Carbohydrate-hydrolyzing Enzymes Research Articles

Exploring the 3,5-Dibromo-4,6-dimethoxychalcones and Their Flavone Derivatives as Dual α-Glucosidase and α-Amylase Inhibitors with Antioxidant and Anticancer Potential.

The rising levels of type 2 diabetes mellitus (T2DM) and the poor medical effects of the commercially available antidiabetic drugs necessitate the development of potent analogs to treat this multifactorial metabolic disorder. It has been demonstrated that targeting two or more biochemical targets associated with the onset and progression of diabetes along with oxidative stress and/or cancer could be a significant strategy for treating complications related to this metabolic disorder. The 3,5-dibromo-4,6-dimethoxychalcones (2a-f) and the corresponding flavone derivatives (3a-f) were synthesized and characterized using spectroscopic (NMR, HR-MS and FT-IR) techniques. The inhibitory effect of both series of compounds against α-glucosidase and α-amylase was evaluated in vitro through enzymatic assays. Selected compounds were also evaluated for potential to activate or inhibit superoxide dismutase. Compound 3c was selected as a representative model for the flavone series and evaluated spectrophotometrically for potential to coordinate Cu(II) and/or Zn(II) ions implicated in the metal-catalyzed free radical generation. A plausible mechanism for metal-chelation of the test compounds is presented. Furthermore, the most active compounds from each series against the test carbohydrate-hydrolyzing enzymes were selected and evaluated for their antigrowth effect on the human breast (MCF-7) and lung (A549) cancer cell lines and for cytotoxicity against the African Green Monkey kidney (Vero) cell line. The parent chalcone 2a and flavone derivatives 3a, 3c and 3e exhibited relatively high inhibitory activity against the MCF-7 cells with IC50 values of 4.12 ± 0.55, 8.50 ± 0.82, 5.10 ± 0.61 and 6.96 ± 0.66 μM, respectively. The chalcones 2a and 2c exhibited significant cytotoxicity against the A549 cells with IC50 values of 7.40 ± 0.67 and 9.68 ± 0.80 μM, respectively. Only flavone 3c exhibited relatively strong and comparable cytotoxicity against the MCF-7 and A549 cell lines with IC50 values of 6.96 ± 0.66 and 6.42 ± 0.79 μM, respectively. Both series of compounds exhibited strong activity against the MCF-7 and A549 cell lines compared to the analogous quercetin (IC50 = 35.40 ± 1.78 and 35.38 ± 1.78 μM, respectively) though moderate compared to nintedanib (IC50 = 0.53 ± 0.11 and 0.74 ± 0.15 μM, respectively). The test compounds generally exhibited reduced cytotoxicity against the Vero cells compared to this anticancer drug. Molecular docking revealed strong alignment of the test compounds with the enzyme backbone to engage in hydrogen bonding interaction/s and hydrophobic contacts with the residues in the active sites of α-glucosidase and α-amylase. The test compounds possess favorable drug-likeness properties, supporting their potential as therapeutic candidates against T2DM.

Hypoglycemic Properties of Leccinum scabrum Extracts-An In Vitro Study on α-Glucosidase and α-Amylase Inhibition and Metabolic Profile Determination.

Type-2 diabetes affects an increasing percentage of the world's population and its control through dietary management, involving the consumption of health-promoting foods or their derived supplements, is a common strategy. Several mushroom species have been demonstrated to be endowed with antidiabetic properties, resulting from their ability in improving insulin sensitivity and production, or inhibiting the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase. This study aimed to investigate for the first time the hypoglycemic properties of the edible mushroom Leccinum scabrum (Bull.) Gray. Mushroom extracts were prepared through the microwave-assisted extraction (MAE) technique using green solvents with different polarity degrees. The inhibition activity of all the obtained extracts on both α-glucosidase and α-amylase was evaluated and the highest activity was observed for the EtOAc extract which showed an IC50 value about 60-fold lower than the reference compound 1-deoxynojirimycin (DNJ) on α-glucosidase (0.42 ± 0.02 and 25.4 ± 0.6 µg/mL, respectively). As expected on the basis of the literature data concerning both α-glucosidase and α-amylase inhibition, a milder inhibition activity on pancreatic α-amylase was observed. Preliminary in vivo tests on Drosophila melanogaster carried out on the most active obtained extract (EtOAc) confirmed the in vitro observed hypoglycemic activity. Finally, the EtOAc extract metabolic profile was determined through GC-MS and HRMS analyses.

