Displaying publications 101 - 120 of 132 in total

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  1. Fulltext UHPLC-ESI-Orbitrap-MS Analysis of Biologically Active Extracts from Gynura procumbens (Lour.) Merr. and Cleome gynandra L. Leaves
    Chandradevan M, Simoh S, Mediani A, Ismail NH, Ismail IS, Abas F
    Evid Based Complement Alternat Med, 2020;2020:3238561.
    PMID: 32047522 DOI: 10.1155/2020/3238561
    This study aimed to determine the total phenolic content, DPPH scavenging, α-glucosidase, and nitric oxide (NO) inhibition of Gynura procumbens and Cleome gynandra extracts obtained with five different ethanolic concentrations. The findings showed that the 100% ethanolic extract of G. procumbens had the highest phenolic content and the lowest IC50 values for DPPH scavenging and NO inhibition activity compared to the properties of the other extracts. For C. gynandra, the 20% and 100% ethanolic extracts had comparably high total phenolic contents, and the latter possessed the lowest IC50 value in the NO inhibition assay. In addition, the 20% ethanolic extract of C. gynandra had the lowest IC50 value in the DPPH scavenging assay. However, none of the extracts from either herb had the ability to inhibit α-glucosidase enzyme. Pearson correlation analysis indicated a strong relationship between the phenolic content and DPPH scavenging activity in both herb extracts. A moderately strong relationship was also observed between the phenolic content and NO inhibition in G. procumbens extracts and not in C. gynandra extracts. The UHPLC-ESI-Orbitrap-MS revealed major phenolics from the groups of hydroxycinnamic acids, hydroxybenzoic acids, and flavonoid derivatives from both herbs, which could be the key contributors to their bioactivities. Among the identified metabolites, 24 metabolites were tentatively assigned for the first time from both species of studied herbs. These two herbs could be recommended as prospective natural products with valuable medicinal properties.
    Matched MeSH terms: alpha-Glucosidases
  2. Fulltext Genotype, phenotype and treatment outcomes of 17 Malaysian patients with infantile-onset Pompe disease and the identification of 3 novel GAA variants
    Chan MY, Jalil JA, Yakob Y, Wahab SAA, Ali EZ, Khalid MKNM, et al.
    Orphanet J Rare Dis, 2023 Aug 04;18(1):231.
    PMID: 37542277 DOI: 10.1186/s13023-023-02848-6
    BACKGROUND: Pompe disease is a rare glycogen storage disorder caused by deficiency of the lysosomal enzyme acid alpha-glucosidase (GAA), leading to glycogen deposition in multiple tissues. Infantile-onset Pompe disease (IOPD) patients present within the first year of life with profound hypotonia and hypertrophic cardiomyopathy. Treatment with enzyme replacement therapy (ERT) has significantly improved survival for this otherwise lethal disorder. This study aims to describe the clinical and molecular spectrum of Malaysian IOPD patients, and to analyze their long term treatment outcomes.

    METHODS: Seventeen patients diagnosed with IOPD between 2000 and 2020 were included in this retrospective cohort study. Clinical and biochemical data were collated and analyzed using descriptive statistics. GAA enzyme levels were performed on dried blood spots. Molecular analysis of the GAA gene was performed by polymerase chain reaction and Sanger sequencing. Structural modelling was used to predict the effect of the novel mutations on enzyme structure.

    RESULTS: Our cohort had a median age of presentation of 3 months and median age of diagnosis of 6 months. Presenting features were hypertrophic cardiomyopathy (100%), respiratory insufficiency (94%), hypotonia (88%), failure to thrive (82%), feeding difficulties (76%), and hepatomegaly (76%). Fourteen different mutations in the GAA gene were identified, with three novel mutations, c.1552-14_1552-1del, exons 2-3 deletion and exons 6-10 deletion. The most common mutation identified was c.1935C > A p.(D645E), with an allele frequency of 33%. Sixteen patients received ERT at the median age of 7 months. Overall survival was 29%. Mean age of death was 17.5 months. Our longest surviving patient has atypical IOPD and is currently 20 years old.

    CONCLUSIONS: This is the first study to analyze the genotype and phenotype of Malaysian IOPD patients, and has identified the c.1935C > A p.(D645E) as the most common mutation. The three novel mutations reported in this study expands the mutation spectrum for IOPD. Our low survival rate underscores the importance of early diagnosis and treatment in achieving better treatment outcomes.

    Matched MeSH terms: alpha-Glucosidases/genetics
  3. Enzymatic characterisation of clinical isolates of Cryptococcus neoformans, Cryptococcus gattii and other environmental Cryptococcus spp
    Chan MY, Tay ST
    Mycoses, 2010 Jan;53(1):26-31.
