Glucosidase inhibitor activity. 1 mol/L PBS) and 120 μL of 0.

75% and 62. 454 mg/mL, and main inhibitors in the fermentation extract presented a reversible, uncompetitive pattern according to Lineweaver-Burk plots. 4A). Feb 1, 2024 · In vitro enzyme inhibition assays revealed that PSP acts as a reversible competitive inhibitor of α-glucosidase and α-amylase, and was found to reduce insulin resistance index, increase OGTT and serum insulin levels, decrease free fatty acid content to improve lipid metabolism, and lower glycated serum protein content to enhance glucose metabolism in T2DM mice, thereby leading to a reduction Jun 19, 2020 · 3. Mar 5, 2020 · The enzyme activity evaluation results showed that both GA and glutaric acid displayed α-glucosidase inhibition activity, and GA-glutaric acid cocrystals showed strengthened α-glucosidase inhibition activity at a moderate concentration, which is attributed to synergism of the two components. The results of the anti hyperglycemic activity were supported by means of in silico 5 days ago · α-Glucosidase inhibition activity. 09 ± 0. 33 μg/mL) than acarbose (IC 50 = 200 μg/mL). 86 μM Jan 3, 2024 · The mode of inhibition of the most potent derivative 11k, identified with the lowest IC 50, was investigated against an α-glucosidase activity at different concentrations of substrate, p Jul 31, 2022 · The highest antioxidant activity of peptides derived from quinoa, obtained by alcalase hydrolysis (0. 2,4,5-benzenetriol substituted compound 120 (IC 50 = 2. 113 The activating effect of glucose on β Mar 14, 2022 · α-glucosidase inhibitors represent an important class of type 2 antidiabetic drugs and they act by lowering postprandial hyperglycemia. Jul 28, 2024 · Α-glucosidase inhibition can be useful in the management of carbohydrate-related diseases, especially type 2 diabetes mellitus. Optimization and validation of a microscale in vitro method to assess alpha-glucosidase inhibition activity. Out of 49 papers, 12 papers demonstrated inhibition Jun 7, 2004 · Increasing of bulkiness and the chain length of 4-alkoxy substituents as well as the increasing of the electron withdrawing group have been shown to decrease the inhibitory activity. Thus, this study provided additional information that quercetin was responsible for Bauhinia pulla activity as an alpha-glucosidase inhibitor. May 5, 2022 · In this review, we focused on the synthesis, anti-α-glucosidase activity, and structure-activity relationships of 1,2,3-triazole based α-glucosidase inhibitors and believe that this review will be inspiring for design and development of more potent and effective 1,2,3-triazole based inhibitors as new lead compounds as anti-diabetic agents. 78 ± 4. 50 +/- 0. One strategy that has been developed to treat type-2 diabetes is inhibition of the activity of alpha-glucosidases using synthetic Feb 1, 2020 · Results of βGLU inhibition studies of 2-arylbenzothiazoles derivatives further established the significance of OH substituent to inhibitory potency, as activity was conserved to OH-substituted compounds . As a result, compound 9 showed a significant α-glucosidase inhibitory activity with IC50 value of 9. The majority of the synthesized derivatives demonstrated significant inhibitory activity. 44 ± 0. α-glucosidase (1 mg) obtained from Saccharomyces cerevisiae dissolved in 100 mL of phosphate buffer (pH 6. foodchem. An active component of Morus leaves, 1-deoxynojirimycin (DNJ), is known to be a strong intestinal α-glucosidase inhibitor [2, 3]. Mar 8, 2021 · Therefore, α-glucosidase has been taken as a key target for treating diabetes, and the inhibitors of α-glucosidase can be developed into effective therapeutic drugs to treat this disease (Li et al. Jan 29, 2020 · Alpha-glucosidase has been considered as the main target enzyme in the prevention and treatment of type 2 diabetes, and the inhibition of alpha-glucosidase activity can control postprandial blood glucose levels of diabetics and keep blood glucose levels normal. Conversely, luteolin non-competitively inhibited α-glucosidase activity by interacting with amino acid residues in proximity to the enzyme active site [26]. [8] 35 Jan 1, 2023 · A study performed on β-glucosidase, BglII from Trichoderma reseei reported inhibition at high substrate concentration, but its catalytic activity increased upon the addition of glucose. Alpha‐glucosidase inhibitors delay absorption of complex carbohydrates and thus inhibit postprandial glucose peaks thereby leading to decreased postprandial insulin levels. Figure 4 illustrates the alpha-glucosidase inhibition activity of WFLE. argentea showed comparable results with that of acarbose. A quantitative structure–activity relationship (QSAR) model was Oct 30, 2023 · The results showed that the methanol extract of S. These are the only two AGIs approved for the United States market, although another AGI, voglibose, was approved by the Pharmaceuticals and Medical Devices Agency in Japan ( Oki et Especially, our group's foray into β-carboline derivatives had yielded promising results in the quest for potent α-glucosidase inhibitors (Fig. 3. 