Screening of anti-diabetic potential of the siddha formulation sambirani poo kuligai by in-vitro alpha glucosidase enzyme inhibition assay

Background: Noninsulin-dependent diabetes mellitus (NIDDM) is a common disease of the endocrine system caused by the decreased secretion of insulin by the pancreatic Langerhans beta cell or by the lowering of insulin resistance due to excessive absorption of glucose. The Siddha system of medicine is a traditional medical system that uses a scientific and holistic approach to provide preventive, promotive, curative, rejuvenative and rehabilitative health care. According to Siddha literature, diabetes is known as Innippu Neer, Madhumegam and Neerizhivu. The various reasons for the cause of this disease are attributed to foodhabits and lifestyle changes and also due to hereditary causes. One of the therapeutic approaches is to decrease the postprandial hyperglycemia by retarding the absorption of glucose through the inhibition of carbohydrate-hydrolyzing enzymes, such as a-amylase and ?-glucosidase. ?-Glucosidase are enzyme that catalyze the absorption of digested glucose from dietary polysaccharides in the small intestine. Aim: The aim of the present study is to evaluate the anti-diabetic potential of the siddha formulation of Sambirani Poo Kuligai(SPK) by alpha glucosidase enzyme inhibition assay. Method: The spectrophotometric assay method was used to find alpha glucosidase inhibitory activity. Results: SPK showed presence of alpha glucosidase inhibitory potential with the maximum inhibition of about 41.74 ± 3.578 % and the corresponding IC50 is 606.5 ± 49.51?g/ml. Conclusion: This in-vitro study revealed the presence of the alpha glucosidase activity in the siddha formulation Sambirani Poo Kuligai possesses antidiabetic activity

Enhancing nutritional and potential antimicrobial properties of poultry feed through encapsulation of metagenome-derived multi-enzymes

BackgroundThe encapsulation of metagenome-derived multi-enzymes presents a novel approach to improving poultry feed by enhancing nutrient availability and reducing anti-nutritional factors. By integrating and encapsulated enzymes such as carbohydrate-hydrolyzing enzymes, protease, lipase, and laccase into feed formulations, this method not only improves feed digestibility but also potentially contributes to animal health and productivity through antimicrobial properties.ResultsThis study investigates the encapsulation of metagenome-derived enzymes, including carbohydrate-hydrolyzing enzymes, protease, lipase, and laccase, using Arabic and Guar gums as encapsulating agents. The encapsulated multi-enzymes exhibited significant antimicrobial activity, achieving a 92.54% inhibition rate against Escherichia coli at a concentration of 6 U/mL. Fluorescence tracking with FITC-labeled enzymes confirmed efficient encapsulation and distribution, while physical characterization, including moisture content and solubility assessments, along with Atomic Force Microscopy (AFM) imaging, validated successful encapsulation. The encapsulated enzymes also effectively hydrolyzed poultry feed, leading to an increase in phenolic content and antioxidant activity, as confirmed by 2,2’-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays.ConclusionsThe encapsulated multi-enzymes improved the overall feed quality by increasing reducing sugars and enhancing physical properties such as solubility and water-holding capacity. The encapsulated multi-enzymes improved the overall feed quality by increasing reducing sugars, antioxidant activity and enhancing physical properties such as solubility and water-holding capacity. Scanning Electron Microscopy (SEM) and Fourier-Transform Infrared Spectroscopy (FTIR) analyses confirmed the enzymatic breakdown of the feed structure. These results suggest that supplementing poultry feed with encapsulated multi-enzymes can enhance its physical, nutritional, and functional properties, leading to improved digestibility and overall feed quality.

Exploring the anti-diabetic activity of 2,6-diamino-4-chloropyrimidinium-hydrogen oxalate conjugates: Synthesis, crystal structure, quantum computational, drug-likeness, molecular docking and dynamics simulation