    PMID: 19389064 DOI: 10.1111/j.1439-0507.2008.01654.x
    This study compared the enzymatic activity of clinical isolates of Cryptococcus neoformans, Cryptococcus gattii, environmental isolates of C. neoformans and non-neoformans Cryptococcus. Most of the cryptococcal isolates investigated in this study exhibited proteinase and phospholipase activities. Laccase activity was detected from all the C. neoformans and C. gattii isolates, but not from the non-neoformans Cryptococcus isolates. There was no significant difference in the proteinase, phospholipase and laccase activities of C. neoformans and C. gattii. However, significant difference in the enzymatic activities of beta-glucuronidase, alpha-glucosidase, beta-glucosidase and N-acetyl-beta-glucosaminidase between C. neoformans and C. gattii isolates was observed in this study. Environmental isolates of C. neoformans exhibited similar enzymatic profiles as the clinical isolates of C. neoformans, except for lower proteinase and laccase activities.
    Matched MeSH terms: alpha-Glucosidases/analysis
  4. Identification of curcumin as a potential α-glucosidase and dipeptidyl-peptidase 4 inhibitor: Molecular docking study, in vitro and in vivo biological evaluation
    Cao W, Chen X, Chin Y, Zheng J, Lim PE, Xue C, et al.
    J Food Biochem, 2021 Apr 04.
    PMID: 33817806 DOI: 10.1111/jfbc.13686
    Natural compounds have tremendous potential to regulate glucose metabolism, but conventional methods for studying their bioactivities are usually labor intensive. Here, hypoglycemic properties in 22 selected food-derived compounds were examined using molecular docking. The results indicated that curcumin is an inhibitor of both α-glucosidase and dipeptidyl-peptidase 4 (DPP-4), which are important for glycemic control. These effects of curcumin were also confirmed by enzymatic determination in vitro. Furthermore, curcumin significantly improved diet-induced hyperglycemia (e.g., fasting plasma glucose levels and glycogen storage in muscle or liver) in mice. This might be attributed to its inhibitory effects on the activities of α-glucosidase and DPP-4 in vivo. Curcumin also upregulated the expression of genes (e.g., glucagon-like peptide 1) related to DPP-4 activity in the small intestine. In conclusion, curcumin is a potential ingredient of functional foods used for diet-induced hyperglycemia management. PRACTICAL APPLICATIONS: Curcumin has been widely used as a colorant in the food industry. Moreover, a growing number of studies have described its diverse biological functions, such as anti-inflammatory, anti-oxidant, and anti-angiogenic activities. Thus, curcumin is regarded as a potential ingredient in functional foods. Our results highlighted the hyperglycemic effect of curcumin, suggesting that curcumin may be included in food products for hyperglycemic patients.
    Matched MeSH terms: alpha-Glucosidases
  5. Fulltext Potential inhibitors of α -glucosidase and α -amylase enzymes from locally available fruit wastes by solid state fermentation
    Barkat, Anumsima Ahmad, Jamal, Parveen, Azlin Suhaida Azmi, Noorbacha, Ibrahim Ali, Zulkarnain Mohamed Idris, Arbain, Dachyar
    Biological and Natural Resources Engineering Journal, 2019;2(1):56-63.
    MyJurnal
    A therapeutic approach for treating diabetes is to decrease thepost-prandial hyperglycaemia. This is done by retarding the absorption of glucose through the inhibition of carbohydrate hydrolyzing enzymes, α-amylaseand α-glucosidase, in the digestive tract. Inhibition of both enzymes helpsto reduce the glucose level in the blood of a diabetic patient. This study was aimed to investigate the production of α-glucosidase and α-amylase inhibitors from local fruit wastes (honeydew skin, banana peel, and pineapple skin) using solid state fermentation. Each of the fruit wastes was fermented with three different types of white rot fungus Phenarochaete chrysosporium(PC), Panus tigrinusM609RQY(M6) andRO209RQY(RO2)for 7 days. Sampling was carried out starting from day 4 to day 7 to determine the enzyme inhibition activity. The samples were extracted using water prior to enzyme analysis. Most of the fruit samples showed varying degree of percentage inhibition activity depending on the sampling time. Extract of fermented banana peels with RO2 on day 4 showed the higherα-glucosidase inhibition (56.57±0.32%), followed byhoneydew extract fermented with the same fungus on the same day (39.68±0.05%). Extracts of each fruit wastesample fermented with PCshowed the least α-glucosidase inhibition (below 15%). Meanwhile for α-amylase inhibition activity, the extract from fermented honeydew skins with PCon day7 showed the highest inhibition activity i.e.98.29±0.63%. The least inhibition activity (43.37±0.54%) was observed in the extract from honeydew skins fermented withM6 on day 5. All positive resultsshowed that fruit wastes could be the alternative sourcesfor antidiabetic agent especially for α-amylase and α-glucosidase inhibitors.
