Displaying publications 61 - 80 of 114 in total

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  1. 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: Glycoside Hydrolase Inhibitors
  2. 3-Benzyl(phenethyl)-2-thioxobenzo[g]quinazolines as a new class of potent α-glucosidase inhibitors: synthesis and molecular docking study
    Al-Salahi R, Ahmad R, Anouar E, Iwana Nor Azman NI, Marzouk M, Abuelizz HA
    Future Med Chem, 2018 08 01;10(16):1889-1905.
    PMID: 29882426 DOI: 10.4155/fmc-2018-0141
    AIM: Using a simple modification on a previously reported synthetic route, 3-benzyl(phenethyl)-2-thioxobenzo[g]quinazolin-4(3H)-ones (1 and 2) were synthesized with high yields. Further transformation of 1 and 2 produced derivatives 3-26, which were structurally characterized based on NMR and MS data, and their in vitro α-glucosidase inhibitory activity was evaluated using Baker's yeast α-glucosidase enzyme.

    RESULTS: Compounds 2, 4, 8, 12 and 20 exhibited the highest activity (IC50 = 69.20, 59.60, 49.40, 50.20 and 83.20 μM, respectively) compared with the standard acarbose (IC50 = 143.54 μM).

    CONCLUSION: A new class of potent α-glucosidase inhibitors was identified, and the molecular docking predicted plausible binding interaction of the targets in the binding pocket of α-glucosidase and rationalized the structure-activity relationship (SARs) of the target compounds.

    Matched MeSH terms: Glycoside Hydrolase Inhibitors/chemical synthesis*; Glycoside Hydrolase Inhibitors/pharmacology*; Glycoside Hydrolase Inhibitors/chemistry
  3. New pyrrolopyridine-based thiazolotriazoles as diabetics inhibitors: enzymatic kinetics and in silico study
    Taha M, Rahim F, Hayat S, Chigurupati S, Khan KM, Imran S, et al.
    Future Med Chem, 2023 Mar;15(5):405-419.
    PMID: 37013918 DOI: 10.4155/fmc-2022-0306
    Aim: To synthesize pyrrolopyridine-based thiazolotriazoles as a novel class of α-amylase and α-glucosidase inhibitors and to determine their enzymatic kinetics. Methodology: Pyrrolopyridine-based thiazolotriazole analogs (1-24) were synthesized and characterized through proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance and high-resolution electron ionization mass spectrometry. Results: All synthesized analogs displayed good inhibitory potential of α-amylase and α-glucosidase ranging 17.65-70.7 μM and 18.15-71.97 μM, respectively, compared with the reference drug, acarbose (11.98 μM and 12.79 μM). Analog 3 was the most potent among the synthesized analogs, having α-amylase and α-glucosidase inhibitory activity at 17.65 and 18.15 μM, respectively. The structure-activity relationship and binding modes of interactions between selected analogs were confirmed via docking and enzymatic kinetics studies. The compounds (1-24) were tested for cytotoxicity against the 3T3 mouse fibroblast cell line and were observed to be nontoxic.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/chemistry
  4. Fulltext Ergogenic, anti-diabetic and antioxidant attributes of selected Malaysian herbs: characterisation of flavonoids and correlation of functional activities
    Sallehuddin, N. A., Azizah Abdul Hamid, Salleh, S. Z., Nazia Abdul Majid, Hani Hafeeza Halim, Nurul Shazini Ramli, et al.
    International Food Research Journal, 2020;27(1):197-207.
    MyJurnal
    In the present work, aqueous ethanolic (60% ethanol) extracts from selected Malaysian herbs
    including Murraya koenigii L. Spreng, Lawsonia inermis L., Cosmos caudatus Kunth, Piper
    betle L., and P. sarmentosum Roxb. were evaluated for their ergogenic, anti-diabetic and
    antioxidant potentials. Results showed that the analysed herbs had ergogenic property and
    were able to activate 5'AMP-activated protein kinase (AMPK) in a concentration dependant
    manner. The highest AMPK activation was exhibited by M. koenigii extract which showed no
    significant (p > 0.05) difference with green tea (positive control). For anti-diabetic potential,
    the highest α-glucosidase inhibition was exhibited by M. koenigii extract with IC50 of 43.35
    ± 7.5 µg/mL, which was higher than acarbose (positive control). The determinations of free
    radical scavenging activity and total phenolics content (TPC) indicated that the analysed herbs
    had good antioxidant activity. However, C. caudatus extract showed superior antioxidant
    activity with IC50 against free radical and TPC of 21.12 ± 3.20 µg/mL and 221.61 ± 7.49 mg
    GAE/g, respectively. RP-HPLC analysis established the presence of flavonoids in the herbs
    wherein L. inermis contained the highest flavonoid (catechin, epicatechin, naringin and rutin)
    content (668.87 mg/kg of extract). Correlations between the analyses were conducted, and
    revealed incoherent trends. Overall, M. koenigii was noted to be the most potent herb for
    enhancement of AMPK activity and α-glucosidase inhibition but exhibited moderate antioxidant activity. These results revealed that the selected herbs could be potential sources of
    natural ergogenic and anti-diabetic/antioxidant agents due to their rich profile of phenolics.