Inhibiting carbohydrate-hydrolyzing enzyme has been considered as an effective approach for controlling starch digestion and postprandial blood glucose level. The aim of this study, the salt molecule was prepared to identify potentially effective compound against diabetic activity and discover the inhibitory mechanism of the targeted enzyme, which is determined by In-silico techniques. And also perform the quantum chemical calculation to provide insights about the internal motions of the molecule at the atomic level. The 2,6-diamino-4-chloropyrimidinium-hydrogen oxalate (C4H6ClN4+. C2HO4-) was newly synthesized molecule, which is detailly discussed in this present work. The title compound has been confirmed by single-crystal X-ray diffraction studies, and this structure was refined by the least-square refinement method. The crystal compound exhibited the P-1 space group (centrosymmetric) and the following unit cell parameters: a = 5.5778(6)Å, b = 9.6687(10)Å, c = 9.9144(10)Å, α = 116.342(1) °, β = 92.610(1) °, γ = 106.370(1) °, Z = 2. The molecular structure is stabilized by the networks of N–H···O, O–H···O, C–H···O, and N–H···N hydrogen bond interactions. The Hirshfeld surface (HS) analysis and fingerprint plots revealed strong intermolecular interaction between the molecules. The structural optimization, frontier molecular orbital (FMO), molecular reactivity, molecular electrostatic potential (MEP), and mulliken atomic charges were generated by the density functional theory (DFT) calculated at B3LYP/6-311G++ (d,p) theory level. Drug-likeness and physicochemical properties were predicted. The molecular docking analysis was showed a binding energy of −8.96 kcal/mol within the active site of alpha-amylase, which is responsible for anti-diabetic activity. The protein-ligand complex stability was verified using molecular dynamics studies with 100 ns.

Inhibitory Activity of Red and Yellow Araçá Genotypes Towards Carbohydrate-Hydrolyzing Enzymes: Putative Role of Ellagitannins

Psidium cattleianum Sabine (araçá) is a species native to Southeast Brazil that grows under abiotic stress conditions conferring high content of bioactive compounds to its fruits. The presence of these compounds is thought to be responsible for the many health-promoting effects including antioxidant, anti-inflammatory, anti-aging and antidiabetic activities. In this study, we evaluated the inhibitory potential of 10 (red and yellow) araçá genotypes towards carbohydrate-hydrolyzing enzymes (CHEs) using cell-free (α-glucosidase, α-amylase) and cell-based assays (sucrase). Araçá extracts displayed stronger inhibition towards α-glucosidase than α-amylase, and only 3 inhibited sucrase activity. The high variability towards the in vitro inhibitory CHEs activity was reflected in the total phenolics content with values ranging between 38.9 and 117 mg/100 g. Of the thirty compounds identified by High-Performance Liquid Chromatography-Diode Array Detection-Electrospray Ionization-Tandem Mass Spectrometry (HPLC-DAD-ESIMS/MS), including caffeic acids (9), organic acids (3) ellagitannins (15) and flavonoids (3), ellagitannins were the most abundant class. Statistical analysis showed ellagitannins were the main discriminators to the CHEs inhibitory activity. In summary, by expanding the panel of red and yellow araçá varieties studied, our results show that not all araçá genotypes inhibit CHE as only YA-23, RA-29, and RA-87 inhibited all 3 CHE which were related to the presence of ellagitannins. Information on the araçá genotypes with greater CHE inhibitory activity allied with the health-promoting effects of ellagitannin-rich foods, can be used to scale-up commercially exploitable genotypes with the aim to develop araçá-containing food formulations targeted to the pre-diabetic population.

Antidiabetic potentials of crude and purified sulphated polysaccharides isolated from Gracilaria gracilis, a seaweed from South Africa

Over 90 % of all cases of diabetes that have been diagnosed are type 2 diabetes (T2D), a disease exacerbated by an increase in sedentary behaviour, bad eating habits, and obesity. This study investigated the antidiabetic properties of Gracilaria gracilis, using in vitro and ex vivo experimental models. The sulphated polysaccharides (SPs) from crude extracts of the seaweed powder was prepared via hot (100°C) and cold (25°C) aqueous extraction procedures before purification via an anion exchange chromatographic technique. Both the crude and purified extracts were characterised by Fourier-transform infrared spectroscopy (FT-IR), LC-MS analysis, and Nuclear Magnetic Resonance (NMR) spectroscopy. The crude cold-aqueous and purified hot-aqueous SPs from G. gracilis had the strongest α-glucosidase inhibitory effect with IC50 value of 0.15 and 0.07 mg/ml, respectively. The purified cold-aqueous SP was the most potent inhibitor of α-glucosidase with an IC50 value of 0.17 mg/ml. The crude and purified SP-rich extracts inhibited pancreatic lipase (hot aqueous SP = 0.03 mg/ml) activity and effectively stimulated glucose uptake in yeast cells. Moreover, they showed significantly (p < 0.05) better intestinal glucose absorption inhibitory properties at the highest concentration (1 mg/ml) and displayed significantly (p < 0.05) better muscle glucose uptake compared to the commercial antidiabetic drug, metformin, at the same concentration. Overall, the current findings indicate that G. gracilis SPs may inhibit carbohydrate-hydrolysing enzymes, limit the release of simple sugars from the gut whilst effectively stimulating the use of glucose by peripheral tissue thus may be suitable to develop antidiabetic food supplements after further animal and clinical trials.