    Matched MeSH terms: alpha-Glucosidases
  6. Synthesis, in vitro biological activities and in silico study of dihydropyrimidines derivatives
    Barakat A, Islam MS, Al-Majid AM, Ghabbour HA, Fun HK, Javed K, et al.
    Bioorg Med Chem, 2015 Oct 15;23(20):6740-8.
    PMID: 26381063 DOI: 10.1016/j.bmc.2015.09.001
    We describe here the synthesis of dihydropyrimidines derivatives 3a-p, and evaluation of their α-glucosidase enzyme inhibition activities. Compounds 3b (IC50=62.4±1.5 μM), 3c (IC50=25.3±1.26 μM), 3d (IC50=12.4±0.15 μM), 3e (IC50=22.9±0.25 μM), 3g (IC50=23.8±0.17 μM), 3h (IC50=163.3±5.1 μM), 3i (IC50=30.6±0.6 μM), 3m (IC50=26.4±0.34 μM), and 3o (IC50=136.1±6.63 μM) were found to be potent α-glucosidase inhibitors in comparison to the standard drug acarbose (IC50=840±1.73 μM). The compounds were also evaluated for their in vitro cytotoxic activity against PC-3, HeLa, and MCF-3 cancer cell lines, and 3T3 mouse fibroblast cell line. All compounds were found to be non cytotoxic, except compounds 3f and 3m (IC50=17.79±0.66-20.44±0.30 μM), which showed a weak cytotoxic activity against the HeLa, and 3T3 cell lines. In molecular docking simulation study, all the compounds were docked into the active site of the predicted homology model of α-glucosidase enzyme. From the docking result, it was observed that most of the synthesized compounds showed interaction through carbonyl oxygen atom and polar phenyl ring with active site residues of the enzyme.
    Matched MeSH terms: alpha-Glucosidases/metabolism*
  7. 'Targeting the feast of a sleeping beast': Nutrient and mineral dependencies of encysted Acanthamoeba castellanii
    Baig AM, Khan NA, Katyara P, Lalani S, Baig R, Nadeem M, et al.
    Chem Biol Drug Des, 2021 01;97(1):18-27.
    PMID: 32602961 DOI: 10.1111/cbdd.13755
    Acanthamoeba spp. cause a corneal infection, Acanthamoeba keratitis (AK), and a cerebral infection, granulomatous amoebic encephalitis (GAE). Though aggressive chemotherapy has been able to kill the active trophozoite form of Acanthamoeba, the encysted form of this parasite has remained problematic to resist physiological concentrations of drugs. The emergence of encysted amoeba into active trophozoite form poses a challenge to eradicate this parasite. Acanthamoeba trophozoites have active metabolic machinery that furnishes energy in the form of ATPs by subjecting carbohydrates and lipids to undergo pathways including glycolysis and beta-oxidation of free fatty acids, respectively. However, very little is known about the metabolic preferences and dependencies of an encysted trophozoite on minerals or potential nutrients that it consumes to live in an encysted state. Here, we investigate the metabolic and nutrient preferences of the encysted trophozoite of Acanthamoeba castellanii and the possibility to target them by drugs that act on calcium ion dependencies of the encysted amoeba. The experimental assays, immunostaining coupled with bioinformatics tools show that the encysted Acanthamoeba uses diverse nutrient pathways to obtain energy in the quiescent encysted state. These findings highlight potential pathways that can be targeted in eradicating amoebae cysts successfully.
    Matched MeSH terms: alpha-Glucosidases/metabolism; alpha-Glucosidases/chemistry
  8. Dihydroquinazolin-4(1H)-one derivatives as novel and potential leads for diabetic management
    Babatunde O, Hameed S, Salar U, Chigurupati S, Wadood A, Rehman AU, et al.
    Mol Divers, 2021 Mar 01.
