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The Houttuynia cordata Thunb. belongs to the Saururaceae family and is a well-known medicine and food homologous plant. Herein, the isolation of an α-glucosidase inhibitor from Houttuynia cordata Thunb. and characterization of its in vitro and in vivo hypoglycemic bioactivities are reported. We optimized the extraction conditions and isolated neochlorogenic acid (nCGA), which has α-glucosidase inhibitory activity from Houttuynia cordata Thunb. for the first time. nCGA competed with glucose for the α-glucosidase binding site, with a 50% inhibitory concentration (IC50) of 0.711 mg/mL. In vivo experiments in zebrafish showed that effects of nCGA on blood glucose varied by its concentrations. In particular, 4 mg/L nCGA significantly decreased the blood glucose level and inhibited effects of α-glucosidase in zebrafish. This work provides a theoretical basis for the extraction of hypoglycemic active ingredients from Houttuynia cordata Thunb. and a foundation for the development of natural and effective α-glucosidase inhibitors. [ABSTRACT FROM AUTHOR]

Agro-residues, including banana peel, pineapple peel, mango peel, apple peel, and coconut husk, were utilized to produce extracellular polysaccharide (EPS) via solid state fermentation(SSF) by the fungus, Trichoderma hamatum. EPS production was highest in pineapple peel (84.2 ± 0.4 mg/g), followed by mango peel (70.3 ± 0.41 mg/g) (p<0.01). The SSF bioprocess was optimized via a two-level full factorial design and response surface methodology. The effects of five selected variables on EPS biosynthesis, namely, the concentrations of glucose (10 to 30%), ammonium sulphate (0.1 to 1%), yeast extract (0.5 to 2%), MgSO4 (0.01 to 0.1%), and medium pH (4.5 to 6.5), were analyzed via a full factorial design (FFD). The EPS production ranged widely from 15.3 to 576.2 mg/g substrate. Three significant variables affecting EPS production were assessed in central composite design (CCD) to optimize concentrations of MgSO4, and glucose, and the pH. The designed CCD model was fitted to the quadratic model and was significant (p<0.0001). For 50 μL of EPS, the scavenging ratio was 43.4 ± 4.1% at a concentration of 200 μL (78.5 ± 6.9 μL) (p<0.01). The extracted EPS exhibited an alpha-glucosidase inhibitory effect (p<0.001). Solid-state fermentation allows the utilization of low-cost biomass for EPS production and the application of T. hamatum EPS as a natural antioxidant and α-glucosidase inhibitor. [ABSTRACT FROM AUTHOR]

The formation of atroposelective biaryl compounds in plants and fungi is well understood; however, polyketide aglycone synthesis and dimerization in bacteria remain unclear. Thus, the biosynthetic gene cluster (BGC) responsible for antibacterial setomimycin production from Streptomyces nojiriensis JCM3382 was examined in comparison with the BGCs of spectomycin, julichromes, lincolnenins, and huanglongmycin. The setomimycin BGC includes post-polyketide synthase (PKS) assembly/cycling enzymes StmD (C-9 ketoreductase), StmE (aromatase), and StmF (thioesterase) as key components. The heterodimeric TcmI-like cyclases StmH and StmK are proposed to aid in forming the setomimycin monomer. In addition, StmI (P-450) is predicted to catalyze the biaryl coupling of two monomeric setomimycin units, with StmM (ferredoxin) specific to the setomimycin BGC. The roles of StmL and StmN, part of the nuclear transport factor 2 (NTF-2)-like protein family and unique to setomimycin BGCs, could particularly interest biochemists and combinatorial biologists. α-Glucosidase, a key enzyme in type 2 diabetes, hydrolyzes carbohydrates into glucose, thereby elevating blood glucose levels. This study aimed to assess the α-glucosidase inhibitory activity of EtOAc extracts of JCM 3382 and setomimycin. The JCM 3382 EtOAc extract and setomimycin exhibited greater potency than the standard inhibitor, acarbose, with IC50 values of 285.14 ± 2.04 μg/mL and 231.26 ± 0.41 μM, respectively. Molecular docking demonstrated two hydrogen bonds with maltase-glucoamylase chain A residues Thr205 and Lys480 (binding energy = −6.8 kcal·mol−1), two π–π interactions with Trp406 and Phe450, and one π–cation interaction with Asp542. Residue-energy analysis highlighted Trp406 and Phe450 as key in setomimycin's binding to maltase-glucoamylase. These findings suggest that setomimycin is a promising candidate for further enzymological research and potential antidiabetic therapy. [ABSTRACT FROM AUTHOR]

Agro-residues, including banana peel, pineapple peel, mango peel, apple peel, and coconut husk, were utilized to produce extracellular polysaccharide (EPS) via solid state fermentation(SSF) by the fungus, Trichoderma hamatum. EPS production was highest in pineapple peel (84.2 ± 0.4 mg/g), followed by mango peel (70.3 ± 0.41 mg/g) (p

Abstract In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a–n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor. 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. This compound showed a competitive type of inhibition in the kinetics. The molecular docking and dynamics demonstrated that compound 5k with a favorable binding energy well occupied the active site of α-glucosidase.

Abstract Olive (Olea europaea) phytochemicals are associated with a reduced risk of type 2 diabetes. Table olives typically have higher phytochemical concentrations than olive oil, but their impact on human intestinal α-glucosidase is largely unknown. Shinzuke, the most common trade preparation in Japan, are alkali-treated non-fermented green olives. In contrast, natural olives are debittered by brining, which may enhance phytochemical retention. We evaluated the α-glucosidase inhibitory effect of Shinzuke and natural green olives produced in-house and compared them with commercial table olives. Eight types of table olives were tested against human intestinal α-glucosidase. Shinzuke Mission was the least effective (IC50 0.710 ± 0.058 mg/mL), while Natural green olives showed double to triple activity, with a non-competitive mechanism. Natural table olives retained more phytochemicals than shinzuke and other treated olives, and are good inhibitors of human α-glucosidase in vitro, exhibiting potential as a functional food for the management of postprandial glycaemia. Graphical Abstract

A talented endophytic Streptomyces sp. PH9030 is derived from the medicinal plant Kadsura coccinea (Lem.) A.C. Smith. The undescribed naphthoquinone naphthgeranine G (5) and seven previously identified compounds, 6–12, were obtained from Streptomyces sp. PH9030. The structure of 5 was identified by comprehensive examination of its HRESIMS, 1D NMR, 2D NMR and ECD data. The inhibitory activities of all the compounds toward α-glucosidase and their antibacterial properties were investigated. The α-glucosidase inhibitory activities of 5, 6, 7 and 9 were reported for the first time, with IC50 values ranging from 66.4 ± 6.7 to 185.9 ± 0.2 μM, as compared with acarbose (IC50 = 671.5 ± 0.2 μM). The molecular docking and molecular dynamics analysis of 5 with α-glucosidase further indicated that it may have a good binding ability with α-glucosidase. Both 9 and 12 exhibited moderate antibacterial activity against methicillin-resistant Staphylococcus aureus, with minimum inhibitory concentration (MIC) values of 16 μg/mL. These results indicate that 5, together with the naphthoquinone scaffold, has the potential to be further developed as a possible inhibitor of α-glucosidase. [ABSTRACT FROM AUTHOR]

