lanzhou lily bulbs was structurally elucidated using partial acid hydrolysis, GC–MS, and 2D NMR techniques (COSY, NOESY, HSQC and HMBC) built on prior research, revealing a backbone of -α-D-(1 → 4)-Glcp-β-D-(1 → 4)-Manp- with the most potential side chains -α-D-(1 → 4)-Glcp-β-D-(1 → 4)-Manp-α-D-(1 → 4)-Glcp-α-D-(1 → Glcp- and -α-D-(1 → 4)-Glcp-β-D-(1 → 4)-Manp-α-D-(1 → Glcp-, attached to O-2 and O-3 of glucose and mannose residues, and featuring O-acetyl groups at O-2 or O-3 position of mannose. The terminal residue was α-D-(1 → Glcp. BHP-1 demonstrated anti-aging and hypoglycemic effects, as assessed by C. elegans model and glycolytic enzyme effect in vitro, respectively. The results showed that BHP-1 dose-dependently prolonged lifespan of C. elegans by 33 % at 4 mg/mL under normal conditions, with greater extensions under thermal and oxidative stress (50 % and 80 % increases, respectively, p < 0.05), which were attributed to enhanced antioxidant enzymes (SOD and CAT) and lowered MDA levels of C. elegans. Additionally, BHP-1 exhibited remarkable inhibition on α-glucosidase (93 %) and moderate inhibition on α-amylase (53 %) at 4 mg/mL, with competitive inhibition of α-glucosidase and mixed non-competitive inhibition of α-amylase, respectively. These potential effects might be linked to BHP-1's diverse sugar linkages, higher content of Glc, and certain O-acetyl contents.

Design, synthesis, biological evaluation, kinetic studies and molecular modeling of imidazo-isoxazole derivatives targeting both α-amylase and α-glucosidase inhibitors

Herein, a novel set of imidazo-isoxazole derivatives containing thiourea and urea scaffolds were synthesized, characterized (1H NMR, 13C NMR, and elemental analysis). These compounds were biologically evaluated for their α-amylase and α-glucosidase inhibitory activity, identifying 5f as the most active (IC50 26.67 ± 1.25 μM and 39.12 ± 1.83 μM against α-amylase α-glucosidase, respectively), better than the standard, acarbose. Enzymatic kinetic results showed that 5f and acarbose complete competitive type inhibitors. The structure-activity relationship (SAR) demonstrated that undergoing substitutions on R1 and R2 groups attached to the thiourea/urea moiety chains controlled the activity. Besides, in-silico ADMET study showed that almost title compounds exhibited satisfactory pharmacokinetic properties. In molecular docking study, the top performing compound (5f) exhibited higher binding energies (−5.501 and −6.414 kcal/mol, respectively) showing crucial interactions and that snuggly fit in their active site. To shed light on their mechanism of action, molecular dynamic (MD) simulations approach executed at 100 ns duration authenticated the high stability of 5f-1B2Y and 5f-3A4A complexes. The results of this investigation disclosed that compound 5f may serve as a potential lead, accomplished with in vivo studies, for the management of diabetes.

Optimizing phlorotannins extraction from Fucus vesiculosus using Box-Behnken design: Unveiling techniques for enhanced antioxidant activity and metabolic enzyme inhibition

Phlorotannins, phenolic compounds found in brown macroalgae, exhibit potential bioactive effects. This study evaluated the extraction of phlorotannins from Fucus vesiculosus using conventional and ultrasound-assisted extraction (UAE) methods, focusing on solvent-material ratio, solvent concentration, extraction time, and sonication power for UAE. The experiments, designed using a Box-Behnken design, measured total phlorotannin content (TPhC), DPPH, FRAP, and ABTS. The conventional method, under optimal conditions, produced TPhC, DPPH, FRAP, and ABTS values of 512.25 ± 14.26 mg PGE/100 g, 29.70 ± 1.40 mg TE/100 g, 589.57 ± 15.06 mg TE/100 g, and 332.73 ± 31.03 mg TE/100 g, respectively. The UAE method, under its optimal conditions, yielded higher values: 954.00 ± 33.65 mg PGE/100 g, 146.35 ± 3.30 mg TE/100 g, 1037.61 ± 32.93 mg TE/100 g, and 809.95 ± 46.58 mg TE/100 g. The extracts were tested for inhibitory effects on α-amylase and α-glucosidase, with the purified UAE extract showing greater inhibition of α-amylase (IC50 = 7.06 ± 0.67 μg/mL) compared to acarbose (IC50 = 14.63 ± 0.28 μg/mL). For α-glucosidase, acarbose had higher activity (IC50 = 11.54 ± 0.04 μg/mL) than the UAE purified extract (IC50 = 15.04 ± 0.07 μg/mL). UHPLC-qTOF-MS analysis identified various phlorotannin derivatives, with Tetrafucotetraphlorethol (m/z 993) only in the UAE purified extract. This study concludes that purified phlorotannin extract from UAE can potentially regulate α-amylase and α-glucosidase, enzymes linked to metabolic disorders like diabetes and obesity.