Chemical Profile and Healthy Properties of Sicilian Diplotaxis harra subsp. crassifolia (Raf.) Maire.

This study was aimed at investigating the phytochemical profile and bioactivity of Diplotaxis harra subsp. crassifolia (Brassicaceae), a species from central-southern Sicily (Italy), where it is consumed as a salad. For this purpose, LC-ESI/HRMSn analysis of the ethanolic extract was performed, highlighting the occurrence, along with flavonoids, hydroxycinnamic acid derivatives, and oxylipins, of sulfated secondary metabolites, including glucosinolates and various sulfooxy derivatives (e.g., C13 nor-isoprenoids, hydroxyphenyl, and hydroxybenzoic acid derivatives), most of which were never reported before in the Brassicaeae family or in the Diplotaxis genus. Following ethnomedicinal information regarding this species used for the treatment of various pathologies such as diabetes and hypercholesterolemia, D. harra ethanolic extract was evaluated for its antioxidant potential using different in vitro tests such as 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), Ferric Reducing Ability Power, and β-carotene bleaching tests. The inhibitory activity of carbohydrate-hydrolyzing enzymes (α-amylase and α-glucosidase) and pancreatic lipase was also assessed. In the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid assay, an IC50 value comparable to the positive control ascorbic acid (2.87 vs. 1.70 μg/mL, respectively) was obtained. The wild-wall rocket salad extract showed a significant α-amylase inhibitory effect. Obtained results indicate that Sicilian wild-wall rocket contains phytochemicals that can prevent hyperglycemia, hyperlipidemia, and obesity.

Isolation of Carbohydrate Hydrolyzing Enzymes from Red Kidney Beans

Isolation of Carbohydrate Hydrolyzing Enzymes from Red Kidney Beans

Synergistic effect of potential alpha-amylase inhibitors from Egyptian propolis with acarbose using in silico and in vitro combination analysis

BackgroundType 2 Diabetes mellitus (DM) is an affliction impacting the quality of life of millions of people worldwide. An approach used in the management of Type 2 DM involves the use of the carbohydrate-hydrolyzing enzyme inhibitor, acarbose. Although acarbose has long been the go-to drug in this key approach, it has become apparent that its side effects negatively impact patient adherence and subsequently, therapeutic outcomes. Similar to acarbose in its mechanism of action, bee propolis, a unique natural adhesive biomass consisting of biologically active metabolites, has been found to have antidiabetic potential through its inhibition of α-amylase. To minimize the need for ultimately novel agents while simultaneously aiming to decrease the side effects of acarbose and enhance its efficacy, combination drug therapy has become a promising pharmacotherapeutic strategy and a focal point of this study.MethodsComputer-aided molecular docking and molecular dynamics (MD) simulations accompanied by in vitro testing were used to mine novel, pharmacologically active chemical entities from Egyptian propolis to combat Type 2 DM. Glide docking was utilized for a structure-based virtual screening of the largest in-house library of Egyptian propolis metabolites gathered from literature, in addition to GC–MS analysis of the propolis sample under investigation. Thereafter, combination analysis by means of fixed-ratio combinations of acarbose with propolis and the top chosen propolis-derived phytoligand was implemented.ResultsAucubin, identified for the first time in propolis worldwide and kaempferol were the most promising virtual hits. Subsequent in vitro α-amylase inhibitory assay demonstrated the ability of these hits to significantly inhibit the enzyme in a dose-dependent manner with an IC50 of 2.37 ± 0.02 mM and 4.84 ± 0.14 mM, respectively. The binary combination of acarbose with each of propolis and kaempferol displayed maximal synergy at lower effect levels. Molecular docking and MD simulations revealed a cooperative binding mode between kaempferol and acarbose within the active site.ConclusionThe suggested strategy seems imperative to ensure a steady supply of new therapeutic entities sourced from Egyptian propolis to regress the development of DM. Further pharmacological in vivo investigations are required to confirm the potent antidiabetic potential of the studied combination.