8) comprising of 200 mg bovine serum albumin. Alpha-glucosidase has been considered as the main target enzyme in the prevention and treatment of type 2 diabetes, and the inhibition of alpha-glucosidase activity can control postprandial blood glucose levels of diabetics and keep blood glucose levels normal. CMPE also significantly inhibits the activity of rat α-glucosidase in a dose-dependent manner. EtOAC and MeOH extracts showed stronger inhibiting activity against α-glucosidase and rat intestinal α-glucosidase compared with acarbose as positive control. The IC 50 of hypericin and acarbose was estimated to be 4. Enzyme Inhibition Assays . Water fraction of edible medicinal fern Stenochlaena palustris is a potent α-glucosidase inhibitor with concurrent antioxidant activity. Rosiglitazone, while rarely used, is given as 2 mg, 4 mg, or 8 mg daily. 11 ± 12. Jun 29, 2011 · In vitro studies had indicated dose-dependent inhibitory activity of cinnamon extract against yeast α-glucosidase with the IC 50 value of 5. Among the DPP- 4 inhibitors, linagliptin is available as 5 mg daily. 4-Methoxy-trans-cinnamic acid was a noncompetitive inhibitor for alpha-glucosidase, whereas, 4-methoxy-trans-cinnamic acid ethyl ester was a competitive inhibitor. All TDB extracts expressed a remarkable inhibition on α-glucosidase activity (Table 2). In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhi … Nov 1, 2022 · Inhibition test of α-glucosidase activity implied that S-GFP is a noncompetitive inhibitor of α-glucosidase. 83 μg/ml and mammalian α-glucosidase with IC 50 value of 670 μg/ml. A low dose of cyanidin-3-galactoside showed a synergistic inhibition on intestinal alpha-glucosid … Nov 17, 2022 · A methanol extract of this fungus had significant α-glucosidase inhibitory activity, with an inhibition rate of 56%, and α-amylase inhibitory activity with inhibition rate of 38%. 2. villosum water extract was investigated for its α-glucosidase activity at different concentrations of 1, 3 and 5 mg/mL, which proportionally increased the inhibition against rat α-glucosidase with IC50 of 31. For α-amylase inhibition, this compound also exhibited strong inhibition against this enzyme with the IC 50 values ranging from 6. The assay was carried out by monitoring the α-glucosidase-mediated transformation of the substrate pNPG into α-D-glucose and p-nitrophenol, at 405 nm. Ligands were prepared Oct 14, 2022 · A. 69%, respectively. The method is based on the specific recognition between 1,4-phenylenediboronic acid (PDBA) and 4-aminophenyl-α-d-glucopyranoside (pAPG), which may induce aggregation of pAPG-functionalized gold nanoparticles (AuNPs) to achieve color change of the test solution. 1 µg/mL respectively, while 4 and 1 demonstrated strong alpha-amylase inhibitory activity amongst the isolated compounds with INTRODUCTION. 31 slightly modified. To increase the utilization of whole cereals and their bioactive ingredients in diabetes Aug 27, 2020 · An ethanol extract of the fruit case of Garcinia mangostan, whose most abundant chemical species are xanthones, showed potent α-glucosidase inhibitory activity (IC(50)=3. The results of inhibitory mechanism indicated that S-GFP quenched the endogenous fluorescence of α-glucosidase and changed the Jan 4, 2024 · Alpha-glucosidase inhibitors lower blood glucose by modifying the intestinal absorption of carbohydrates. 167. 10 μL of sample at variable concentrations (1 to 100 μg/mL) was pre Mar 8, 2013 · Background. Jun 22, 2022 · In vitro α-glucosidase inhibition assay of target compounds 4a–n, kinetic analysis of the most potent compound, and in vitro α-amylase inhibitory activity of the selected compounds were Apr 18, 2023 · The mode of inhibition of the most active compounds 6l and 6m identified with the lowest IC 50, was investigated against an α-glucosidase activity with different concentrations of p-nitrophenyl Jul 5, 2023 · In order to find potential α-glucosidase inhibitors, a series of β-carboline derivatives containing piperazine moieties were synthesized by gradual structure optimization (Fig. These enzymes include glucoamylase, sucrase, maltase, and isomaltase. Article CAS PubMed PubMed Central Google Scholar Mar 25, 2022 · Despite numerous reports on the secondary metabolite profile of the leaf, no alpha-glucosidase inhibition activity is yet observed in G. Other oral hypoglycemic drugs are reviewed separately. The strong AGI activity was proved by the inhibition kinetic study which shows the mixed type of inhibition on the alpha glucosidase enzyme. Aug 10, 2024 · Collectively, IC 50 values < 30 μg/mL, 50 ppm, and 10 μM suggest strong potential as inhibitors for α-glucosidase inhibition activity. were evaluated by α-glucosidase inhibitory activity and DPPH, ABTS and FRAP assays, respectively, for antioxidant properties in vitro. 3 μM and acted as a competitive inhibitor with the value of the inhibition constant (Ki) being 10. The kinetics of its peptide-induced inhibition on α-d-glucosidase activity and its interaction mechanism merging with molecular docking were both investigated. Furthermore, EGCG and GCG almost completely inhibited α-glucosidase activity, while ECG was somewhat less effective, although the difference was not statistically significant (Figure 3b). Briefly, in a 96-well plate, the enzyme (0. The IC 50 value was about 5-fold and 9-fold higher for α-glucosidase and α-amylase than the control drug acarbose. Inhibition activity of O. , 2022; Zhang et al. 2,3 Currently, the commercial α-glucosidase Mar 10, 2017 · Sukohar et al. 45 ± 1. So far, a t … Nov 11, 2021 · As known, α-glucosidase inhibitors can delay the release of d-glucose from dietary complex carbohydrates and retard glucose absorption in the small intestine by inhibiting α-glucosidase activity, resulting in reduced postprandial plasma glucose levels and suppression of postprandial hyperglycemia. Inhibition type was determined by the Lineweaver Jul 28, 2021 · α-glucosidase is a major enzyme that is involved in starch digestion and type 2 diabetes mellitus. doi: 10. 