    Further analysis in vivo should be carried out to further elucidate the mechanism of actions of
    these herbs as ergogenic aids and anti-diabetic/antioxidant agents.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors
  5. Fulltext In vitro antioxidant capacities and antidiabetic properties of phenolic extracts from selected citrus peels
    Lim, S.M., Loh, S.P.
    International Food Research Journal, 2016;23(1):211-219.
    MyJurnal
    This study aims to determine the antioxidant capacities (AC) and antidiabetic properties of
    phenolic extracts (free and bound) from white Tambun pomelo peels, kaffir lime peels, lime
    peels and calamansi peels. AC, total phenolic content (TPC) and antidiabetic properties of
    selected citrus peels extracts were determined spectrophotometrically using 2,2-Diphenyl-1-
    picrylhydrazyl free radical (DPPH) scavenging, ferric-reducing antioxidant power (FRAP),
    Folin-Ciocalteu (FC) and α-amylase and α-glucosidase inhibition assay, respectively. This
    study found that the methanolic extract of kaffir lime showed the best AC with the lowest
    IC50 value of DPPH radical (7.51 ± 0.50 mg/ml) and highest FRAP value [369.48 ± 20.15
    mM Fe (II) E/g DW]. TPC of free phenolic extracts of all citrus peels were significantly (p<
    0.05) higher compared to the bound phenolic extracts with extract of calamansi showed the
    highest TPC. Free- and bound phenolic extract of calamansi also had the highest α-amylase
    inhibition activity (61.79 ± 4.13%; 45.30 ± 5.35%) respectively. The highest inhibitory effect in
    α-glucosidase inhibition assay of free- and bound phenolic extracts were white Tambun pomelo
    (41.06 ± 10.94%) and calamansi (43.99 ± 22.03%) respectively. Hence, the citrus peels could
    be furthered study for their potential in management and/or prevention of diabetes.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors
  6. Synthesis of indole derivatives as diabetics II inhibitors and enzymatic kinetics study of α-glucosidase and α-amylase along with their in-silico study
    Taha M, Alrashedy AS, Almandil NB, Iqbal N, Anouar EH, Nawaz M, et al.
    Int J Biol Macromol, 2021 Nov 01;190:301-318.
    PMID: 34481854 DOI: 10.1016/j.ijbiomac.2021.08.207
    In this study, we have investigated a series of indole-based compounds for their inhibitory study against pancreatic α-amylase and intestinal α-glucosidase activity. Inhibitors of carbohydrate degrading enzymes appear to have an essential role as antidiabetic drugs. All analogous exhibited good to moderate α-amylase (IC50 = 3.80 to 47.50 μM), and α-glucosidase inhibitory interactions (IC50 = 3.10-52.20 μM) in comparison with standard acarbose (IC50 = 12.28 μM and 11.29 μM). The analogues 4, 11, 12, 15, 14 and 17 had good activity potential both for enzymes inhibitory interactions. Structure activity relationships were deliberated to propose the influence of substituents on the inhibitory potential of analogues. Docking studies revealed the interaction of more potential analogues and enzyme active site. Further, we studied their kinetic study of most active compounds showed that compounds 15, 14, 12, 17 and 11 are competitive for α-amylase and non- competitive for α-glucosidase.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology*; Glycoside Hydrolase Inhibitors/chemistry
  7. Antioxidant and α-glucosidase inhibitory activities of 40 tropical juices from Malaysia and identification of phenolics from the bioactive fruit juices of Barringtonia racemosa and Phyllanthus acidus
    Sulaiman SF, Ooi KL
    J Agric Food Chem, 2014 Oct 1;62(39):9576-85.