Inhibitory Properties of Polyphenolic Phytochemicals of Cola nitida on Carbohydrate Hydrolyzing Enzymes of Wistar Rat In-Vivo

Polyphenolic phytochemicals of Cola nitida, with their potential therapeutic ability can modulate metabolic and transcriptional expression of proteins and enzymatic activities that culminate to hyperglyceamic effects. This study investigated the hyperglyceamic effects of polyphenolic phytochemical extracts of Cola nitida in Wistar rat in-vivo and established a parallel inhibition of the enzymes (α-amylase and α-glucosidase) in their activities as the concentration increased. On administration of the extracts, the activity of α-amylase was inhibited from control, 32 ± 0.00 to 16 ± 0.02u/L as the concentration increased. Also, the activity of α- glucosidase was inhibited from 17 ± 0.01 to 10 ± 0.00u/L in relation to the concentration of the extracts. The inhibitory effect of Cola nitida on carbohydrate hydrolyzing enzymes delayed glucose utilization resulting to elevated glucose concentration from 6.07 ± 0.02 to 9.11 ± 0.01 mMol/L. The composition of the polyphenolic phytochemicals in the Cola nitida analyzed with gas chromatographic techniques was found to contain; apigenin, 6.0 ± 0.01; catechin, 7.1± 0.01; epicatechin, 4.8 ± 0.02; narigenin, 4.9 ± 0.10 mg/100mg and these are the active ingredients of the bioactive compounds that are responsible for the hyperglyceamic effects of Cola nitida.

Identification of isobenzofuranone derivatives as promising antidiabetic agents: Synthesis, in vitro and in vivo inhibition of α-glucosidase and α-amylase, computational docking analysis and molecular dynamics simulations

Diabetes mellitus, one of the major health challenges of the 21st century, is associated with numerous biomedical complications including retinopathy, neuropathy, nephropathy, cardiovascular diseases and liver disorders. To control the chronic hyperglycemic condition, the development of potential inhibitors of drug targets such as α-glucosidase and α-amylase remains a promising strategy and focus of continuous efforts. Therefore, in the present work, a concise library of isobenzofuranone derivatives (3a-q) was designed and synthesized using Suzuki-Miyaura cross-coupling approach. The biological potential of these heterocyclic compounds against carbohydrate-hydrolyzing enzymes; α-glucosidase and α-amylase, was examined. In vitro inhibitory results demonstrated that the tested isobenzofuranones were considerably more effective and potent inhibitors than the standard drug, acarbose. Compound 3d having an IC50 value of 6.82 ± 0.02 μM was emerged as the lead candidate against α-glucosidase with ⁓127-folds strong inhibition than acarbose. Similarly, compound 3g demonstrated ⁓11-folds higher inhibition strength against α-amylase when compared with acarbose. Both compounds were tested in vivo and results demonstrate that the treatment of diabetic rats with α-amylase inhibitor show more pronounced histopathological normalization in kidney and liver than with α-glucosidase inhibitor. The Lineweaver-Burk plot revealed an uncompetitive mode of inhibition for 3d against α-glucosidase whereas compound 3g exhibited mixed inhibition against α-amylase. Furthermore, in silico molecular docking and dynamics simulations validated the in vitro data for these compounds whereas pharmacokinetics profile revealed the druglike properties of potent inhibitors.

GC-MS and HPTLC bioautography-based phytochemical profiling and evaluation of biological activity Neptunia prostrata Linn whole plant and leaves