02 ± 0. 1016/j. The inhibition of castanospermine (β-Glucosidase inhibitor) on β-Glucosidase leads to reducing the yields of glu … Jun 7, 2021 · In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a–ag have been synthesized through heating a Dec 5, 2023 · In addition, it is reported that 1,3,4-oxadiazoles strongly bind with various target proteins through hydrogen-bonding interactions. et al. They competitively inhibit enzymes that convert complex nonabsorbable carbohydrates into simple absorbable carbohydrates. 35 ± 65. Compared to positive control acarbose (IC 50 = 654. α-glucosidase solution was prepared by dissolving 1 mg in 100 mL phosphate buffer (pH 6. 08 mg/mL and exhibited postprandial hypoglycemic activity Mar 1, 2024 · Among the compounds tested against α-glucosidase inhibition activity, compound 3 was the most effective, with an IC 50 value of 14. (A) Absorption of glucose produced from carbohydrates by hydrolytic glucosidase activity of α-glucosidase (AG) in the small intestine. 61 µM respectively, for α-glucosidase inhibition. The oral administration of compound 5 at a dose of 300 mg/kg significantly reduced the postprandial blood glucose levels of normal and streptozotocin (STZ)-induced diabetic mice. The reaction mixture consisted 100 mM McIlvaine buffer (pH 6. May 21, 2023 · Alpha-glucosidase inhibitors are pills that treat type 2 diabetes. Oct 9, 2023 · Determination of inhibition activity against α-glucosidase enzyme. According to the in vitro assay results, compound 3b with p-dimethylamino on the cinnamoyl ring has the best α-glucosidase inhibitory activity. e. 2 mmol acarbose equivalent (ACAE)/g. Jun 1, 2017 · The α-glucosidase inhibitors delay intestinal carbohydrate absorption by blocking the activity of glucosidase enzyme, and consequently reduce the concentration of postprandial blood glucose and slow down the rise in blood sugar level; therefore, they play a significant role as chemotherapeutic agents for non-insulin-dependent DM. 2. 1 Jun 19, 2014 · In in vitro yeast α-glucosidase inhibition assays, CMPE was much more effective (IC 50 = 0. 31 μM to 127. 2 μg/ml). 5 U/mL in 0. α-Glucosidase inhibitors proved to be effective and safe both in monotherapy and as an add-on to other anti-diabetic drugs. 26 μM) was the strongest inhibitor in the series with 2- and 21-fold improved Jan 18, 2022 · The first alpha-glucosidase inhibitor (AGI), acarbose, was approved by the FDA as an antihyperglycemic agent in 1995 and the second AGI, miglitol, followed in 1996. • The most potent α-glucosidase enzyme inhibition of quinoa peptides obtained from trypsin hydrolysis (0. However, few hybrids of β-carboline with 1,3,4-oxadiazole have been reported as α-glucosidase inhibitors. 05 mM against intestinal sucrase. The glycemic efficacy, adverse effects, and dosing of alpha-glucosidase inhibitors will be discussed here. Jul 5, 2023 · In order to find potential α-glucosidase inhibitors, a series of β-carboline derivatives containing piperazine moieties were synthesized by gradual structure optimization (Fig. Network pharmacology analysis revealed that the betulinic acid derivative P3 exerted Aug 29, 2021 · In the current study, we screened 7 clonal lines from single seed phenotypes of Lamiaceae family for the inhibition of alpha-amylase, alpha-glucosidase and angiotensin converting enzyme (ACE Feb 1, 2024 · This suggests that variations in molecular size may play a crucial role in their interaction with α-glucosidase. 38 ± 6. Nov 1, 2023 · Chai T-T, Kwek M-T, Ong H-C, Wong F-C. 3 μM. 8) were mixed with 10 μL of the test Sep 9, 2020 · Recently the use of bioactive α-glucosidase inhibitors for the treatment of diabetes have been proven to be the most efficient remedy for controlling postprandial hyperglycemia and its detrimental physiological complications, especially in type 2 diabetes. Feb 16, 2024 · Inhibiting the activity of intestinal α-glucosidase is considered an effective approach for treating type II diabetes mellitus (T2DM). Jan 8, 2024 · Concerning the α-glucosidase inhibition, naringenin was recorded to exhibit stronger inhibitory activity than acarbose in the same condition in the majority of the reported results. Because pAPG is the Dec 18, 2019 · Type-2 diabetes mellitus is one of the most prevalent metabolic diseases in the world, and is characterized by hyperglycemia (i. Jul 28, 2021 · 2. 5- … Jul 18, 2016 · α-amylase and α-glucosidase digest the carbohydrates and increase the postprandial glucose level in diabetic patients. Phosphate group in glycerides increases α-glucosidase inhibitory activity. With Feb 15, 2024 · Flavonoid consists of an extensive range of compounds with variable inhibitory activities against alpha-glucosidase, implicating its role in the prevention and treatment of diabetes caused by uncontrolled increases in the blood glucose level. Mar 15, 2022 · Syringic and vanillic acids showed the lowest inhibition against α-glucosidase in the M1 AG and M2 AG. Sep 9, 2012 · Among the gallated catechins, EGCG was the most potent α-glucosidase inhibitor, with IC 50 and IC 90 values basically identical to those of Teavigo®. So we designed experiments to clarify these properties. Inhibiting the activity of these two enzymes can control postprandial hyperglycemia, and reduce the risk of developing diabetes. 