    PMID: 33650031 DOI: 10.1007/s11030-021-10196-5
    A variety of dihydroquinazolin-4(1H)-one derivatives (1-37) were synthesized via "one-pot" three-component reaction scheme by treating aniline and different aromatic aldehydes with isatoic anhydride in the presence of acetic acid. Chemical structures of compounds were deduced by different spectroscopic techniques including EI-MS, HREI-MS, 1H-, and 13C-NMR. Compounds were subjected to α-amylase and α-glucosidase inhibitory activities. A number of derivatives exhibited significant to moderate inhibition potential against α-amylase (IC50 = 23.33 ± 0.02-88.65 ± 0.23 μM) and α-glucosidase (IC50 = 25.01 ± 0.12-89.99 ± 0.09 μM) enzymes, respectively. Results were compared with the standard acarbose (IC50 = 17.08 ± 0.07 μM for α-amylase and IC50 = 17.67 ± 0.09 μM for α-glucosidase). Structure-activity relationship (SAR) was rationalized by analyzing the substituents effects on inhibitory potential. Kinetic studies were implemented to find the mode of inhibition by compounds which revealed competitive inhibition for α-amylase and non-competitive inhibition for α-glucosidase. However, in silico study identified several important binding interactions of ligands (synthetic analogues) with the active site of both enzymes.
    Matched MeSH terms: alpha-Glucosidases
  9. Identification and characterization of novel α-amylase and α-glucosidase inhibitory peptides from camel whey proteins
    Baba WN, Mudgil P, Kamal H, Kilari BP, Gan CY, Maqsood S
    J Dairy Sci, 2021 Feb;104(2):1364-1377.
    PMID: 33309363 DOI: 10.3168/jds.2020-19271
    This study explores the inhibitory properties of camel whey protein hydrolysates (CWPH) toward α-amylase (AAM) and α-glucosidase (AG). A general full factorial design (3 × 3) was applied to study the effect of temperature (30, 37, and 45°C), time (120, 240, and 360 min), and enzyme (pepsin) concentration (E%; 0.5, 1, and 2%). The results showed that maximum degree of hydrolysis was obtained when hydrolysis was carried out at higher temperature (45°C; P < 0.05), compared with lower temperatures of 30 and 37°C. Electrophoretic pattern displays degradation of all protein bands upon hydrolysis by pepsin at various hydrolysis conditions applied. All the 27 CWPH generated showed significant AAM and AG inhibitory potential as indicated by their lower IC50 values (mg/mL) compared with intact whey proteins. In total 196 peptides were identified from selected hydrolysates and 15 potential peptides (PepSite score > 0.8; http://pepsite2.russelllab.org/) were explored via in silico approach. Novel peptides PAGNFLMNGLMHR, PAVACCLPPLPCHM, MLPLMLPFTMGY, and PAGNFLPPVAAAPVM were identified as potential inhibitors for both AAM and AG due to their high number of binding sites and highest binding probability toward the target enzymes. CCGM and MFE, as well as FCCLGPVPP were identified as AG and AAM inhibitory peptides, respectively. This is the first study that reports novel AG and AAM inhibitory peptides from camel whey proteins. The future direction for this research involves synthesis of these potential AG and AAM inhibitory peptides in a pure form and investigate their antidiabetic properties in the in vitro, as well as in vivo models. Thus, CWPH can be considered for potential applications in glycaemic regulation.
    Matched MeSH terms: alpha-Glucosidases/metabolism
  10. Fulltext Effect of Different Extraction Methods on the Total Phenolics of Sugar Cane Products
    Azlan A, Sultana S, Mahmod II
    Molecules, 2023 May 28;28(11).
    PMID: 37298880 DOI: 10.3390/molecules28114403
    The health benefits of sugar cane products are attributed to certain antioxidant compounds in plant materials. The presence of antioxidants in plant materials depends on the extraction method in terms of yield and the number of phenolic compounds identified. This study was carried out to evaluate the performance of the three extraction methods, which were selected from previous studies to show the effect of the extraction method on the content of antioxidant compounds in different types of sugar. This study also evaluates the potential of different sugar extracts in anti-diabetic activity based on in vitro assays (α-glucosidase and α-amylase). The results showed that sugar cane extracted with acidified ethanol (1.6 M HCl in 60% ethanol) was the best condition to extract a high yield of phenolic acids compared to other methods. Among the three types of sugar, less refined sugar (LRS) showed the highest yield of phenolic compounds, 57.72 µg/g, compared to brown sugar (BS) and refined sugar (RS) sugar, which were at 42.19 µg/g and 22.06 µg/g, respectively. Whereas, among the sugar cane derivatives, LRS showed minor and BS moderate inhibition towards α-amylase and α-glucosidase activity compared to white sugar (RS). Thus, it is suggested that sugar cane extracted with acidified ethanol (1.6 M HCl in 60% ethanol) is the optimum experimental condition for antioxidant content determination and provides a basis for further exploitation of the health-beneficial resources of the sugarcane products.