This work used experimental methods to evaluate the chemical composition of GC-MS, HPTLC-based bioautographaphy, antioxidant, anti-diabetic, and protein denaturation properties of the Neptunia prostrata Linn (family: Mimosaceae) whole plant and leaves. Three methods, namely DPPH, metal chelating, and reducing power assays, were used to estimate the antioxidant effects. In addition, α-amylase, a carbohydrate-hydrolyzing enzyme, was targeted to test the anti-diabetic activity. The protein denaturation assay was used to evaluate the anti-inflammatory activity of the plant. GC-MS, an important analytical tool, was performed to identify bioactive compounds of medicinal plants used in pharmaceutical industries. Biochemical derivatization HPTLC-based bioautography with DPPH was executed to identify antioxidant agents from N. prostrata. The validated HPTLC method was used to quantify identified antioxidant agents. The stability of compounds, preparation of calibration curves, linearity, range, precision, limit of detection, limit of quantification, robustness, and accuracy are examined to develop a robust method. Higher total phenolic content (TPC) content was observed in N. prostrata hydroalcoholic extract of the whole plant (81.12 ± 4.19 mg GAE/g) and methanolic extract of leaves (105.16 ± 3.11 mg GAE/g). Methanolic extract of N. prostrata leaves showed significantly high antioxidant potential for all DPPH (IC50:28.05 ± 1.78 µg/mL), metal chelating (IC50:1598 ± 23.51 µg/mL), and reducing power assay compared to standard ascorbic acid (DPPH assay: IC50:24.14 ± 2.34 µg/mL and metal chelating: IC50:1301.16 ± 6.14 µg/mL). N. prostrata aqueous extract of the whole plant (IC50:179.47 ± 10.59 µg/mL) and leaves (IC50:130.86 ± 3.58 µg/mL) showed significantly high α-amylase inhibitory activity as compared to standard acarbose (IC50:148.62 ± 7.84 µg/mL). Methanolic extract of whole plants (IC50:131.46 ± 11.81 µg/mL) and chloroform extract of leaves (IC50:122.61 ± 8.19 µg/mL) exhibited strong anti-inflammatory activity as compared to standard acetylsalicylic acid (IC50:117.77 ± 4.95 µg/mL). GC-MS analysis revealed the presence of several bioactive compounds, where 2-cyclopenten-1-one, 2-hydroxy showed the most abundant bioactive compounds in the plant with 17.01%. HPTLC-bioautography identified three phenolic acids (chlorogenic acid, gallic acid, and 4-hydroxybenzoic acid) and one flavonoid (naringenin), further quantified with the validated HPTLC method. These findings propose that N. prostrata has therapeutic potential for treating diseases related to oxidative damage, diabetes, and inflammation, which may be due to the presence of bioactive compounds.

Characterization of Lactobacillus spp. as Probiotic and Antidiabetic Potential Isolated from Boza, Traditional Fermented Beverage in Turkey.

Boza, a cereal-based beverage popular in southeast Europe, is fortified with probiotics and is believed to positively impact the composition of the gut microflora. This investigation focused on fermented cereal-based beverage boza to identify strains of probiotic Lactobacillus spp. capable of inhibiting carbohydrate-hydrolysing enzymes α-glucosidase (AG) and α-amylase (AA). The isolated bacterial strains underwent a comprehensive assessment, including biochemical, molecular, and probiotic trait analyses such as tolerance survivability, adhesion, safety, and health-promoting attributes. We evaluated the inhibitory potential of the supernatant, cell lysate, and intact cells of Lactobacillus spp. Molecular analysis has revealed that isolates RAMULAB30 and RAMULAB29 exhibit a significant genetic similarity (>97%) to Lacticaseibacillus paracasei and Limosilactobacillus fermentum, respectively. These findings are documented in the NCBI database. They exhibited significant resistance to gastrointestinal and intestinal fluids, also indicating their potential for adhesion. Additionally, the isolates showed a significant antibacterial activity, particularly against Micrococcus luteus. They showed resistance to vancomycin and methicillin antibiotics but were more susceptible to streptomycin and ampicillin. Furthermore, the strains demonstrated antioxidant properties. To ensure their safety, a haemolytic assay was conducted despite their general recognition as safe (GRAS) status. The study primarily aimed to evaluate the inhibitory effects of the extract on enzymes AG and AA. Bacterial isolates demonstrated a significant inhibitory activity against both enzyme AG (32%-67% inhibition) and enzyme AA (18%-46% inhibition) in different forms, including supernatant (CS), lysed extract (CE), and intact cell (IC). These findings underscore the potential of bacterial isolates to inhibit the enzyme activity effectively. Furthermore, the L. fermentum RAMULAB29 and L. paracasei RAMULAB30 strains exhibit remarkable antidiabetic potential. Food products incorporating these strains have promising prospects as nutraceuticals, providing improved health benefits.

Effects and mechanisms of anti-diabetic dietary natural products: an updated review.