Olive (Olea europaea) phytochemicals are associated with a reduced risk of type 2 diabetes. Table olives typically have higher phytochemical concentrations than olive oil, but their impact on human intestinal α-glucosidase is largely unknown. Shinzuke, the most common trade preparation in Japan, are alkali-treated non-fermented green olives. In contrast, natural olives are debittered by brining, which may enhance phytochemical retention. We evaluated the α-glucosidase inhibitory effect of Shinzuke and natural green olives produced in-house and compared them with commercial table olives. Eight types of table olives were tested against human intestinal α-glucosidase. Shinzuke Mission was the least effective (IC50 0.710 ± 0.058 mg/mL), while Natural green olives showed double to triple activity, with a non-competitive mechanism. Natural table olives retained more phytochemicals than shinzuke and other treated olives, and are good inhibitors of human α-glucosidase in vitro, exhibiting potential as a functional food for the management of postprandial glycaemia. [ABSTRACT FROM AUTHOR]

Background The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Methods Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan’s multiple range test at α=0.05. Results Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC 50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC 50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. Conclusions This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

One of the global health issues is diabetes mellitus, characterized by elevated blood glucose levels. The absorption of glucose in the body occurs through the digestion of carbohydrates by the enzyme α-glucosidase, which is responsible for hydrolyzing carbohydrates into sugar. Ashitaba (Angelica keiskei) is a herbal plant from Japan and has long been utilized in traditional medicine for its various health benefits and preventive properties against multiple diseases. This plant has also been cultivated in Indonesia, including Trawas Mojokerto, East Java. This study aims to develop ashitaba crackers and evaluate their potential α-glucosidase inhibitory activity to develop safe and effective natural products to assist in managing diabetes more efficiently. This research was conducted from July to September 2022. Two formulations of fresh ashitaba leaves were used (12% CAST 1 and 18% CAST 2 of 100 g of flour). Based on the results of this research, chemical composition tests showed that the carbohydrate and dietary fiber content in CAST 1 were higher than those in CAST 2. Protein, lipid, water, and ash content in CAST 2 had higher values than in CAST 1. Flavonoid content and inhibitory activity test results of ashitaba crackers showed significant differences between the two formulation groups regarding flavonoid content and percentage inhibition against the α-glucosidase enzyme. Both flavonoid content and inhibitory activity in CAST 2 were higher than in CAST 1. Ashitaba crackers with the best formulation in this study, based on flavonoid levels and their ability to inhibit α-glucosidase enzyme, were identified as CAST 2. [ABSTRACT FROM AUTHOR]

Two α-pyrone analogs were isolated from the endophytic fungus Diaporthe sp. CB10100, which is derived from the medicinal plant Sinomenium acutum. These analogs included a new compound, diaporpyrone F (3), and a known compound, diaporpyrone D (4). The structure of 3 was identified by a comprehensive examination of HRESIMS, 1D and 2D NMR spectroscopic data. Bioinformatics analysis revealed that biosynthetic gene clusters for α-pyrone analogs are common in fungi of Diaporthe species. The in vitro α-glucosidase inhibitory activity and antibacterial assay of 4 revealed that it has a 46.40% inhibitory effect on α-glucosidase at 800 μM, while no antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), Mycolicibacterium (Mycobacterium) smegmatis or Klebsiella pneumoniae at 64 μg/mL. Molecular docking and molecular dynamics simulations of 4 with α-glucosidase further suggested that the compounds are potential α-glucosidase inhibitors. Therefore, α-pyrone analogs can be used as lead compounds for α-glucosidase inhibitors in more in-depth studies. [ABSTRACT FROM AUTHOR]

Objective: Graptophyllum pictum (L.) Griff is a medicinal shrub belonging to the Acanthaceae family and is traditionally used to treat various diseases. Therefore, this study aimed to evaluate the pharmaceutical properties and phytochemical profiles of the methanolic extract of G. pictum. Materials and Methods: G. pictum leaves was extracted using methanol. Antioxidant, cytotoxic on Michigan Cancer Foundation-7 (MCF-7) and HepG2, antidiabetic, and antibacterial properties were evaluated in vitro. Chemical profile of the extract was identified through qualitative (for phytochemicals), quantitative (for phenolic and flavonoid content), and gas chromatography-mass spectrometry (GC-MS) analysis. Results: The results showed that the extract had potent antioxidant activity against 2,2-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) and 2,2-diphenyl-1-picrylhydrazyl radicals with IC50 values of 49.00 ± 3.20 µg/mL and 70.18 ± 3.27 µg/mL, respectively. It also exhibited cytotoxic effects on human breast (MCF-7) and liver (HepG2) carcinoma cells with growth inhibition percentages of 74.29 ± 1.53% and 64.90 ± 1.94%, respectively. The antidiabetic assay showed that the extract had inhibitory effects on a-glucosidase activity with IC50 value 194.59 ± 15.59 µg/mL, indicating its potential to be developed as an antidiabetic agent. Furthermore, it had antibacterial properties against four test strains, and the highest activity was found against Bacillus subtilis American Type Culture Collection 19659, with minimum inhibitory concentration and minimum bactericidal concentration values of 625 µg/mL and 1250 µg/mL, respectively. Phytochemical tests indicated the presence of alkaloids, flavonoid and terpenoids in the extract, with total phenolic content and total flavonoid content of 41.17 ± 2.38 mg gallic acid equivalents/g and 26.52 ± 0.61 mg quercetin equivalent/g, respectively. GC-MS analysis revealed that it contained several active compounds, including eicosane, 2,4-Di-tertbutylphenol, hentriacontane, tetracosane, octacosane, sulfurous acid, 2-methylhexacosane, docosane, heneicosane, 1-propene-1,2,3-tricarboxylic acid, tributyl ester, and pentacosane. Conclusion: The extract derived from G. pictum leaves was a potential source of therapeutic compounds, particularly for antioxidant, antidiabetic, anticancer, and antibacterial agents. [ABSTRACT FROM AUTHOR]

Background The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Methods Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan’s multiple range test at α=0.05. Results Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. Conclusions This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

Nine new compounds (1–9), including four dihydrochalcone glycosides, two dibenzofuran glycosides, and two biphenyl glycosides, were isolated from the leaves of the medicinal plant Malus hupehensis collected in Shennongjia Forestry District (Hubei, China). Their structures were elucidated by comprehensive spectroscopic techniques, including HRESIMS and NMR spectra. All compounds were tested by preliminary biological evaluation for their α-glucosidase inhibitory and NO production activities. Compound 4 was found to show significant inhibitory activity against NO production in LPS-activated RAW 264.7 macrophage cells with an IC50 value of 29.60 μM, and compounds 3 and 4 were found to exhibit potent α-glucosidase inhibition with IC50 values of 44.17 and 60.15 μM, respectively. This work represents the first report of the diverse glycosides from the plant Malus hupehensis. It expands our understanding of the secondary metabolites of this medicinal plant and lays the foundation for the study of the bioactive principles of the ethnic hypoglycemic medicinal plant.