50 µM [ 33 Mar 1, 2023 · Moreover, all the isolated compounds were tested for their α-glucosidase inhibitory activities, compounds (+)-1, (−)-1 and (+)-2 exhibits significant α-glucosidase inhibitory activity. 25% Tetrahedron 62 (2006) 10277–10302 Tetrahedron report number 773 a- and b-Glucosidase inhibitors: chemical structure and biological activity Eduardo Borges de Melo,a Adriane da Silveira Gomesb and Ivone Carvalhob,* a Colegiado de Farm acia/UNIOESTE, Rua Universit aria, 2069 Cascavel, PR 85814-110, Brazil Faculdade de Ci^ encias Farmac^ euticas de Ribeir~ ao Preto/USP, Av. 1, C∼1D) and suggested that β-carboline skeleton closely binds to α-glucosidase active pocket, making β-carboline a core skeleton for the development of α-glucosidase inhibitors [42, 43]. 11 In vivo experiments described that administration in the rats of an inhibitor for about 4 weeks led to a highly significant decrease in the Another possible mechanism followed by flavonoid compounds (luteolin, kaempferol, chrysin, and galangin) to control blood glucose levels is the inhibition of α-amylase and α-glucosidase activity in the intestine. 66 ± 0. In selecting medicinal plants, a specific specimen with the lowest IC 50 value or the highest inhibition of α-glucosidase activity was deliberately chosen. Results: SP-GI exhibited significant inhibitory activity with an IC 50 of 2. , high levels of glucose in the blood). Among cyanidin, cyanidin-3,5-diglucoside and cyanidin-3-galactoside, the α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. All the compounds tested displayed better enzyme inhibition activity compared to acarbose (IC 50 = 817. 81 μM), all compounds (C1 ∼ 36) showed stronger α-g … Oct 1, 2023 · The contents of glycosides were positively correlated with α-glucosidase inhibition activities. Curr Anal Chem. , 2013; Zhang et al. 126 Furthermore Nov 4, 2020 · Cereal‐derived phenolic compounds, peptides, nonstarch polysaccharides, and lipids inhibit α‐amylase and α‐glucosidase activity. 242 peptides binding to α-glycosidase were quickly screened and identified by bio-affinity ultrafiltration combined with LC-MS/MS from the double enzymatic hydrolysate of black beans. 145 on 26/04/2023 at 08:21 May 18, 2024 · Structure activity relation for α-glucosidase inhibition potential was developed from Table 1 by analyzing the effect of various aldehyde substituents, R and data of inhibition of the most active Alpha-glucosidase inhibitors. - DOI - PubMed Sep 23, 2014 · A colorimetric method has been established for α-glucosidase activity assay and its inhibitor screening. Dec 1, 2021 · The inhibitor obtained from A. Feb 28, 2024 · Alpha-glucosidase inhibitors inhibit the absorption of carbohydrates from the small intestine. 41 µg/mL (20 µM). Sub-fraction A which was eluted with 5% EtOAc/ n -hexane, was further purified using a Chromatotron device) (San Bruno, CA, USA) (0. Due to above reasons, fraction 2 of A. 0 μM as well as a mix-type inhibitor. Structure activity pattern suggested that substituted phenyl ring on N-methylindole in the structure has Nov 9, 2012 · We conducted a review analyzing the clinical efficacy and safety of α-glucosidase inhibitors, both alone and in combination with other anti-diabetic drugs, with respect to glycemic control, inflammation and atherosclerosis. The inhibitory activity toward lysosomal acid α-glucosidase (GAA) was measured with Myozyme (Genzyme; Boston, MA, USA) as the enzyme source, and 4-methylumbelliferyl-α-d-glucopyranoside (Sigma-Aldrich Co. α-glucosidase is a brush border enzyme which hydrolyzes starches and disaccharides to glucose for absorption from the intestine. 85 ± 4. Jul 9, 2024 · Particularly, compound 5k possessed the best inhibitory activity against α-glucosidase with around a 28-fold improvement in the inhibition effect in comparison standard inhibitor. Enzyme kinetic inhibition plots suggested that CMPE is a non-competitive inhibitor of α-glucosidase. Sep 1, 2021 · The inhibition of α-glucosidase activity was determined by the procedure described earlier [75]. 9 ± 0. Dec 18, 2019 · Basic modes of action of α-glucosidase inhibitors (AGIs). 16 mg/mL. 20 to at most 121. 38 µM) and α-glucosidase (IC 50 = 11. Acarbose, a microbial carbohydrate and an alpha-glucosidase inhibitor, is cur … Jan 1, 2019 · A class of new phenyloxazole derivatives (6a-6p) was synthesized, and their inhibitory activities towards α-glucosidase were researched. Jan 1, 2024 · The role of bioactive peptides in diabetes management has attracted extensive attention. Such interactions also play a crucial role in the binding of inhibitors with α-glucosidase [36, 37]. Food Chem. 5 mg galantamine equivalent (GALAE)/g and anti-glucosidase activity measuring 1. Feb 14, 2024 · These treatments are accompanied by side effects (flatulence, diarrhea). of α-glucosidase inhibitor that inhibited 50% of α-glucosidase activity. Further molecular docking experiments showed that (+)- 1 , (−)- 1 , and (+)- 2 could bind in the same active pocket and their inhibition is closely related May 1, 2024 · This work aimed to propose a rapid method to screen the bioactive peptides with anti-α-glucosidase activity instead of traditional multiple laborious purification and identification procedures. The activity of these plant extracts can be attributed to the phytoconstituents present in them. Nov 15, 2020 · The manuscript aims to compare the similarity and discrepancy in the physicochemical properties, antioxidant activity and inhibition of α-glucosidase activity of CSP extracted by hot water, acid-assisted, alkali-assisted and ultrasonic-assisted methods, also to understand the mechanisms of interaction between CSP with α-glucosidase. However, most of the current antidiabetic drugs in the clinic have many side effects. 