Correction: Cassia siamea Role in Diabetes Management: Insights from In vitro and In silico Investigations on α-Glucosidase and α-Amylase Inhibition

Correction: Cassia siamea Role in Diabetes Management: Insights from In vitro and In silico Investigations on α-Glucosidase and α-Amylase Inhibition

Utilizing pistachio green hull extract to produce sugar-free muffins with antioxidant and antidiabetic potential

The current study aimed to produce sugar-free muffins containing pistachio green hull extract (PGHE) as a natural source of antioxidant and antidiabetic compounds. The effects of PGHE substitution (1, 2, and 4% w/w) on the total phenolic content, antioxidant activity (DPPH scavenging), inhibition of α-amylase and α-glucosidase activities, storage stability (peroxide value and TBA), physicochemical, and sensory properties of muffins were investigated. The antioxidant activity of samples containing 4 % PGHE, demonstrated a 22-fold increase compared to the control. Furthermore, muffins containing PGHE displayed higher oxidation stability over a 14-day storage period. PGHE could improve α-amylase and α-glucosidase inhibitory activities of muffins up to 7-fold and 2-fold, respectively. Texture analysis revealed that increasing the amount of PGHE decreased the hardness, gumminess, and chewiness of muffins. Incorporation of PGHE into samples had a significant effect on the color. The muffins containing 2 % PGHE had an overall acceptance that was not significantly different from the control.

Antidiabetic and Antioxidant Activities of Indian Bay Leaf (Cinnamomum tamala (Buch.-Ham.) T. Nees & Eberm.) Essential Oils Collected from Meghalaya.

The current work investigates the chemodiversity, in vitro antioxidant, α-amylase and α-glucosidase inhibitory potential of Cinnamomum tamala (CT) leaf essential oil (EO) collected from different localities of East Khasi Hills District of Meghalaya, India. Gas chromatography-mass spectrometry (GC-MS) analysis of all the extracted leaf essential oils facilitated the identification of several compounds in a variable range along with eugenol as the major component (74.79-95.12 %). CT8 exhibited the highest antioxidant activity (IC50=11.23±0.27 μg/mL for 2,2-diphenyl-1-picrylhydrazyl (DPPH) and IC50=21.54±0.37 μg/mL for 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) among all EO evaluated. The results showed that the ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC) values for CT8 were 83.26±1.92 μM trolox/g oil and 70.29±1.90 ascorbic acid equivalents (AAE)/g of oil. α-amylase and α-glucosidase inhibition were highest in sample CT8 with IC50 values of 3.62±0.42 μg/mL and 16.29±0.32 μg/mL respectively. Caryophyllene, cyclohexene, 1, 5, 5-trimethyl-6-(2-propenylidene), germacrene D and eugenol showed strong binding potential toward α-amylase and α-glucosidase. It concluded that the chemodiversity and antidiabetic potential of C. tamla oil from Khasi Hills have never been studied. It can be taken as a dietary supplement as an antioxidant and antidiabetic to control blood glucose.

Cookies Fortified with Polyphenols Extracts: Impact on Phenolic Content, Antioxidant Activity, Inhibition of α-Amylase and α-Glucosidase Enzyme, Colour and Sensory Attractiveness.