    PMID: 25198055 DOI: 10.1021/jf502912t
    The present study compared pH, total soluble solids, vitamin C, and total phenolic contents, antioxidant activities, and α-glucosidase inhibitory activities of 40 fresh juices. The juice of Baccaurea polyneura showed the highest yield (74.17 ± 1.44%) and total soluble solids (32.83 ± 0.27 °Brix). The highest and lowest pH values were respectively measured from the juices of Dimocarpus longan (6.87 ± 0.01) and Averrhoa bilimbi (1.67 ± 0.67). The juice of Psidium guajava gave the highest total phenolic (857.24 ± 12.65 μg GAE/g sample) and vitamin C contents (590.31 ± 7.44 μg AAE/g sample). The juice of Phyllanthus acidus with moderate contents of total phenolics and vitamin C was found to exhibit the greatest scavenging (613.71 ± 2.59 μg VCEAC/g sample), reducing (2784.89 ± 3.93 μg TEAC/g sample), and α-glucosidase inhibitory activities (95.37 ± 0.15%). The juice of Barringtonia racemosa was ranked second in the activities and total phenolic content. Gallic and ellagic acids, which were quantified as the major phenolics of the respective juices, are suggested to be the main contributors to the antioxidant activities. The α-glucosidase inhibitory activity of the juices could be derived from myricetin and quercetin (that were previously reported as potent α-glucosidase inhibitors) in the hydrolyzed juice extracts. The juice of Syzygium samarangense, which was found to be highest in metal chelating activity (82.28 ± 0.10%), also was found to have these phenolics.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/chemistry*
  8. Antioxidant and α-glucosidase inhibitory activities of cucurbit fruit vegetables and identification of active and major constituents from phenolic-rich extracts of Lagenaria siceraria and Sechium edule
    Sulaiman SF, Ooi KL, Supriatno
    J Agric Food Chem, 2013 Oct 23;61(42):10080-90.
    PMID: 24059845 DOI: 10.1021/jf4031037
    Antioxidant and α-glucosidase activities and total phenolic contents (TPC) in sequential extracts of dried pulps from seven cucurbit fruit vegetables were determined for the first time. The highest TPC and metal chelating activity were obtained from the chloroform extracts of Luffa acutangula (28.04 ± 0.37 mg GAE/g extract) and Benincasa hispida (EC50 = 0.44 ± 0.03 mg/mL), respectively. The ethyl acetate extract of Sechium edule showed the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity (951.73 ± 29.14 mM TE/g extract). The highest reducing and anti-α-glucosidase activities were shown by the methanol and ethyl acetate extracts of Momordica charantia (692.56 ± 43.38 mM AscAE/g extract; 66.64 ± 2.94%, respectively). The highest correlation (r = 0.99) was observed between the TPC and DPPH values of S. edule. Although caffeic acid was quantified as the major constituent in the methanol extract of Lagenaria siceraria , isoquercetin was found to be the main contributor to the activities. Gallic acid was identified as both the main and most active antioxidant constituent in the ethyl acetate extract of S. edule.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors*
  9. Cytotoxicity, alpha-glucosidase inhibition and molecular docking studies of hydroxamic acid chromium(III) complexes
    Hassan LR, Anouar EH, Bahron H, Abdullah F, Mohd Tajuddin A
    J Biol Inorg Chem, 2020 03;25(2):239-252.
    PMID: 31974764 DOI: 10.1007/s00775-020-01755-6
    Hydroxamic acids [R(CO)N(OH)R'] are flexible compounds for organic and inorganic analyses due to their frailer structures compared to the carboxylic acid. The syntheses and characterization of benzohydroxamic acid (BHA), its CH3-, OCH3-, Cl- para-substituted derivatives and their Cr(III) complexes are reported herein. The metal complexes were synthesized by reacting the hydroxamic acids with chromium(III) chloride hexahydrate in 2:1 molar ratio. The compounds were characterized via melting point, elemental analysis, FTIR, 1H and 13C NMR, TGA, mass spectrometry, molar conductance and UV-Visible. Data analysis suggests that each complex has the Cr(III) center coordinated to the carbonyl and hydroxy oxygen atoms of the hydroxamic acids in bidentate O,O manner and two water molecules to form octahedral geometry. Non-electrolytic behavior of the complexes was shown through their low molar conductivity. Cytotoxicity study against HCT116 and alpha-glucosidase inhibition test revealed that all complexes have higher activity than their parent ligands. Molecular docking study shows that the docking of active complexes is thermodynamically favorable and the inhibition efficiency may depend on the types and the numbers of molecular interactions established in the corresponding stable conformers.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/chemical synthesis; Glycoside Hydrolase Inhibitors/pharmacology*; Glycoside Hydrolase Inhibitors/chemistry
  10. Synthesis, α-amylase and α-glucosidase inhibition and molecular docking studies of indazole derivatives
    Nawaz M, Taha M, Qureshi F, Ullah N, Selvaraj M, Shahzad S, et al.