Diabetes is a global public health issue, characterized by an abnormal level of blood glucose. It can be classified into type 1, type 2, gestational, and other rare diabetes. Recent studies have reported that many dietary natural products exhibit anti-diabetic activity. In this narrative review, the effects and underlying mechanisms of dietary natural products on diabetes are summarized based on the results from epidemiological, experimental, and clinical studies. Some fruits (e.g., grape, blueberry, and cherry), vegetables (e.g., bitter melon and Lycium barbarum leaves), grains (e.g., oat, rye, and brown rice), legumes (e.g., soybean and black bean), spices (e.g., cinnamon and turmeric) and medicinal herbs (e.g., Aloe vera leaf and Nigella sativa), and vitamin C and carotenoids could play important roles in the prevention and management of diabetes. Their underlying mechanisms include exerting antioxidant, anti-inflammatory, and anti-glycation effects, inhibiting carbohydrate-hydrolyzing enzymes, enhancing insulin action, alleviating insulin resistance, modulating the gut microbiota, and so on. This review can provide people with a comprehensive knowledge of anti-diabetic dietary natural products, and support their further development into functional food to prevent and manage diabetes.

Gamma Irradiation Promotes the Growth Rate of Thai Pigmented Rice As Well As Inducing the Accumulation of Bioactive Compounds and Carbohydrate Hydrolyzing Enzymes Inhibitors (α-Glucosidase and α-Amylase) under Salt Conditions.

Rice contains many bioactive compounds that perform various biological activities. Some of these compounds have been identified as α-glucosidase and α-amylase inhibitors, including guaiacol, vanillin, methyl vanillate, vanillic acid, syringic acid, and 2-pentyl furan. In this study, we assessed the growth rate, photosynthetic pigment content, phenolic content, and flavonoid content of gamma-irradiated Thai pigmented rice. Bioactive components of gamma-irradiated rice that had been subjected to salt treatment were also investigated. The findings showed that production of photosynthetic pigments, which are associated with plant growth, was induced by low gamma exposure. Phenolic and flavonoid content of rice was increased after gamma irradiation at 5 to 1,000 Gy. Both gamma irradiation and the salt conditions changed the quantity of vanillin, methyl vanillate, and vanillic acid in the rice. However, at a salt concentration of 40 mM, the salt stress had more of an effect than the gamma dosage. However, the high concentrations of methyl vanillate and vanillic acid detected in the rice under salt conditions were ameliorated by gamma irradiation. Guaiacol served as the substrate of guaiacol peroxidase for catalyzed reactive oxygen species, as evidenced by the observation that the guaiacol content of rice decreased between increased gamma dosages. A gamma dose of 40 to 1,000 Gy resulted in the production of syringic acid. Under salt stress, syringic acid buildup was also seen to be ameliorated by gamma irradiation. In comparison to salt conditions, particularly for 20 mM salt, gamma irradiation had less of an impact on the 2-pentyl furan in rice.

Nutritional, physicochemical and quality profiles of organically sweetened gluten-free breakfast meal from quinoa (Chenopodium quinoa Willd) and tigernuts (Cyperus esculentus L.)

By formulating a breakfast meal from quinoa and tigernuts that is organically sweetened, this study aimed to synergistically utilize the natural bioactive compounds embedded in both foods. When compared to commercial sample, all formulations had higher protein and fat contents. The meals contained little starch, and most significantly, over 35% of this starch was non-digestible. The main minerals found in the meals were potassium (481.81—592.47 mg/100 g), phosphorus (231.75—257.20 mg/100 g), magnesium (152.34—176.29 mg/100 g), and calcium (257.45—266.61 mg/100 g, with the Na/K molar ratio < 1.0 advantageous for those with high blood pressure. Regarding overall phenol and flavonoid contents, the meals outperformed the commercial product with remarkable antioxidant capacities when tested against different assays (FRAP, ABTS, and DPPH). The meals' inhibitory capacities on both carbohydrate-hydrolyzing enzymes were noticeably higher than that of the commercial product. Regardless of the amount of quinoa or tigernuts in each blend, the inhibitory performance was satisfactory (α-amylase 26.98—60.18%; α -glucosidase 19.47—40.02%). Similarly, the chemical properties of the meals as influenced by its higher protein, fats, dietary fibre, and low sugar, modulated its functional properties in a unique way. In terms of sensory assessment, the panelists ranked the meals similar and sometimes above the commercial ones with respect to all the organoleptic parameters considered.Graphical A graphical representation of production, nutritional and functional characterization of stevia-sweetened breakfast meals from quinoa-tigernuts blends

Natural deep eutectic ready to use extract of astilbin: Super high in vitro bioaccessibility, α-amylase and α-glucosidase enzyme inhibition kinetics