Background The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Methods Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan’s multiple range test at α=0.05. Results Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC 50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC 50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. Conclusions This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

Four new glycosides, named amplexicosides A-D (1–4), and five known compounds: benzyl 2-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyloxy]-benzoate (5), benzyl 2-neohesperidosyloxy-6-hydroxybenzoate (6), chrysandroside A (7), chrysandroside B (8) and camelliquercetiside C (9) were isolated from the branches and leaves of Camellia amplexicaulis (Pit.) Cohen-Stuart. Their structures were elucidated using HR-ESI-MS and 1D- and 2D-NMR spectra and compared to reported NMR data. All of the isolated compounds were screened in an α-glucosidase assay. Compounds 4, 8, and 9 significantly inhibited α-glucosidase with respective IC50 values of 254.9 ± 4.2, 304.8 ± 11.9 and 228.1 ± 16.4 μM. [ABSTRACT FROM AUTHOR]

Three new catecholic compounds, named meirols A–C (2–4), and one known analog, argovin (1), were isolated from the marine-derived fungus Meira sp. 1210CH-42. Their structures were determined by extensive analysis of 1D, 2D NMR, and HR-ESIMS spectroscopic data. Their absolute configurations were elucidated based on ECD calculations. All the compounds exhibited strong antioxidant capabilities with EC50 values ranging from 6.01 to 7.47 μM (ascorbic acid, EC50 = 7.81 μM), as demonstrated by DPPH radical scavenging activity assays. In the α-glucosidase inhibition assay, 1 and 2 showed potent in vitro inhibitory activity with IC50 values of 184.50 and 199.70 μM, respectively (acarbose, IC50 = 301.93 μM). Although none of the isolated compounds exhibited cytotoxicity against one normal and six solid cancer cell lines, 1 exhibited moderate cytotoxicity against the NALM6 and RPMI-8402 blood cancer cell lines with GI50 values of 9.48 and 21.00 μM, respectively. Compound 2 also demonstrated weak cytotoxicity against the NALM6 blood cancer cell line with a GI50 value of 29.40 μM. [ABSTRACT FROM AUTHOR]

Sucrose is a disaccharide that is degraded into fructose and glucose in the small intestine. High-sucrose and high-fructose diets have been reported, using two-dimensional imaging, to alter the intestinal morphology and the expression of genes associated with sugar transport, such as sodium glucose co-transporter 1 (SGLT1), glucose transporter 2 (GLUT2), and glucose transporter 5 (GLUT5). However, it remains unclear how high-fructose and high-sucrose diets affect the expression of sugar transporters and the intestinal morphology in the whole intestine. We investigate the influence of a chronic high-sucrose diet on the expression of the genes associated with sugar transport as well as its effects on the intestinal morphology using 3D imaging. High sucrose was found to increase GLUT2 and GLUT5 mRNA levels without significant changes in the intestinal morphology using 3D imaging. On the other hand, the delay in sucrose absorption by an α-glucosidase inhibitor significantly improved the intestinal morphology and the expression levels of SGLT1, GLUT2, and GLUT5 mRNA in the distal small intestine to levels similar to those in the proximal small intestine, thereby improving glycemic control after both glucose and sucrose loading. These results reveal the effects of chronic high-sugar exposure on glucose absorption and changes in the intestinal morphology. [ABSTRACT FROM AUTHOR]

Erythrina variegata L., a member of the Fabaceae family, is a valuable medicinal plant with a rich history of traditional medicinal uses. However, its potential as an antidiabetic agent has remained largely unexplored. In this study, three isoflavonoid compounds, namely eryvarin M (1), eryvarin H (2), and neobavaisoflavone (3), were isolated from E. variegata. These compounds displayed significant inhibitory effects on both protein tyrosine phosphatase 1B and α-glucosidase enzymes. The specific attachment position of the prenyl group to the isoflavonoid skeleton plays a pivotal role in determining the variation in their activity. Moreover, the results obtained from docking simulations corroborate the experimental findings, confirming the robust binding affinities of these metabolites toward the target proteins. The docking analysis further highlights that these compounds exhibit highly negative values of binding-free energies against proteins, indicative of their favorable binding affinities. In addition, the formation of hydrogen bonds in the binding region contributes to their binding interactions. These findings significantly enhance our understanding of the therapeutic potential of both E. variegata and its isoflavonoids as potential inhibitors for diabetes and related metabolic disorders, shedding light on their promising role in the field of diabetes research. [ABSTRACT FROM AUTHOR]

Hematoxylin (HT) as a natural phenolic dye compound is generally used together with eosin (E) dye as H&E in the histological staining of tissues. Here, we report for the first time the polymeric particle preparation from HT as poly(Hematoxylin) ((p(HT)) microgels via microemulsion method in a one-step using a benign crosslinker, glycerol diglycidyl ether (GDE). P(HT) microgels are about 10 µm and spherical in shape with a zeta potential value of −34.6 ± 2.8 mV and an isoelectric point (IEP) of pH 1.79. Interestingly, fluorescence properties of HT molecules were retained upon microgel formation, e.g., the fluorescence emission intensity of p(HT) at 343 nm was about 2.8 times less than that of the HT molecule at λex: 300 nm. P(HT) microgels are hydrolytically degradable and can be controlled by using an amount of crosslinker, GDE, e.g., about 40%, 20%, and 10% of p(HT) microgels was degraded in 15 days in aqueous environments for the microgels prepared at 100, 200, and 300% mole ratios of GDE to HT, respectively. Interestingly, HT molecules at 1000 mg/mL showed 22.7 + 0.4% cell viability whereas the p(HT) microgels exhibited a cell viability of 94.3 + 7.2% against fibroblast cells. Furthermore, even at 2000 mg/mL concentrations of HT and p(HT), the inhibition% of α-glucosidase enzyme were measured as 93.2 ± 0.3 and 81.3 ± 6.3%, respectively at a 0.03 unit/mL enzyme concentration, establishing some potential application of p(HT) microgels for neurogenerative diseases. Moreover, p(HT) microgels showed two times higher MBC values than HT molecules, e.g., 5.0 versus 2.5 mg/mL MIC values against Gram-negative E. coli and Gram-positive S. aureus, respectively. [ABSTRACT FROM AUTHOR]