    Matched MeSH terms: alpha-Glucosidases
  11. Fulltext Potentially Bioactive Metabolites from Pineapple Waste Extracts and Their Antioxidant and α-Glucosidase Inhibitory Activities by 1H NMR
    Azizan A, Xin LA, Abdul Hamid NA, Maulidiani M, Mediani A, Abdul Ghafar SZ, et al.
    Foods, 2020 Feb 11;9(2).
    PMID: 32053982 DOI: 10.3390/foods9020173
    Pineapple (Ananascomosus) waste is a promising source of metabolites for therapeutics, functional foods, and cosmeceutical applications. This study strives to characterize the complete metabolite profiles of a variety of MD2 pineapple waste extracts. Metabolomics strategies were utilized to identify bioactive metabolites of this variety prepared with different solvent ratios. Each pineapple waste extract was first screened for total phenolic content, 2,2-diphenyl-1-picrylhydrazyl free radical scavenging, nitric oxide scavenging, and α-glucosidase inhibitory activities. The highest TPC was found in all samples of the peel, crown, and core extracted using a 50% ethanol ratio, even though the results were fairly significant than those obtained for other ethanol ratios. Additionally, crown extracted with a 100% ethanol ratio demonstrated the highest potency in DPPH and NO scavenging activity, with IC50 values of 296.31 and 338.52 µg/mL, respectively. Peel extracted with 100% ethanol exhibited the highest α-glucosidase inhibitory activity with an IC50 value of 92.95 µg/mL. Then, the extracts were analyzed and the data from 1H NMR were processed using multivariate data analysis. A partial least squares and correlogram plot suggested that 3-methylglutaric acid, threonine, valine, and α-linolenic acid were the main contributors to the antioxidant activities, whereas epicatechin was responsible for the α-glucosidase inhibitory activity. Relative quantification further supported that 100% crown extract was among the extracts that possessed the most abundant potential metabolites. The present study demonstrated that the crown and peel parts of MD2 pineapple extracted with 100% ethanol are potentially natural sources of antioxidants and α-glucosidase inhibitors, respectively.
    Matched MeSH terms: alpha-Glucosidases
  12. 5-Bromo-2-aryl benzimidazole derivatives as non-cytotoxic potential dual inhibitors of α-glucosidase and urease enzymes
    Arshad T, Khan KM, Rasool N, Salar U, Hussain S, Asghar H, et al.
    Bioorg Chem, 2017 06;72:21-31.
    PMID: 28346872 DOI: 10.1016/j.bioorg.2017.03.007
    On the basis of previous report on promising α-glucosidase inhibitory activity of 5-bromo-2-aryl benzimidazole derivatives, these derivatives were further screened for urease inhibitory and cytotoxicity activity in order to get more potent and non-cytotoxic potential dual inhibitor for the patients suffering from diabetes as well as peptic ulcer. In this study, all compounds showed varying degree of potency in the range of (IC50=8.15±0.03-354.67±0.19μM) as compared to standard thiourea (IC50=21.25±0.15μM). It is worth mentioning that derivatives 7 (IC50=12.07±0.05μM), 8 (IC50=10.57±0.12μM), 11 (IC50=13.76±0.02μM), 14 (IC50=15.70±0.12μM) and 22 (IC50=8.15±0.03μM) were found to be more potent inhibitors than standard. All compounds were also evaluated for cytotoxicity towards 3T3 mouse fibroblast cell line and found to be completely non-toxic. Previously benzimidazole 1-25 were also showed α-glucosidase inhibitory potential. In silico studies were performed on the lead molecules i.e.2, 7, 8, 11, 14, and 22, in order to rationalize the binding interaction of compounds with the active site of urease enzyme.
    Matched MeSH terms: alpha-Glucosidases/metabolism*
  13. Antidiabetic activities of chloroform fraction of Anthocleista vogelii Planch root bark in rats with diet- and alloxan-induced obesity-diabetes
    Anyanwu GO, Iqbal J, Khan SU, Zaib S, Rauf K, Onyeneke CE, et al.
    J Ethnopharmacol, 2018 Oct 18.
    PMID: 30342966 DOI: 10.1016/j.jep.2018.10.021
    ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista vogelii Planch is a medicinal plant traditionally used in West Africa for the management and treatment of diabetes mellitus.

    AIM OF THE STUDY: To determine the antidiabetic activities of chloroform fraction (CF) of Anthocleista vogelii Planch root bark in rats with diet- and alloxan-induced obesity-diabetes.

    MATERIALS AND METHODS: Inhibitory activities of CF against α-amylase and α-glucosidase activities were determined in vitro. Three weeks old rats were fed with high-fat diet for 9 weeks to induce obesity prior to further induction of diabetes using alloxan (150mg/kg body weight, i.p.). Blood glucose levels and body weight were measured every 7 days throughout the experiment. Glucose tolerance was assessed in normal and CF-treated rats on day 21. Terminal blood samples were collected from sacrificed animals for the measurement of serum insulin levels. Pancreases were excised from treated and untreated animals for histopathological examination.