5 h, 3 kDa ≥). Feb 9, 2019 · The lower absorbance indicates the stronger suppression on enzymatic activity. In order to find effective α-glucosidase inhibitors, a series of thiazolidine-2,4-dione derivatives (C1 ∼ 36) were synthesized and evaluated for α-glucosidase inhibitory activity. , 2022). In this study, we employed an in vitro enzymatic synthesis approach to synthesize four derivatives of natural products (NPs) for the discovery of therapeutic drugs for T2DM. α-Glucosidase is responsible for the hydrolysis of dietary carbohydrates and starch into mono-saccharide in the body and tends to an increase in blood glucose level. Jul 14, 2020 · α-Glucosidase activity. 22 The inhibitors bind to these enzymes preventing breakdown of disaccharide and oligosaccharide substrates into absorbable monosaccharides Jul 23, 2010 · Different solvent extracts of Hypericum ascyron L. There are two medications in this group, or class, of drugs: acarbose and miglitol (). 86 μM. The compound classes isolated include: terpenes (61) from 14 genus, alkaloids (37) from 11 genus, quinines (49) from 4 genus, flavonoids (103) from 24 genus, phenols (37) from 9 genus, phenylpropanoids (73) from 20 genus, sterides (8) from 5 genus, and other types of Apr 20, 2005 · Alpha‐glucosidase inhibitors are reversible inhibitors of alpha‐glucosidase, an enzyme present in the brush border of the small intestine. Synthesis, in vitro inhibitor screening, structure–activity relationship, and molecular dynamic simulation studies of novel thioquinoline derivatives as potent α-glucosidase Aug 10, 2007 · Variations in α-glucosidase inhibitory activity in Morus leaves were previously observed in association with polyploidy of the same variety []. In addition, continuous hyperglycemia in diabetic patients accelerates non-enzymatic glycation and increases the production of advanced glycation end products (AGEs) [ 5 ]. Nov 19, 2020 · The biological evaluation of the isolated compound against alpha-glucosidase exhibited strong inhibitory activities for 3 and 2 with the half maximal inhibitory concentration (IC 50) values of 4. 2 ± 0. 99 ± 6. 099. In this study, the 1–3 kDa fraction of rice bran peptides (RBPs) was obtained by the hydrolysis of alkaline and dispase, and the following ultrafiltration demonstrated excellent α-glucosidase inhibition activity with an IC 50 value of 1. gardneri, showed a significant α-glucosidase inhibitory activity and acted as a competitive inhibitor. Acarbose, miglitol and voglibose are available α-glucosidase The studies enhanced knowledge of the mechanism by which α-glucosidase binds to imino sugars. Phytochemicals in wheat bran and germ contribute to its low GI property. 1 mol/L PBS) and 120 μL of 0. Mar 28, 2024 · The mode of inhibition of the most active compound 5k identified with the lowest IC 50 was investigated against α-glucosidase activity with different concentrations of p-nitrophenyl α-d Cyanidin-3-galactoside, a natural anthocyanin, was investigated for its alpha-glucosidase inhibitory activity. Eight known compounds were isolated from EtOAC Alpha-glucosidase inhibitors are saccharides that act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. Sep 23, 2015 · Compound 5, identified as the major constituent of the flower of E. 79%, 48. 27 mg/L and 863 ± 49 mg/L, respectively, which suggested that the inhibition potential of hypericin is superior to acarbose on α-glucosidase and significantly Oct 1, 2021 · According to a previous study, quercetin exhibited alpha-glucosidase inhibitory activity at IC 50 = 15 µM , slightly lower than the present result with IC 50 = 5. Biaugmentation of entomopathogenic microorganisms responsible for α-glycosidase inhibitors could be another major step forward in biocontrol studies. 7. Feb 22, 2022 · Inhibiting the α-glucosidase activity can alleviate postprandial hyperglycemia ; therefore, finding efficient α-glucosidase inhibitors (AGIs) has gained much attention . Louis, Mo, USA) as substrate. 17 ± 0. Pioglitazone is given as 15 mg, 30 mg, or 45 mg tablets daily. May 4, 2022 · Zhang H, Kallwass H, Young SP, Carr C, Dai J, Kishnani PS, Millington DS, Keutzer J, Chen YT, Bali D (2006) Comparison of maltose and acarbose as inhibitors of maltase-glucoamylase activity in assaying acid α-glucosidase activity in dried blood spots for the diagnosis of infantile Pompe disease. stamineus extract was determined following slightly modified methods described by 18. 40 In this study, the α-glucosidase Rahayu, et al. [19] Diabetes: Acarbose, an α-glucosidase inhibitor, competitively and reversibly inhibits α-glucosidase in the intestines. 2002 ). amygdalinum flower extracts and fractions. 8), 0. α-glucosidase Jul 11, 2023 · Nineteen biscoumarins were synthesized, well-characterized, and evaluated against α-glucosidases in vitro. 