Abstract Mulberry (Morus alba L.) leaf can effectively inhibit the digestion of starchy foods, and α‐glucosidase (AG) is its main target. This study employed an untargeted metabolomics approach combined with molecular docking to identify AG inhibitors. Subsequently, inhibition kinetics, fluorescence spectroscopy, and interaction force analysis were utilized to investigate the inhibitory mechanism. Results indicated that vitexin exhibited significant reversible inhibition of AG through competitive inhibition, with an IC50 value of 105.50 ± 1.30 μg/mL. Molecular docking revealed hydrogen bonding as the main interaction force between vitexin and AG, and quenching mechanism analysis showed that they underwent static quenching driven by entropy. The results of the combined experiment showed that 1‐deoxynojirimycin (DNJ), a known bioactive component in mulberry, has a synergistic effect of inhibiting AG activity with vitexin. This study elucidates the potential mechanism of vitexin in inhibiting AG activity and provides theoretical evidence for utilizing vitexin‐DNJ complexes as functional components of AG inhibitors.

Background: According to the International Diabetes Federation, there will be 578 million individuals worldwide with diabetes by 2030 and 700 million by 2045. One of the promising drug targets to fight diabetes is α-glucosidase (AG), and its inhibitors may be used to manage diabetes by reducing the breakdown of complex carbohydrates into simple sugars. The study aims to identify and validate potential AG inhibitors in natural sources to combat diabetes. Methods: Computational techniques such as structure-based virtual screening and molecular dyncamic simulation were employed to predict potential AG inhibitors from compounds of Oroxylum indicum. Finally, in silico results were validated by in vitro analysis using n-butanol fraction of crude methanol extracts. Results: The XP glide scores of top seven hits OI_13, OI_66, OI_16, OI_44, OI_43, OI_20, OI_78 and acarbose were –14.261, –13.475, –13.074, –13.045, –12.978, –12.659, –12.354 and –12.296 kcal/mol, respectively. These hits demonstrated excellent binding affinity towards AG, surpassing the known AG inhibitor acarbose. The MM-GBSA dG binding energies of OI_13, OI_66, and acarbose were −69.093, −62.950, and −53.055 kcal/mol, respectively. Most of the top hits were glycosides, indicating that active compounds lie in the n-butanol fraction of the extract. The IC50 value for AG inhibition by n-butanol fraction was 248.1 μg/ml, and for that of pure acarbose it was 89.16 μg/ml. The predicted oral absorption rate in humans for the top seven hits was low like acarbose, which favors the use of these compounds as anti-diabetes in the small intestine. Conclusion: In summary, the study provides promising insights into the use of natural compounds derived from O. indicum as potential AG inhibitors to manage diabetes. However, further research, including clinical trials and pharmacological studies, would be necessary to validate their efficacy and safety before clinical use.

Natural products are a boundless source for the development of pharmaceutical agents against a wide range of human diseases. Accordingly, naturally occurring aurones possess various biological benefits, such as anticancer, antioxidant, antimicrobial, antidiabetic, anti-inflammatory, antiviral and neuroprotective effects. In addition, various studies have revealed that aurones are potential templates for the regulation of diabetes mellitus and its associated complications. Likewise, certain aurones and their analogues have been found to be remarkable kinase inhibitors of DARK2, PPAR-γ, PTPM1, AGE, α-amylase and α-glucosidase, which represents a promising approach for the treatment of chronic metabolic disorders such as diabetes. Therefore, in our present study, we provide a detailed account of the advances in aurones as antidiabetic agents over the past decade.

A talented endophytic Streptomyces sp. PH9030 is derived from the medicinal plant Kadsura coccinea (Lem.) A.C. Smith. The undescribed naphthoquinone naphthgeranine G (5) and seven previously identified compounds, 6–12, were obtained from Streptomyces sp. PH9030. The structure of 5 was identified by comprehensive examination of its HRESIMS, 1D NMR, 2D NMR and ECD data. The inhibitory activities of all the compounds toward α-glucosidase and their antibacterial properties were investigated. The α-glucosidase inhibitory activities of 5, 6, 7 and 9 were reported for the first time, with IC50 values ranging from 66.4 ± 6.7 to 185.9 ± 0.2 μM, as compared with acarbose (IC50 = 671.5 ± 0.2 μM). The molecular docking and molecular dynamics analysis of 5 with α-glucosidase further indicated that it may have a good binding ability with α-glucosidase. Both 9 and 12 exhibited moderate antibacterial activity against methicillin-resistant Staphylococcus aureus, with minimum inhibitory concentration (MIC) values of 16 μg/mL. These results indicate that 5, together with the naphthoquinone scaffold, has the potential to be further developed as a possible inhibitor of α-glucosidase.

Antimicrobial compounds were purified from culture filtrates from 2 edible Pleurotus species. Using a bioassay-guided fractionation of the culture filtrate extracts, 3 compounds (1-3) were obtained from Pleurotus ostreatus, and another compound (4) was obtained from Pleurotus pulmonarius . Spectroscopic analysis revealed that 1-3 was identified as 5,7-dimethoxyphthalide, 4,6-dimethoxyphthalide, and cheimonophyllon E, respectively, while 4 were identified as pleuroton A. The minimum inhibitory concentration and minimum bactericidal concentration of these compounds were determined against 6 pathogenic bacterial species, Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter cloacae. Compounds 2 and 4 were inhibitory against all tested bacteria, while 1 and 4 were inhibitory against 3 and 2 species, respectively. In addition, 1-4 inhibited tyrosinase, with IC50 values of 0.10-0.30 mg/mL, and α-glucosidase, with IC50 values of 0.12-0.54 mg/mL. However, their antioxidant capacities were marginal. [ABSTRACT FROM AUTHOR]

Peyer’s patches (PPs) are specialized gut-associated lymphoid tissues that initiate follicular helper T (Tfh)-mediated immunoglobulin A (IgA) response to luminal antigens derived from commensal symbionts, pathobionts, and dietary sources. IgA-producing B cells migrate from PPs to the small intestinal lamina propria and secrete IgA across the epithelium, modulating the ecological balance of the commensal microbiota and neutralizing pathogenic microorganisms. α-glucosidase inhibitors (α-GIs) are antidiabetic drugs that inhibit carbohydrate digestion in the small intestinal epithelium, leading to alterations in the commensal microbiota composition and metabolic activity. The commensal microbiota and IgA responses exhibit bidirectional interactions that modulate intestinal homeostasis and immunity. However, the effect of α-GIs on the intestinal IgA response remains unclear. We investigated whether α-GIs affect IgA responses by administering voglibose and acarbose to mice via drinking water. We analyzed Tfh cells, germinal center (GC) B cells, and IgA-producing B cells in PPs by flow cytometry. We also assessed pathogen-specific IgA responses. We discovered that voglibose and acarbose induced Tfh cells, GCB cells, and IgA-producing B cells in the PPs of the proximal small intestine in mice. This effect was attributed to the modification of the microbiota rather than a shortage of monosaccharides. Furthermore, voglibose enhanced secretory IgA (S-IgA) production against attenuated Salmonella Typhimurium. Our findings reveal a novel mechanism by which α-GIs augment antigen-specific IgA responses by stimulating Tfh-GCB responses in PPs, and suggest a potential therapeutic application as an adjuvant for augmenting mucosal vaccines. [ABSTRACT FROM AUTHOR]