    RESULTS: LCMS/MS chromatographic profile of CF via positive and negative modes revealed 13 and 23 compounds respectively. Further analysis revealed quebrachitol (QCT), loganin, sweroside, oleoside 11-methyl ester and ferulic acid, which have been previously reported for their antidiabetic activities, as constituents of CF. CF inhibited activities of α-amylase (IC50 = 51.60 ± 0.92µg/ml) and α-glucosidase (IC50 = 5.86 ± 0.97µg/ml) in a dose-dependent manner. Treatment of animals with obesity-diabetes with 100 and 200mg/kg CF significantly improved glucose tolerance (P<0.001) and enhanced serum insulin levels (P<0.05) compared to diabetic control rats.

    CONCLUSIONS: Antidiabetic activities of CF might be mediated via inhibition of α-amylase and α-glucosidase activities, elevation of serum insulin concentration, and enhancement of insulin and leptin sensitivity in obesity-diabetes rats. This study further substantiates the traditional use of A. vogelii in the management and treatment of diabetes in Africa and encourages further studies to investigate its mechanism of action.

    Matched MeSH terms: alpha-Glucosidases
  14. α-Glucosidase activity of oleanolic acid and its oxidative metabolites: DFT and Docking studies
    Anouar el H, Zakaria NS, Alsalme A, Shah SA
    Mini Rev Med Chem, 2015;15(14):1148-58.
    PMID: 26205959
    A natural pentacyclic triterpenoid oleanolic acid 1 and its biotransformed metabolites 2-3 are potential α-glucosidase inhibitors. To elucidate the inhibitory mechanism of compounds 1, 2 and 3 against α-glucosidase, we calculated (i) their electronic and optical properties using DFT and TD-DFT at the B3LYP/6-31G(d) level in gas and IEF-PCM solvent; and (ii) their binding energies to α-glucosidase via docking study. DFT results showed that the α-glucosidase inhibtion is mainly depend on the polarity parameters of the studied compounds. Docking results revealed that the activity increased with binding energies (i.e. the stability of ligand-receptor complex). The specroscopic data of oleanolic acid 1 and its metabolites 2 and 3 are well predicetd for 13C NMR chemical shifts (R2=99%) and 1H NMR chemical shifts (R2=90%); and for (ii) UV/vis spectra. The assignments and interpretation of NMR chemical shifts and bathochromic shift of λMAX absorption bands are discussed.
    Matched MeSH terms: alpha-Glucosidases/metabolism*; alpha-Glucosidases/chemistry
  15. Martynia annua safety and efficacy: heavy metal profile, in silico and in vitro approaches on antibacterial and antidiabetic activities
    Alrabie A, Al-Rabie NA, Al Saeedy M, Al Adhreai A, Al-Qadsy I, Farooqui M
    Nat Prod Res, 2023 Mar;37(6):1016-1022.
    PMID: 35801965 DOI: 10.1080/14786419.2022.2097227
    Liquid Chromatography-Mass Spectrometry (LC-MS) analysis of methanol extract of Martynia annua seed revealed the presence of haploperozide and austricine. For safety, heavy metals content investigation of plant powder using the Inductively Coupled Plasma-Mass Spectrometry (ICP-MS) technique showed that the toxic metals (Pb: 2.07 mg/kg; Cd: 0.07 mg/kg; and As: 0.18 mg/kg) concentrations were found to be below the permissible limit. The extract demonstrated significant antibacterial activity against E. coli (MIC value 125 g/mL). Furthermore, it was effective in inhibiting both α-glucosidase and α-amylase enzymes with a high percentage and IC50 values were 42.28 ± 0.39 µg/mL and 34.11 ± 0.31 µg/mL, respectively. These findings were supported by a molecular docking study, some of the phytochemicals showed higher docking score values than references. However, Martynia annua seeds are safe to consume because they contain low levels of toxic heavy metals and possess antibacterial and anti-diabetic properties.
    Matched MeSH terms: alpha-Glucosidases
  16. Synthesis of indole-based-thiadiazole derivatives as a potent inhibitor of α-glucosidase enzyme along with in silico study
    Alomari M, Taha M, Rahim F, Selvaraj M, Iqbal N, Chigurupati S, et al.
    Bioorg Chem, 2021 03;108:104638.