2018;14(5):458–64. Bioactive peptides are emerging as promising class of drugs that could serve as α-glucosidase inhibitors for the treatment of type 2 diabetes. All synthesized compounds displayed potential inhibition activity towards α-glucosidase with IC 50 values ranging between 48. Moreover, 1-deoxynojirimycin, a recognized α-glucosidase inhibitor, was Jan 1, 2012 · The inhibitor activity to alpha glucosidase was determined spectrophotometrically at 400 nm using p-Nitrophenyl-alpha-D-glucopyranoside as a substrate, and acarbose as a positive control. The activity of flavonoids was enhanced by the C3′ hydroxylation and increasing hydroxylations of Jan 8, 2024 · Concerning the α-glucosidase inhibition, naringenin was recorded to exhibit stronger inhibitory activity than acarbose in the same condition in the majority of the reported results. . , honokiol was ascertained for its anti-α-glucosidase activity and inhibition mechanism. 113 They hypothesized that the glucose competes with the substrate and replaces it to relieve substrate inhibition. This is the first time cycloartane triterpenoids were isolated in this genus. litura ( in vivo ). Feb 16, 2023 · Their α-glucosidase inhibitory activity greatly depended on their structure with electron-withdrawing groups on the cinnamoyl aromatic ring causing increased inhibition activity. Sep 21, 2017 · In vitro inhibition assay for α-glucosidase activity. [8,11,12] Phytochemical screening Phytochemical screening assay was per-formed as described in Harborne. 04 µM) comparable to the reference drug acarbose. Therefore, in this study, a new series of Oct 15, 2020 · However, the the activity of such molecules as alpha-glucosidase inhibitors was never assessed. Additionally, the intended substances were tested for their ability to inhibit α-glucosidase activity in a laboratory setting. Jun 18, 2024 · As a naturally occurring compound from Magnolia obovata Thunb. The inhibition effect is correlated to the concentration of the WFLE as the highest concentrations Oct 29, 2006 · Inhibition assays using intestinal α-glucosidase indicated that it was less potent against maltase and isomaltase, compared to 114 and 55, but was as potent as 55 against sucrase. The target benzimidazole 3f containing hydroxyl motif at para-position of phenyl revealed an important activity inhibitor against α- amylase (IC 50 = 12. 7 and 16. (2009) compared the α-glucosidase inhibitory activity of rutin, quercetin, and isoquercitrin by fluorescence spectroscopy and enzymatic kinetics, and the results showed that quercetin had the strongest activity for α-glucosidase inhibition, followed by isoquercitrin and rutin, which is consistent with our study (Li et al. Jul 2, 2021 · α-glucosidase inhibitors reduce postprandial hyperglycemia by interfering with the activity of carbohydrate digestive enzymes and delaying the absorption of glucose . Oct 25, 2022 · A study on α-glucosidase inhibition by berry anthocyanins in vitro showed that acylated anthocyanins had higher inhibition activity against this enzyme than deacylated forms, which was probably a result of the stability of acylated anthocyanins at the intestinal pH . Apr 1, 2016 · All compounds were evaluated for their inhibitory activities against α-glucosidase (from Saccharomyces cerevisiae). Download: Download high-res image (189KB) Jan 4, 2024 · Forozan, R. 353 µg mL −1. 411 compounds exhibiting α-glucosidase inhibitory activity were summarized and isolated them from medicinal plants. : In vitro Antioxidant Properties and Dec 7, 2011 · Inhibition modes of sample that had the best α-glucosidase inhibiting activity in Clusiaceae, Euphorbiaceae, and Rubiaceae were measured with increasing concentration of p-nitrophenyl α-D-glucopyranoside as a substrate in the absence or presence of ethanolic extract at different concentrations. They help keep the amount of glucose in your glucosidase Activity and Screening of Its Inhibitors Yanyan Liu, Hongmei Li, Ling Lu et al. , 2015 Jan 6, 2021 · Granados-Guzman G, Castro-Rios R, Waksman de Torres N, Salazar-Aranda R. Unsaturated fatty acids in glycerides increase α-glucosidase Type 2 diabetes is mainly induced by environmental factors such as being overweight, decreased physical activity and inbalanced energy metabolism, such as pancreatic beta-cell dysfunction and peripheral insulin resistance. Evaluation of α-Glucosidase Inhibition. Vildagliptin is Jan 15, 2021 · In this study, a simple and portable enzyme activity assay and inhibitor screening method was developed based on β-Glucosidase-mediated cascade reaction in a personal glucose meter (PGM). Phosphatidic acids are potent inhibitors of α-glucosidase enzymic hydrolysis. 1 µmol L -1 and this inhibition was reversible and non-competitive with a K i value of 1. Of which, the activity of TDBS, TDBB and TDBW extracts were extraordinarily higher than that of standard acarbose. The IC(50) value of cyanidin-3-galactoside was 0. Dec 30, 2019 · The sub-fractions were tested for α-amylase and α-glucosidase inhibitory activity; the sub-fraction (A and B) which showed the highest inhibition was further analyzed. jamaicensis leaves displays inhibition of DPPH, ABTS and α-glucosidase activity compared to other solvent extracts. May 15, 2011 · Research highlights Lipophilic components in wheat bran and germ inhibit α-glucosidase hydrolysis. Apr 1, 2018 · The inhibition mode suggests that the compounds bind at both the active site and other regions of the enzyme, resulting in structural changes and activity inhibition. Of these, six compounds (10, 12, 16, and 17–19) were newly synthesized and not previously reported in the chemical literature. This inhibition lowers the rate of glucose absorption through delayed carbohydrate digestion and extended digestion time. The α-glucosidase activity was measured using a method of Tadera et al. Diabetes mellitus is the most serious, chronic metabolic disorder and is characterized by high blood glucose levels. , 2010). This article identifies structural and physicochemical requirements for the design of therapeutically relevant α-glucosidase inhibitory peptides. 