Boehmeria formosana, with its related species, demonstrates anti-glycemic effect, inhibition of HBV production, anticancer activities, etc. Some indolizidine alkaloids from the same genus are bioactive but sensitive to light. To overcome this problem and obtain more phenanthroindolizidine alkaloids, isolation was performed in darkness, yielding 10 new indolizidine alkaloids and 17 known compounds. Among them, seven enhanced glucagon-like receptor 1 (GLP-1) activity at 50 mM, especially 14 and 6 (3.5- and 2.3-fold than the negative control). This procedure yielded bioactive indolizidine alkaloids with novel structures. [ABSTRACT FROM AUTHOR]

Four secondary metabolites, including daidzein (1), genistein (2), glycitein (3), and daidzin (4) have been isolated and structural elucidated from the methanolic extract of the stems and leaves of Erythrina variegata L. collected in Hanoi city, Vietnam. These compounds showed good in vitro inhibition on α-glucosidase enzyme with IC50 values of 97.6 ± 0.6, 230.4 ± 0.4, 34.3 ± 0.9, and 217.2 ± 0.2 µM, respectively as compared with that of acarbose (IC50 value of 125.8 ± 1.2 µM). This finding suggests the possible application of product containing high content of these compounds from the leaves and stems of E. variegata L. for research and development of anti-obese agent.

Two α-pyrone analogs were isolated from the endophytic fungus Diaporthe sp. CB10100, which is derived from the medicinal plant Sinomenium acutum. These analogs included a new compound, diaporpyrone F (3), and a known compound, diaporpyrone D (4). The structure of 3 was identified by a comprehensive examination of HRESIMS, 1D and 2D NMR spectroscopic data. Bioinformatics analysis revealed that biosynthetic gene clusters for α-pyrone analogs are common in fungi of Diaporthe species. The in vitro α-glucosidase inhibitory activity and antibacterial assay of 4 revealed that it has a 46.40% inhibitory effect on α-glucosidase at 800 μM, while no antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), Mycolicibacterium (Mycobacterium) smegmatis or Klebsiella pneumoniae at 64 μg/mL. Molecular docking and molecular dynamics simulations of 4 with α-glucosidase further suggested that the compounds are potential α-glucosidase inhibitors. Therefore, α-pyrone analogs can be used as lead compounds for α-glucosidase inhibitors in more in-depth studies.

Background: Pneumatosis cystoides intestinalis is a rare intestinal disease characterized by single or multiple air cysts in the submucosa or subserosa of the intestinal wall. It is often accompanied by other gastrointestinal diseases. The clinical manifestations were nonspecific, and the diagnosis mainly depended on colonoscopy, imaging, and other auxiliary examinations. Case presentation: The reason for pneumatosis cystoides intestinalis's occurrence remains unclear. Enteral nutrition deficiency, especially the use of glucosidase inhibitors, may be involved in the pathogenesis of pneumatosis cystoides intestinalis in this patient. Here, we report a rare case of pneumatosis cystoides intestinalis in an elderly man who had been taking acarbose for diabetes for a long time. Colonoscopy of the patient was normal before taking acarbose. Conclusion: In patients with diabetes who are treated with glucosidase inhibitors for gastrointestinal symptoms, the possibility of pneumatosis cystoides intestinalis should be considered, and a thorough gastrointestinal examination should be performed in such patients. [ABSTRACT FROM AUTHOR]

Based on the easy cultivation of microorganisms and their short cycle time, research on α-glucosidase inhibitors (α-GIs) of microbial origin is receiving extensive attention. Raw materials used in food production, such as cereals, dairy products, fruits, and vegetables, contain various bioactive components, like flavonoids, polyphenols, and alkaloids. Fermentation with specific bacterial strains enhances the nutritional value of these raw materials and enables the creation of hypoglycemic products rich in diverse active ingredients. Additionally, conventional food processing often results in significant byproduct generation, causing resource wastage and environmental issues. However, using bacterial strains to ferment these byproducts into α-GIs presents an innovative solution. This review describes the microbial-derived α-GIs that have been identified. Moreover, the production of α-GIs using industrial food raw materials and processing byproducts as a medium in fermentation is summarized. It is worth analyzing the selection of strains and raw materials, the separation and identification of key compounds, and fermentation broth research methods. Notably, the innovative ideas in this field are described as well. This review will provide theoretical guidance for the development of microbial-derived hypoglycemic foods. [ABSTRACT FROM AUTHOR]

Seaweeds have gained interest from the pharmaceutical industry due to their diverse secondary metabolites with potential applications in the prevention and treatment of lifestyle diseases. In spite of the abundance of seaweeds in the coastal area of Iligan Bay in the Philippines, there has been limited investigation into their pharmacological properties. Therefore, this study aimed to evaluate the in vitro α-glucosidase inhibition, angiotensin-converting enzyme (ACE) inhibition, and acetylcholinesterase (AChE) inhibition properties of various fractions obtained from the marine red alga Galaxaura oblongata. The methanol extract of G. oblongata was sequentially partitioned into hexane, dichloromethane, ethyl acetate, butanol, and methanol fractions. All assays were performed in vitro and microplate based. The results of α-glucosidase inhibition activity assay showed that the n-hexane fraction and dichloromethane fraction exhibited greater than 50% inhibitory activity at 200 ppm. Furthermore, ACE inhibition activity assay revealed that dichloromethane fraction, ethyl acetate fraction, and butanol fraction displayed ACE inhibition activity above 50% at 250 ppm. In addition, the hexane fraction, dichloromethane fraction, and ethyl acetate fraction demonstrated potent AChE inhibitory activity at 250 ppm. Overall, the findings show that G. oblongata has antidiabetic, anti-hypertensive, and neuroprotective potentials. This is the first report of the in vitro α-Glucosidase, ACE, and AChE inhibition activities of G. oblongata. Further investigation and purification of the highly potent fractions in each assay is highly suggested to identify and characterize the compounds responsible for the observed bioactivities, which could serve as possible leads for drug discovery efforts in the management of various lifestyle diseases [ABSTRACT FROM AUTHOR]