Astilbin, a natural flavonoid, possesses multiple functionalities, while the poor bioavailability seriously restricts its application in functional food and medicine. Therefore, in this study, a natural deep eutectic solvent (NaDES) with choline chloride: lactic acid (CHCL-LAC) is selected to deliver astilbin by evaluating the bioaccessibility and antioxidant capacity during in vitro gastrointestinal digestion, and the inhibitory effect with underlying mechanism of astilbin-CHCL-LAC against α-amylase/α-glucosidase were investigated. The CHCL-LAC showed significant high astilbin bioaccessibility (84.1% bioaccessible) and DPPH and ORAC antioxidant capacity with 75.7% and 57.7% respectively after 3 h in vitro digestion, which may be attributed by hydrogen bond based supramolecule formed between astilbin and CHCL-LAC. Moreover, significant inhibitions of astilbin-CHCL-LAC on α-amylase (IC50 of 0.67 g/L) and α-glucosidase (IC50 of 0.64 g/L) were observed in mixed competitive and non-competitive manners. The dominant binding force between enzymes and astilbin were the hydrogen and hydrophobic interaction. This is the first time that the underlying mechanisms for astilbin delivered by NaDESs were revealed, suggesting that CHCL-LAC-based NaDESs are promising ready-to-use vehicles of natural inhibitors for carbohydrate-hydrolyzing enzymes.

Natural &amp;alpha;-glucosidase inhibitors from selected medicinal plants in Malaysia

The most prevalent subtype of diabetes is Type 2 Diabetes Mellitus which results from an abnormal postprandial increase in blood glucose. Inhibition of the carbohydrate-hydrolysing enzymes (alpha-glucosidase and alpha-amylase) in the human digestive organs can control blood glucose levels, making it an important strategy in the management of Type 2 Diabetes Mellitus. A majority of the oral synthetic drugs which have been developed to treat Type 2 Diabetes Mellitus are expensive and have undesirable side effects. As a result, plant-derived remedies have become preferred alternatives as they are easily available, affordable and less harmful. Angustine (1) the major constituent in Nauclea subdita (Korth.) Steud., and (E)-labda-8(17),12-dien-15,16-dial (2) and zerumin A (3) of Alpinia pahangensis Ridley were evaluated for their α-glucosidase inhibitory activity. (E)-Labda-8(17),12-dien-15,16-dial (2) (IC50 = 39.7 μM) was identified as the most potent inhibitor among all three, followed by angustine (1) (IC50 = 48.1 μM) and zerumin A (3) (IC50 = 53.3 μM). Enzyme kinetic studies indicated that angustine (1) was a mixed-type inhibitor, while (E)-labda-8(17),12-dien-15,16-dial (2), and zerumin A (3) were non-competitive inhibitors. Molecular docking and molecular dynamics (MD) simulation studies were performed to predict the key interactions between the ligands and the target protein, 1AGM (complex of acarbose with glucoamylase from Aspergillus awamori). The results of the study of binding interaction energy suggested that angustine (1) has the potential to be used as a natural drug lead in the treatment of type 2 diabetes mellitus.

Increased therapeutic effect of nanotized silibinin against glycation and diabetes: An in vitro and in silico-based approach

BackgroundThe global prevalence of diabetes has increased sharply, with the number of cases expected to rise from 424.9 million in 2017 to 628.6 million by 2045. Flavonoids are plant derived molecules with well-established antioxidant potential in addition to other therapeutic properties. Silibinin is a naturally occurring flavonoid with antioxidant and antidiabetic properties. However, its rapid metabolism and low bioavailability limit its therapeutic effects. Aims & objectivesIn this study, we have synthesized the nanoformulation of silibinin and compared its antiglycating and antidiabetic potential with the soluble form. MethodologyThe inhibitory effect was tested on carbohydrate-hydrolyzing enzymes as well as glycation of human serum albumin (HSA). The structural and biochemical changes in HSA were assessed by spectroscopic analyses and different assays. Key findingsThe nanoforms were found to be better inhibitors of α-amylase and α-glucosidase compared to the bulk forms. Glycation of HSA in the presence of nano-silibinin resulted in the formation of lower level of early and advanced glycation products. This was also confirmed by spectroscopic studies and by estimating protein oxidation and free lysine residues. Molecular docking studies further supported the experimental outcomes. These results indicate that the nano form has significantly stronger antidiabetic and antiglycating effects than the bulk form. Nano-silibinin could therefore be recommended as a dietary supplement for diabetics to help control glycation and other associated complications.