The goal of the research was to determine the impact of fortification with polyphenolic compounds on (i) sensory attractiveness (global satisfaction, appearance, colour, odour, flavour, sweetness, bitterness), (ii) content of polyphenols and colour (L*, a*, b*) after the baking process and (iii) their bioactive potential (antioxidants activity and inhibiting of α-amylase and α-glucosidase enzyme). Fortification was made with extracts of polyphenolic compounds of selected plant raw materials rich in polyphenols from quince (fruits), tilia (flowers), pomegranate (skin), passion fruit (endocarp), sour cherries (leaves), haskap and chokeberry (berries), silver skin (coffee beans), rosehip (seeds). Depending on the nature of the polyphenol extract, flavan-3-ols (monomeric and polymeric), phenolic acid, flavonols and anthocyanins were identified in the product in amounts ranging from 53.7 to 212.6 mg/100 g DM. Cookies' colour (L*, a*, b*) depended on the type of polyphenol extract used for fortification. Cookies with haskap, chokeberry and sour cherry presented the highest antioxidant potential. Cookies with chokeberry, haskap and rosehip presented high activity in inhibiting α-amylase (65.5, 60.6 and 62.2% of inhibition, respectively), but cookies with haskap, silver skin and quince in inhibiting α-glucosidase activity (23.0, 20.4 and 21.4% of inhibition, respectively). In the sensory evaluation, the most attractive were cookies with rosehip and pomegranate (6.3 and 5.8 score, respectively), but the lowest ratings were given to cookies with passion fruit and silver skin but especially quince cookies, which obtained the lowest desirability (3.7 score). The acceptability of fortified cookies was determined to the least extent by monomeric flavan-3-ols and phenolic acids (in minus in odour/flavour, bitterness, sweetness and global satisfaction), but anthocyanins, polymeric procyanidins and flavonols had the most significant positive impact on consumer acceptance of the assessed features, i.e., global satisfaction, odour/flavour, sweetness and bitterness (positive consumer drivers).

Nanoencapsulation of quinoa oil enhanced the antioxidant potential and inhibited digestive enzymes

Quinoa oil is rich in unsaturated fatty acids and vitamin E, but its instability limits its application in food, pharmaceutical, and cosmetic products. Nanoencapsulation emerges as a promising strategy to promote water dispersibility, preserve and enhance functional properties, and increase the bioavailability of bioactive compounds. This study encapsulated quinoa oil through O/W emulsification, using porcine gelatin (OG) and isolated whey protein (OWG) as encapsulating agents. The particles were characterized by different physical and chemical methods and evaluated in vitro for cytotoxicity using Chinese hamster ovary (CHO) cells, human hepatocarcinoma cells (HepG2) and epithelial cells, and bioactive potential through the determination of Total Antioxidant Capacity (CAT) (acidic and neutral media) and iron chelation, and inhibition of digestive enzymes (α-amylase and amyloglucosidase). OG and OWG particles presented smooth surfaces, with an average size between 161 ± 7 and 264 ± 6 nm, with a polydispersity index of 0.11 ± 0.03 and 0.130 ± 0.04, encapsulation efficiency of 74 ± 1.47 % and 83 ± 2.92 %, and water dispersibility >70 %, respectively. Free and nanoencapsulated quinoa oil did not show cytotoxic effects (cell viability >70 %). Nanoencapsulation promoted the enhancement of the antioxidant activity of quinoa oil in the range of 50–63 % in a neutral medium and 96–153 % in an acidic medium than free oil (p < 0.05). OG and OWG also enhanced the inhibition of the enzymes α-amylase (by 5–7 %) and amyloglucosidase (6–9 times more) than free oil (p < 0.05). The results showed that nanoencapsulation increased the potential for quinoa oil application, enabling the development of innovative products.

Synthesis of furo[2,3-c]carbazoles as potent α-glucosidase and α-amylase inhibitors

The carbazole-3-carbaldehyde 2, produced by N-ethyl carbazole via Vilsmeier-Haack reaction, was subjected to Dakin type oxidation with H2O2 and H2SO4 in methanol to produce the carbazole-3-ol 3. The reaction of 3 with a range of commercially available α-haloketones 4a–f in the presence of Al2O3 as catalyst in xylene led to their regio-selective cyclization to afford the furo[2,3-c]carbazoles 5a–f. Identification of the furo[2,3-c]carbazoles 5a–f were performed through 1H NMR,13C NMR, FT-IR and high resolution mass spectrometry. Single crystal X-ray diffraction analysis was employed to further confirm the structures of the some of the targeted compounds. In vitro antidiabetic activities of the newly synthesized furocarbazoles 5a–e were investigated utilizing α-glucosidase and α-amylase enzymes. The biological evaluation revealed the obvious efficiencies of the targeted molecules toward the α-glucosidase enzyme inhibition with the potent IC50 values compared to the standard acarbose. In the case of α-glucosidase inhibition, the furo[2,3-c]carbazoles chloro substituted 5c and nitro substituted 5f were found to be more potent than acarbose with the values of 215.0 and 162.70 μM, respectively. On the other hand, the compound 5f was found to be only promising candidate for α-amylase enzyme but not as effective as the standard acarbose.