Background and Objective: Control of hyperglycemia after meals is an important strategy in the management of type II diabetes, and the reduction of chronic complications associated with it. Therefore, inhibitors of carbohydrate-degrading enzymes such as α-glucosidase can be useful in the treatment of this disease. The aim of this study was to evaluate the α-glucosidase inhibitory activity in some traditional medicines in Sulaymaniyah province of Iraq. Methods: Eight plant species were prepared with advisory from authentic spiceries in Sulaymaniyah. After air drying and preparation of their methanolic extracts, enzyme microplate assay was conducted on them in four different extract concentrations (1, 0.1, 0.01 and 0.001 mg/ml) along with negative and positive controls. Finally, enzyme kinetic analysis was performed on effective extracts. Findings: Among the eleven studied plant species, Rubus idaeus L., Rheum ribes R. and Salix alba L. extracts at 1 mg/mL concentration showed highest inhibitory activity (98.13±1.05% (IC50=0.046 mg/mL), 93.39±2.11% (IC50=0.085 mg/mL) and 84.46±1.12% (IC50=0.125 mg/mL), respectively) against α-glucosidase,. After kinetic analysis of α-glucosidase inhibition, Rubus idaeus L., Rheum ribes R. extracts showed mixed type of inhibition (competitive- uncompetitive) while extract of Salix alba showed uncompetitive type of inhibition. Conclusion: The leave extract from both Rubus idaeus, Salix alba and root extract of Rheum ribes are remarkable α-glucosidase inhibitors, and may be used in the treatment of type II diabetics after clinical tests.

Aromatic ginger (Kaempferia galanga L.) is one of the natural sources containing ethyl-p-methoxycinnamate, which is known to have beneficial activity, especially as an α-glucosidase inhibitor. This study aims to convert ethyl-p-methoxycinnamate into amide form as N-phenethyl-p-methoxycinnamamide (4a) and N-morpholinyl-p-methoxycinnamamide (4b) through some synthetic ways then tested their activity as an α-glucosidase inhibitor. The FTIR spectra of 4a present a short single peak at 3269.34 cm−1 that belongs to the N-H group, while spectra of 4b show no absorption band between 3200–3400 cm−1 due to its tertiary amide structure. Spectroscopy analysis through 1H- and 13C-NMR exhibits the successful synthesis of both compounds. Bioactivity test results show that compound 4b has better activity than 4a. In molecular dynamics simulation, the binding energy of compounds 4a and 4b reveal that both compounds have a similar binding energy of about -98980.8 and -97696.7 kJ mol−1, respectively.

Filamentous bacteria have been known as actinobacteria which could produce various secondary metabolites, including an α-glucosidase inhibitor. The α-glucosidase inhibitor has been identified to be potentially valuable for the treatment of diabetes mellitus. Endophytic actinobacteria are able to produce bioactive compounds that are similar to their hosts. Indonesian Ficus deltoidea is one of the medicinal plants which has the activity of the α-glucosidase inhibitor. The α-glucosidase inhibitor has been characterized by optimizing compound production, fractionation, analysis using TLC and LC-MS, and identifying inhibitor mechanisms. The α-glucosidase inhibitor substance is present in Streptomyces sp. IPBCC.a.29.1556 aqueous extract. The aqueous extract was separated and fraction 1 had an IC50 value of 58.8 μg/mL, which is better than acarbose (IC50 = 90.4 μg/mL). Kinetic studies revealed that this fraction inhibited the enzyme through a non-competitive mechanism. Chemical profile based on LC-MS, fraction 1 showed the presence of Phenylpropynal, Butyric acid, 2-(2-Ethoxyethoxy)ethanolate, 1,1-Diethoxyethane acetate, N,N-dimethyl-3-oxide-1H-Benzotriazole-1-propanamine, p-coumaric acid, and isoquinolinium which might contribute individually or synergistically to the observed α-glucosidase inhibitor activity. These results suggest that fraction 1 from the aqueous extract of Streptomyces sp. IPBCC.a.29.1556 is the potential source to produce an α-glucosidase inhibitor for the management of postprandial hyperglycemia.

The discovery of bioactive compounds from medicinal plants has played a crucial role in drug discovery. In this study, a simple and efficient method utilizing affinity-based ultrafiltration (UF) coupled with high-performance liquid chromatography (HPLC) was developed for the rapid screening and targeted separation of α-glucosidase inhibitors from Siraitia grosvenorii roots. First, an active fraction of S. grosvenorii roots (SGR2) was prepared, and 17 potential α-glucosidase inhibitors were identified based on UF-HPLC analysis. Second, guided by UF-HPLC, a combination of MCI gel CHP-20P column chromatography, high-speed counter-current countercurrent chromatography, and preparative HPLC were conducted to isolate the compounds producing active peaks. Sixteen compounds were successfully isolated from SGR2, including two lignans and fourteen cucurbitane-type triterpenoids. The structures of the novel compounds (4, 6, 7, 8, 9, and 11) were elucidated using spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance spectroscopy and high-resolution electrospray ionization mass spectrometry. Finally, the α-glucosidase inhibitory activities of the isolated compounds were verified via enzyme inhibition assays and molecular docking analysis, all of which were found to exhibit certain inhibitory activity. Compound 14 exhibited the strongest inhibitory activity, with an IC50 value of 430.13 ± 13.33 μM, which was superior to that of acarbose (1332.50 ± 58.53 μM). The relationships between the structures of the compounds and their inhibitory activities were also investigated. Molecular docking showed that the highly active inhibitors interacted with α-glucosidase through hydrogen bonds and hydrophobic interactions. Our results demonstrate the beneficial effects of S. grosvenorii roots and their constituents on α-glucosidase inhibition. [ABSTRACT FROM AUTHOR]

In the pursuit of identifying the novel resin glycoside modulators glucose-6-phosphatase and α-glucosidase enzymes, associated with blood sugar regulation, methanol-soluble extracts from the flowers of Ipomoea murucoides (cazahuate, Nahuatl), renowned for its abundance of glycolipids, were employed. The methanol-soluble extracts were fractionated by applying the affinity-directed method with glucose-6-phosphatase enzymes from a rat’s liver and α-glucosidase enzymes from its intestines. Mass spectrometry and nuclear magnetic resonance were employed to identify the high-affinity compound as a free ligand following the release from the enzymatic complex. Gel permeation through a spin size-exclusion column allowed the separated high-affinity molecules to bind to glucose-6-phosphatase and α-glucosidase enzymes in solution, which led to the identification of some previously reported resin glycosides in the flowers of cazahuate, where a glycolipid mainly structurally related to murucoidin XIV was observed. In vitro studies demonstrated the modulating properties of resin glycosides on the glucose-6-phosphatase enzyme. Dynamic light scattering revealed conformational variations induced by resin glycosides on α-glucosidase enzyme, causing them to become more compact, akin to observations with the positive control, acarbose. These findings suggest that resin glycosides may serve as a potential source for phytotherapeutic agents with antihyperglycemic properties.