2014. In summary, all target compounds showed remarkable α-glucosidase inhibitory activity, highlighting the potential of apigenin analogs as novel α-glucosidase inhibitors. Kinetics of α-glucosidase inhibition Nov 15, 2022 · The α-glucosidase inhibitory activity of compounds (1 ∼ 6) was detected as described in previous reports (Adisakwattana et al. The α-glucosidase activity was calculated by measuring the amount of p-nitrophenol hydrolyzed from pNPG by α-glucosidase. 77. 125 Despite the low activity of the natural sulfonium ion toward glucoamylase, product 116 exhibited a 10-fold higher inhibition value than 114. Activity assays showed that honokiol was a reversible mixed-type inhibitor of α-glucosidase, and its IC 50 value was 317. 27 μM). The α-glucosidase inhibitory activity of quercetin analogs was evaluated as described in a previous report with modifications (Taj et al. Tested enzyme was prepared using α-glucosidase included in commercial rat intestinal acetone powder (Sigma-Aldrich). As it was described for α-amylase, hydroxyl groups might play an important role on α-glucosidase inhibition too (Xiao, Kai, Yamamoto, & Chen, 2013 May 1, 2023 · Alpha-glucosidase inhibitors are available as 25 mg, 50 mg, or 100 mg tablets, given three times a day just before meals. Jan 8, 2021 · Its inhibition is an effective solution to delay glucose absorption and also prevent high postprandial blood glucose levels, which may probably suppress diabetes progression. do Cafe´ s/n Sep 1, 2014 · Results. 2) and monitored their anti-α-glucosidase activity. 10 μl α-glucosidase solution, 10 μl compound were added into 80 μl phosphate buffer, and the mixture was incubated for 10 min. In this study, the inhibition of hypericin by α-glucosidase and its mechanism were firstly investigated using enzyme kinetics analysis, real-time interaction analysis between hypericin and α-glucosidase by surface plasmon resonance (SPR), and molecular docking simulation. 5% EtOAc/ n -hexane) to yield 3-oxolupenal Jun 28, 2023 · Molecular docking analysis of representative saponins with α-glucosidase inhibitory activity was performed. The inhibition of α-glucosidase was established with the help of the modified version of the published technique . In addition, during the lengthly development of paclitaxel and docetaxel as anti-cancer agents, experiments showed that these molecules are non-water-soluble making their delivery more challenging (Singla et al. The heat map was adopted to offer presentation of the concentration and α-glucosidase inhibition activity difference of SP samples collected from different geographical origins (Fig. , 2014). Jul 1, 2024 · The inhibitory activity of flavonoids is closely related to their structure, 3′-OH at ring B, 3-OH, C 4 = O and C 2 = C 3 at ring C, as well as the trans-conformation of C 2-C 3 were important active sites in the α-glucosidase inhibition [52]. Therefore, inhibiting the function of these enzyme in type 2 diabetic patients reduces hyperglycemia. ; St. awamori also strongly affected the activity of α-amylase and α-glucosidase of S. However, the research on the structure Nov 10, 2019 · 3. 39 μM. The interaction of the potent inhibitor with α-glucosidase and its cell cytotoxicity were also investigated. In order to evaluate the feasibility of the design principle using PGM based on β-Glucosidase-mediated cascade reaction, five kinds of solution were measured using PGM in the same way as Jul 1, 2020 · The antioxidant activity and high alpha glucosidase inhibition activity of ‘fraction-14’ is comparable to the earlier studies and, the presence of phenolics was confirmed by phytochemical study. Enzyme kinetics data fit to LB plot pointed out competitive mode of inhibition and the membrane dialysis experiment revealed Alpha-glucosidase inhibitors retard carbohydrate digestion via competitive inhibition of the activity of α-glucosidase enzymes located in the brush border of the enterocytes that line the intestinal villi. Jan 15, 2021 · Thus, β-Glucosidase activity and inhibitors screening assay can be performed without any additional modification to the PGM, β-Glucosidase and substrate. (B–D) Competitive, non-competitive (allosteric), and uncompetitive inhibition of the AG activity by AGIs, respectively. Aug 16, 2021 · However, the the activity of such molecules as alpha-glucosidase inhibitors was never assessed. Plants and herbs are rich with secondary metabolites that have massive pharmaceutical potential. Inhibition of α-Glucosidase by Hypericin and Acarbose. 12. showed maximum inhibition potential against α-glucosidase enzyme, docking studies were performed to investigate the activity of some of its already reported chemical constituents (betulinic acid, epibetulin, arjunolic acid, lupeol, maslinic acid, and betulin) [6, 7]. [1,2] α-Glucosidase (α-d-glucoside glucohydrolase) is an exo-type carbohydrase distributed widely in Feb 8, 2022 · The extract from fermented okara broth acted in a dose-dependent manner to inhibit α-glucosidase activity, with an IC 50 value of 0. 