    PMID: 33508679 DOI: 10.1016/j.bioorg.2021.104638
    A series of nineteen (1-19) indole-based-thiadiazole derivatives were synthesized, characterized by 1HNMR, 13C NMR, MS, and screened for α-glucosidase inhibition. All analogs showed varied α-glucosidase inhibitory potential with IC50 value ranged between 0.95 ± 0.05 to 13.60 ± 0.30 µM, when compared with the standard acarbose (IC50 = 1.70 ± 0.10). Analogs 17, 2, 1, 9, 7, 3, 15, 10, 16, and 14 with IC50 values 0.95 ± 0.05, 1.10 ± 0.10, 1.30 ± 0.10, 1.60 ± 0.10, 2.30 ± 0.10, 2.30 ± 0.10, 2.80 ± 0.10, 4.10 ± 0.20 and 4.80 ± 0.20 µM respectively showed highest α-glucosidase inhibition. All other analogs also exhibit excellent inhibitory potential. Structure activity relationships have been established for all compounds primarily based on substitution pattern on the phenyl ring. Through molecular docking study, binding interactions of the most active compounds were confirmed. We further studied the kinetics study of analogs 1, 2, 9 and 17 and found that they are Non-competitive inhibitors.
    Matched MeSH terms: alpha-Glucosidases/metabolism*
  17. Hydrazinyl arylthiazole based pyridine scaffolds: Synthesis, structural characterization, in vitro α-glucosidase inhibitory activity, and in silico studies
    Ali F, Khan KM, Salar U, Taha M, Ismail NH, Wadood A, et al.
    Eur J Med Chem, 2017 Sep 29;138:255-272.
    PMID: 28672278 DOI: 10.1016/j.ejmech.2017.06.041
    Acarbose, miglitol, and voglibose are the inhibitors of α-glucosidase enzyme and being clinically used for the management of type-II diabetes mellitus. However, many adverse effects are also associated with them. So, the development of new therapeutic agents is an utmost interest in medicinal chemistry research. Current study is based on the identification of new α-glucosidase inhibitors. For that purpose, hydrazinyl arylthiazole based pyridine derivatives 1-39 were synthesized via two step reaction and fully characterized by spectroscopic techniques EI-MS, HREI-MS, (1)H-, and (13)C NMR. However, stereochemistry of the iminic bond was confirmed by NOESY. All compounds were subjected to in vitro α-glucosidase inhibitory activity and found many folds active (IC50 = 1.40 ± 0.01-236.10 ± 2.20 μM) as compared to the standard acarbose having IC50 value of 856.45 ± 5.60 μM. A limited structure-activity relationship was carried out in order to make a presumption about the substituent's effect on inhibitory activity which predicted that substituents of more negative inductive effect played important role in the activity as compared to the substituents of less negative inductive effect. However, in order to have a good understanding of ligand enzyme interactions, molecular docking study was also conducted. In silico study was confirmed that substituents like halogens (Cl) and nitro (NO2) which have negative inductive effect were found to make important interactions with active site residues.
    Matched MeSH terms: alpha-Glucosidases/metabolism*
  18. Fulltext New quinoxalinone inhibitors targeting secreted phospholipase A2 and α-glucosidase
    Alasmary FAS, Alnahdi FS, Ben Bacha A, El-Araby AM, Moubayed N, Alafeefy AM, et al.
    J Enzyme Inhib Med Chem, 2017 Dec;32(1):1143-1151.
    PMID: 28856929 DOI: 10.1080/14756366.2017.1363743
    Elevated blood glucose and increased activities of secreted phospholipase A2 (sPLA2) are strongly linked to coronary heart disease. In this report, our goal was to develop small heterocyclic compound that inhibit sPLA2. The title compounds were also tested against α-glucosidase and α-amylase. This array of enzymes was selected due to their implication in blood glucose regulation and diabetic cardiovascular complications. Therefore, two distinct series of quinoxalinone derivatives were synthesised; 3-[N'-(substituted-benzylidene)-hydrazino]-1H-quinoxalin-2-ones 3a-f and 1-(substituted-phenyl)-5H-[1,2,4]triazolo[4,3-a]quinoxalin-4-ones 4a-f. Four compounds showed promising enzyme inhibitory effect, compounds 3f and 4b-d potently inhibited the catalytic activities of all of the studied proinflammatory sPLA2. Compound 3e inhibited α-glucosidase (IC50 = 9.99 ± 0.18 µM); which is comparable to quercetin (IC50 = 9.93 ± 0.66 µM), a known inhibitor of this enzyme. Unfortunately, all compounds showed weak activity against α-amylase (IC50 > 200 µM). Structure-based molecular modelling tools were utilised to rationalise the SAR compared to co-crystal structures with sPLA2-GX as well as α-glucosidase. This report introduces novel compounds with dual activities on biochemically unrelated enzymes mutually involved in diabetes and its complications.