Hematoxylin (HT) as a natural phenolic dye compound is generally used together with eosin (E) dye as H&E in the histological staining of tissues. Here, we report for the first time the polymeric particle preparation from HT as poly(Hematoxylin) ((p(HT)) microgels via microemulsion method in a one-step using a benign crosslinker, glycerol diglycidyl ether (GDE). P(HT) microgels are about 10 µm and spherical in shape with a zeta potential value of −34.6 ± 2.8 mV and an isoelectric point (IEP) of pH 1.79. Interestingly, fluorescence properties of HT molecules were retained upon microgel formation, e.g., the fluorescence emission intensity of p(HT) at 343 nm was about 2.8 times less than that of the HT molecule at λex: 300 nm. P(HT) microgels are hydrolytically degradable and can be controlled by using an amount of crosslinker, GDE, e.g., about 40%, 20%, and 10% of p(HT) microgels was degraded in 15 days in aqueous environments for the microgels prepared at 100, 200, and 300% mole ratios of GDE to HT, respectively. Interestingly, HT molecules at 1000 mg/mL showed 22.7 + 0.4% cell viability whereas the p(HT) microgels exhibited a cell viability of 94.3 + 7.2% against fibroblast cells. Furthermore, even at 2000 mg/mL concentrations of HT and p(HT), the inhibition% of α-glucosidase enzyme were measured as 93.2 ± 0.3 and 81.3 ± 6.3%, respectively at a 0.03 unit/mL enzyme concentration, establishing some potential application of p(HT) microgels for neurogenerative diseases. Moreover, p(HT) microgels showed two times higher MBC values than HT molecules, e.g., 5.0 versus 2.5 mg/mL MIC values against Gram-negative E. coli and Gram-positive S. aureus, respectively.

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Increasing age is the single largest risk factor for a variety of chronic illnesses. As a result, improving the capability to target the aging process leads to an increased health span. A lack of appropriate glucoregulatory control is a recurring issue associated with aging and chronic illness, even though many longevity therapies result in the preservation of glucoregulatory control. In this study, we suggest that targeting glucose metabolism to improve regulatory control can help slow the aging process. Male Wistar rats, both young (age 4 months) and old (age 24 months), were given acarbose (ACA) (30 mg/kg b.w.) for 6 weeks. An array of oxidative stress indicators was assessed after the treatment period, including plasma antioxidant capacity as determined by the ferric reducing ability of plasma (FRAP), reactive oxygen species (ROS), lipid peroxidation (malondialdehyde [MDA]), reduced glutathione (GSH), total plasma thiol (sulfhydryl [SH]), plasma membrane redox system (PMRS), protein carbonyl (PCO), advanced oxidation protein products (AOPPs), advanced glycation end products (AGEs), and sialic acid (SA) in control and treated groups. When compared with controls, ACA administration increased FRAP, GSH, SH, and PMRS activities in both age groups. The treated groups, on the contrary, showed substantial decreases in ROS, MDA, PCO, AOPP, AGE, and SA levels. The effect of ACA on almost all parameters was more evident in old-age rats. ACA significantly increased PMRS activity in young rats; here the effect was less prominent in old rats. Our data support the restoration of antioxidant levels in older rats after short-term ACA treatment. The findings corroborate the potential role of ACA as a putative calorie restriction mimetic. [ABSTRACT FROM AUTHOR]

The biological activities of extracts and isolated compounds of Macaranga mappa stem bark for antidiabetic herbal medicine, antioxidant, and cytotoxicity activities have been determined. The antidiabetic, antioxidant, and cytotoxicity activities of the sample were carried out by inhibition value of a-glucosidase, DPPH method, and brine shrimp larvae method, respectively. The initial methanol extract and its fractions have good activities against antidiabetics and antioxidants, except for the hexane fraction. The fractions with the highest activity for the antidiabetic and antioxidant tests were the water fraction IC50 6.654 ppm and the butanol fraction IC50 32.34 ppm, respectively. The toxicity test results with the BSLT method showed that all fractions were non-toxic LC50>1000 ppm. The isolated compound from the ethyl acetate fraction was a coumarin derivative, namely scopoletin, with antidiabetic and antioxidant activities. [ABSTRACT FROM AUTHOR]

A rapid, easy and simple method for the isolation and purification of α-glucosidase inhibitors of the ethyl acetate extract of Thymelaea hirsuta (EaTh) by a combination of thin layer chromatography (TLC) and enzymatic test has been developed. EaTh was demonstrated previously a potent α-glucosidase inhibitory effect. In this study, we developed a simple TLC-enzymatic test (TLC/EZ) combination to isolate α-glucosidase inhibitors present in EaTh.EaTh was extracted by Soxhlet from Thymelaea hirsuta (T. hirsuta). The EaTh was separated on a silica gel column and then on a TLC plate. After TLC separation, the TLC/EZ combination method was applied. α-glucosidase inhibitors were detected directly in the TLC plate using the glucose oxidase peroxidase method (GOD-POD). A good detection of active compounds was obtained in the TLC favoring the TLC/EZ method. Active compounds were then characterized using high performance liquid chromatography-mass spectrometry (HPLC–MS) analysis. The main α-glucosidase inhibitors present in EaTh have a molecular ion [M + H]+ at m/z = 543. This proposed method is suitable for a reliable isolation and purification of α-glucosidase inhibitors present in EaTh. It could be proposed as an interesting alternative of the classical method for the isolation and purification of α-glucosidase inhibitors in plant extracts. [ABSTRACT FROM AUTHOR]

A library of 4-Hydroxy Pd–C-Ⅲ derivatives (5a - 5p and 8a - 8h) as α-glucosidase inhibitors was prepared and the activity of these compounds against α-glucosidase was evaluated. The outcomes displayed that most of the derivatives had moderate to potent α-glucosidase inhibition with IC 50 values ranging from 66.3 ± 2.4 to 299.7 ± 6.0 μM. Amongst these compounds, 8a had the strongest α-glucosidase inhibition than others with an IC 50 value of 66.3 ± 2.4 μM. Therefore, 8a was chosen to detect the inhibitory activities on PTP1B and α-amylase, the results revealed that 8a had the potential to be PTP1B (IC 50 = 47.0 ± 0.5 μM) and α-amylase (IC 50 = 30.62 ± 2.13 μM) inhibitor. Additionally, the enzyme kinetic study displayed that 8a was a mixed-type inhibitor. Moreover, the results of the spectroscopy experiments proved that 8a could quench the fluorescence intensity of α-glucosidase in a dose-dependent manner, destroy the secondary structure of α-glucosidase and change the conformation of the enzyme. Significantly, the investigation of cellular thermal shift assay exhibited that 8a could target the PTP1B protein, and the in vitro cytotoxicity discovered compound 8a had no significant toxicity to normal HEK-293 cells. Additionally, the results of molecular docking found that 8a could both bind the active sites of the α-glucosidase and PTP1B. Importantly, the in vivo sucrose-loading test displayed 8a had potential to reduce the postprandial blood glucose. All results proved that compound 8a had great potential as a dual-target inhibitor in treating Type 2 diabetes mellitus. [Display omitted] • A series of novel 4-hydroxy Pd–C-Ⅲ 5a - 5p and 8a - 8h had been synthesized. • Most derivatives had potential ability to inhibit α-glucosidase. • Compound 8a exhibited excellent activities against α-glucosidase and PTP1B. • Compound 8a could dock into the active pockets of α-glucosidase and PTP1B. • Compound 8a had excellent in vitro and in vivo activities. [ABSTRACT FROM AUTHOR]