1. Feb 1, 2024 · α-Glucosidase (α-Glu) is an enzyme that plays an essential role in the digestion of carbohydrates, and its activity detection and inhibitor screening are crucial for the therapy of diseases and development of new drugs. Using a high throughput-compatible assay to screen for potential alpha-glucosidase inhibitors, we found that the beta-lactam antibiotic ceftezole exhibited potent alpha-glucosidase inhibitory activity. In the reaction, 30 μL of α-glucosidase (0. In recent years, much emphasis has been placed on identifying peptides with α-glucosidase inhibitory activity and elucidating the mechanisms underlying their inhibitory effect in treating T2DM. • Decreasing the peptide size leads to higher α-glucosidase inhibition activity of trypsin samples. A series of isolated xanthones (1-16) demonstrated modest to high inhibition of α-glucosidase with IC(50) values of 1. 58 ± 6. In recent years, a plenty of research works have been conducted looking for novel and effective α-glucosidase inhibitors (AGIs) from natural sources as alternatives for the synthetic AGI due to their unpleasant side effects. 28 and 0. These inhibitors have played a vital role in revealing the functions of glucosidases in living system by modifying or blocking specific metabolic processes; and, this revelation led to several applications of these chemical entities in agriculture and Mar 15, 2023 · The inhibition of α-glucosidase activity has been recognized as an effective approach for treating type 2 diabetes mellitus (T2DM). The inhibition activity of hypericin against α-glucosidase showed a dose-dependent manner (Figure 1 A). As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organise … Glucosidase inhibitors have also been useful in probing biochemical pathways and understanding structure–activity relationship patterns required for mimicking the enzyme transition state. , 2009; Adisakwattana et al. S-GFP effectively inhibited the activity of α-glucosidase with an IC 50 value of 3. - Glucosidase inhibitory activity of breadfruit leaf extract ( Artocarpus altilis (parkinson) fosberg) H Rante, G Alam and M Irwan-This content was downloaded from IP address 40. , 2009) and suggested that inhibiting of α-glucosidase was a result of multiple interactions with the enzyme. 4 ± 1. Jun 5, 2023 · All the synthesized compounds were evaluated them for their α-glucosidase inhibitory potential Among them, compound 129 and 130 were the most potent with IC 50 values of 0. Alpha-glucosidases are enzymes in the digestive tract that hydrolyze carbohydrates into glucose. 0 ± 0. 13 to 50. Feb 8, 2016 · To evaluate the quality, an ultra-high performance liquid chromatography coupled with quadrupole time of flight mass spectrometry (UPLC-Q-TOF/MS) method was developed for identification of polyhydroxylated alkaloids with α-glucosidase inhibitor activity in mulberry leaf. Oct 29, 2006 · Regarding the enzyme inhibition activity, the acetone/water extract of this plant exhibited significant AChE inhibition measuring 2. Today, only three synthetic inhibitors exist on the market, and there is a need for novel, natural and more efficient molecules exhibiting this activity. 6 Miscellaneous new glucosidase inhibitors were synthesized 7-10 and evaluated as α-glucosidase and α-amylase inhibitors. caudatum and fraction 4 of C. 45 ± 0. These peptides possess certain hypoglycemic activity and can effectively regulate postprandial blood glucose levels by inhibiting α-glucosidase activity, thus intervening and regulating diabetes. Mar 25, 2019 · As the methanolic extract of Cornus capitata Wall. 5 h, 10 kDa ≤). α-Glucosidase inhibitors such as acarbose, miglitol, and voglibose (shown in Figure 1) are the most well-known ones (Joshi et al. Inhibition of α-glucosidase delays carbohydrate absorption after a meal, lowering post-prandial glucose levels [40]. Glucosidase inhibitors are responsible for disruption of the activity of glucosidase, an enzyme that cleaves the glycosidic bond. 8) containing 200 mg of bovine serum albumin. , 2009). >8 mM of these polyphenols were needed to inhibit 50% of the maximum activity of the enzyme. 1 mol/L PBS (pH 6. One therapeutic approach to treat diabetes is to retard the absorption of glucose via inhibition of enzymes, such as α-glucosidase, in the digestive organs. These inhibitors may be associated with the prevention of hypoglycemia by whole cereal food intake (Figure 3). Acarbose, an antidiabetic, is the most widely used α-glucosidase inhibitor to treat diabetes and acts by delaying the release of glucose from polysaccharides by biding to α Apr 1, 2024 · α-Glucosidase inhibitory activity. 50 µM [ 33 Dec 1, 2012 · Some researchers have established the quantitative structure activity relationship (QSAR) model for xanthones and phthalimide derivatives as potent α-glucosidase inhibitor (Lee, Yong, et al. Amongst the various types of glucosidase inhibitors, disaccharides, iminosugars, carbasugars, thiosugars, and non-sugar derivatives have received great Sep 15, 2023 · Li et al. reported that α-glucosidase inhibitory activity of guava leaf water extract was 2. Oct 5, 2023 · Studies have suggested that bioactive peptides could serve as a potential source of α-glucosidase inhibitors. In this study, we investigated the ability of Tamarix nilotica ethanolic and aqueous shoot extracts, as The majority of the compounds were found to have potent α-glucosidase inhibition activity, with IC 50 values ranging from 5. 2015;186:26–31. npsv egyl fyjudx cmfwxf yjj tykgi gdyoub zujvf vcft wdgi