    Matched MeSH terms: alpha-Glucosidases/metabolism*
  19. Fulltext In vitro antioxidant and, α-glucosidase inhibitory activities and comprehensive metabolite profiling of methanol extract and its fractions from Clinacanthus nutans
    Alam MA, Zaidul IS, Ghafoor K, Sahena F, Hakim MA, Rafii MY, et al.
    BMC Complement Altern Med, 2017 Mar 31;17(1):181.
    PMID: 28359331 DOI: 10.1186/s12906-017-1684-5
    BACKGROUND: This study was aimed to evaluate antioxidant and α-glucosidase inhibitory activity, with a subsequent analysis of total phenolic and total flavonoid content of methanol extract and its derived fractions from Clinacanthus nutans accompanied by comprehensive phytochemical profiling.

    METHODS: Liquid-liquid partition chromatography was used to separate methanolic extract to get hexane, ethyl acetate, butanol and residual aqueous fractions. The total antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazy (DPPH) radical scavenging and ferric reducing antioxidant power assay (FRAP). The antidiabetic activity of methanol extract and its consequent fractions were examined by α-glucosidase inhibitory bioassay. The chemical profiling was carried out by gas chromatography coupled with quadrupole time-of-flight mass spectrometry (GC Q-TOF MS).

    RESULTS: The total yield for methanol extraction was (12.63 ± 0.98) % (w/w) and highest fractionated value found for residual aqueous (52.25 ± 1.01) % (w/w) as compared to the other fractions. Significant DPPH free radical scavenging activity was found for methanolic extract (63.07 ± 0.11) % and (79.98 ± 0.31) % for ethyl acetate fraction among all the fractions evaluated. Methanol extract was the most prominent in case of FRAP (141.89 ± 0.87 μg AAE/g) whereas most effective reducing power observed in ethyl acetate fraction (133.6 ± 0.2987 μg AAE/g). The results also indicated a substantial α-glucosidase inhibitory activity for butanol fraction (72.16 ± 1.0) % and ethyl acetate fraction (70.76 ± 0.49) %. The statistical analysis revealed that total phenolic and total flavonoid content of the samples had the significant (p 

    Matched MeSH terms: alpha-Glucosidases/metabolism; alpha-Glucosidases/chemistry
  20. Potent Antidiabetic Activity and Metabolite Profiling of Melicope Lunu-ankenda Leaves
    Al-Zuaidy MH, Hamid AA, Ismail A, Mohamed S, Abdul Razis AF, Mumtaz MW, et al.
    J Food Sci, 2016 May;81(5):C1080-90.
    PMID: 27074520 DOI: 10.1111/1750-3841.13293
    Diabetes mellitus is normally characterized by chronic hyperglycemia associated with disturbances in the fat, carbohydrate, and protein metabolism. There is an increasing trend of using natural products instead of synthetic agents as alternative therapy for disorders due to their fewer side effects. In this study, antidiabetic and antioxidant activities of different Melicope lunu-ankenda (ML) ethanolic extracts were evaluated using inhibition of α-glucosidase and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals scavenging activity, respectively; whereas, proton nuclear magnetic resonance ((1) H NMR) and ultra-high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) techniques were used for metabolite profiling of ML leaf extracts at different concentrations of ethanol and water. Sixty percent of ethanolic ML extract showed highest inhibitory effect against α-glucosidase enzyme (IC50 of 37 μg/mL) and DPPH scavenging activity (IC50 of 48 μg/mL). Antidiabetic effect of ML extracts was also evaluated in vivo and it was found that the high doses (400 mg/Kg BW) of ML extract exhibited high suppression in fasting blood glucose level by 62.75%. The metabolites responsible for variation among ML samples with variable ethanolic levels have been evaluated successfully using (1) H-NMR-based metabolomics. The principal component analysis (PCA) and partial least squares(PLS) analysis scores depicted clear and distinct separations into 4 clusters representing the 4 ethanolic concentrations by PC1 and PC2, with an eigenvalue of 69.9%. Various (1) H-NMR chemical shifts related to the metabolites responsible for sample difference were also ascribed. The main bioactive compounds identified attributing toward the separation included: isorhamnetin, skimmianine, scopoletin, and melicarpinone. Hence, ML may be used as promising medicinal plant for the development of new functional foods, new generation antidiabetic drugs, as a single entity phytomedicine or in combinational therapy.
    Matched MeSH terms: alpha-Glucosidases/analysis; alpha-Glucosidases/metabolism*
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