Withania coagulans (WC) is used in traditional and Ayurveda medicine to treat various ailments, including diabetes. Our investigation found that WC fruit hexane extract effectively suppresses α-glucosidase activity (IC 50 = 0.013 mg/ml, K i = 0.012 mg/ml). The purified molecule has an IC 50 of 0.004 mg/ml and K i of 0.0037 mg/ml. FTIR examination indicates distinctive peaks at 3500, 2900, 1770, and 1500 cm−1 corresponding to functional groups OH bending, C H stretching, C O stretching, and C O stretching. GCMS analysis reveals plant secondary metabolites (PSM) such as n-hexadecenoic acid and methyl 9,10-octadecadienoate. NMR confirms the existence of olefinic fatty acids. The bioactive fraction recorded a non-competitive mode of inhibition of α-glucosidase activity. The cytotoxicity exhibited against HELA cell was IC 50 0.4 mg/ml and found positive in inhibiting the growth of Bacillus cereus, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, and Pseudomonas aeruginosa. Additionally, ensemble docking and molecular dynamic simulation showed that, out of the four PSMs examined, methyl 12,13-tetradecadienoate interacted with the α-glucosidase enzyme's allosteric site (BE −128.78 kJ/mol) and changed the configurations of the catalytic sites, as demonstrated by the enzyme's decreased affinity for isomaltose. The study found that PSMs from WC fruit may inhibit α-glucosidase, making them viable candidates for antidiabetic medication development. • Purification of alpha-glucosidase inhibitory phytomolecules from Withania coagulans showed a significant reduction in IC 50 values i.e., 0.13 mg/ml to 0.004 mg/ml. • The FTIR spectra showed the presence of compounds like hexadecanoic acid and 9,12-octadecadienoic acid. • The active compound was identified as olefinic fatty acid with many additional properties. [ABSTRACT FROM AUTHOR]

Nowadays, the food industry attaches more importance to studies on using purple components in food formulations due to their bioactive properties. This study evaluated the phenolic compound content, antioxidant activity, physicochemical properties, sensory properties, and α-glucosidase activities in yogurt enriched with purple wheat flour. Yogurts were produced using varying concentrations of purple wheat flour labeled as sample A (1.5 %), sample B (3 %), and sample C (4.5 %). It was observed that incorporating purple wheat flour led to a decrease in pH and an increase in L *, a *, and b * values, as well as the acidity and viscosity of the yogurts. Sample C contained the highest phenolic content (37.6 mg GAE/100 g dry matter) on day 14, along with the highest flavonoid content (14.59 mg CE/100 g) on day 21 when than control yogurt. In addition, sample C had the highest α-glucosidase activity (38.35 %) on day 14 and anthocyanin content (13.55 g/100 g) on day 21. As a result, C yogurt can be consumed as a diabetic product with antidiabetic and antihypertensive properties by reaching optimal α-glycosidase inhibition activity. Furthermore, yogurts containing purple wheat flour received higher sensory scores from panelists. [ABSTRACT FROM AUTHOR]

As a medicinal and edible plant, Mulberry has shown good hypoglycaemic activity at the animal level, but its active ingredients and hypoglycaemic mechanisms remain unclear. In this study, we used ultrafiltration-ultra performance liquid chromatography-quadrupole time-of-flight-mass spectrometry (UF-UPLC-QTOF-MS/MS) and molecular docking to screen for high-affinity α-glucosidase inhibitors in Mulberry. Our innovation was to determine the inhibitory activity of Mulberry extracts in vitro and screen the active small molecules in the extracts using advanced UF-UPLC-QTOF-MS/MS techniques and validate these compounds at the molecular docking and cellular levels, laying the foundation for studying the mechanism of type 2 diabetes in Mulberry. α-Glucosidase incubation experiments showed that the IC50 value of Mulberry crude extracts was 37.58 μg/mL. Six possible α-glucosidase activity inhibitory components were identified using UF-UPLC-QTOF-MS/MS. Molecular docking studies showed that these small molecules were more likely to occupy the active site of α-glucosidase than the positive control acarbose, scoring above the threshold, indicating that Mulberry is a potential source of hypoglycemic agents. Further cellular level studies showed that different extracts and active small molecules of Mulberry improved insulin resistance in HepG2 cells. Through the analysis of glucose-lowering targeting components, the subject clarified that Mulberry exerts therapeutic effects on Diabetes Mellitus (DM) through a multi-component, multi-target, and multi-pathway relationship, which is consistent with Traditional Chinese Medicine (TCM) theory as a potential source of glucose-lowering agents.

[Display omitted] 3-Arylidene-1-(2,6-dichlorophenyl)indolones and in particular their 5-methylaminosulfonyl derivatives efficiently inhibit α-glucosidase enzyme. The results are corroborated by in silico docking studies which show the binding of aminosulfonyl derivatives to be more favorable due to additional hydrogen bonding. The most active compound of the series shows the IC 50 of 6.19 μm. [ABSTRACT FROM AUTHOR]

α-Glucosidase and α-amylase are the two main glycosidases that participate in the metabolism of carbohydrates. Inhibitors of these two enzymes are considered an important medical treatment for carbohydrate uptake disorders, such as diabetes and obesity. Microbes are an important source of constituents that have the potential to inhibit glycosidases and can be used as sources of new drugs and dietary supplements. For example, the α-glucosidase inhibitor acarbose, isolated from Actinoplanes sp., has played an important role in adequately controlling type 2 diabetes, but this class of marketed drugs has many drawbacks, such as poor compliance with treatment and expense. This demonstrates the need for new microorganism-derived resources, as well as novel classes of drugs with better compliance, socioeconomic benefits, and safety. This review introduces the literature on microbial sources of α-glucosidase and α-amylase inhibitors, with a focus on endophytes and marine microorganisms, over the most recent 5years. This paper also reviews the application of glycosidase inhibitors as drugs and dietary supplements. These studies will contribute to the future development of new microorganism-derived glycosidase inhibitors. [ABSTRACT FROM AUTHOR]