    J Biomol Struct Dyn, 2022;40(21):10730-10740.
    PMID: 34463216 DOI: 10.1080/07391102.2021.1947892
    Herein, we report the synthesis and inhibitory potential of indazole (Methyl 1H-indazole-4-carboxylate) derivatives (1-13) against α-amylase and α-glucosidase enzymes. The described derivatives demonstrated good inhibitory potential with IC50 values, ranging between 15.04 ± 0.05 to 76.70 ± 0.06 µM ± SEM for α-amylase and 16.99 ± 0.19 to 77.97 ± 0.19 µM ± SEM for α-glucosidase, respectively. In particular, compounds (8-10 and 12) displayed significant inhibitory activities against both the screened enzymes, with their inhibitory potential comparable to the standard acarbose (12.98 ± 0.03 and 12.79 ± 0.17 µM ± SEM, respectively). Additionally, the influence of different substituents on enzyme inhibition activities was assessed to study the structure activity relationships. Molecular docking simulations were performed to rationalize the binding of derivatives/compounds with enzymes. All the synthesized derivatives (1-13) were characterized with the aid of spectroscopic instruments such as 1H-NMR, 13C-NMR, HR-MS, elemental analysis and FTIR.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology; Glycoside Hydrolase Inhibitors/chemistry
  11. Molecular dynamics simulations reveal the inhibitory mechanism of Withanolide A against α-glucosidase and α-amylase
    Oyewusi HA, Wu YS, Safi SZ, Wahab RA, Hatta MHM, Batumalaie K
    J Biomol Struct Dyn, 2023;41(13):6203-6218.
    PMID: 35904027 DOI: 10.1080/07391102.2022.2104375
    Diabetes mellitus (DM) is a global chronic disease characterized by hyperglycemia and insulin resistance. The unsavory severe gastrointestinal side-effects of synthetic drugs to regulate hyperglycemia have warranted the search for alternative treatments to inhibit the carbohydrate digestive enzymes (e.g. α-amylase and α-glucosidase). Certain phytochemicals recently captured the scientific community's attention as carbohydrate digestive enzyme inhibitors due to their low toxicity and high efficacy, specifically the Withanolides-loaded extract of Withania somnifera. That said, the present study evaluated in silico the efficacy of Withanolide A in targeting both α-amylase and α-glucosidase in comparison to the synthetic drug Acarbose. Protein-ligand interactions, binding affinity, and stability were characterized using pharmacological profiling, high-end molecular docking, and molecular-dynamic simulation. Withanolide A inhibited the activity of α-glucosidase and α-amylase better, exhibiting good pharmacokinetic properties, absorption, and metabolism. Also, Withanolide A was minimally toxic, with higher bioavailability. Interestingly, Withanolide A bonded well to the active site of α-amylase and α-glucosidase, yielding the lowest binding free energy of -82.144 ± 10.671 kcal/mol and -102.1043 ± 11.231 kcal/mol compared to the Acarbose-enzyme complexes (-63.220 ± 13.283 kcal/mol and -82.148 ± 10.671 kcal/mol). Hence, the findings supported the therapeutic potential of Withanolide A as α-amylase and α-glucosidase inhibitor for DM treatment.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology; Glycoside Hydrolase Inhibitors/chemistry
  12. 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: Glycoside Hydrolase Inhibitors/analysis*; Glycoside Hydrolase Inhibitors/metabolism
  13. Fulltext Inhibitory evaluation of Curculigo latifolia on α-glucosidase, DPP (IV) and in vitro studies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus
    Zabidi NA, Ishak NA, Hamid M, Ashari SE, Mohammad Latif MA
    J Enzyme Inhib Med Chem, 2021 Dec;36(1):109-121.
    PMID: 33249946 DOI: 10.1080/14756366.2020.1844680
    The inhibition of α-glucosidase and DPP enzymes capable of effectively reducing blood glucose level in the management of type 2 diabetes. The purpose of the present study is to evaluate the inhibitory potential of α-glucosidase and DPP (IV) activity including with the 2-NBDG uptake assay and insulin secretion activities through in vitro studies. The selected of active compounds obtained from the screening of compounds by LC-MS were docked with the targeted enzyme that involved in the mechanism of T2DM. From the results, root extracts displayed a better promising outcome in α-glucosidase (IC50 2.72 ± 0.32) as compared with the fruit extracts (IC50 3.87 ± 0.32). Besides, root extracts also displayed a better activity in the inhibition of DPP (IV), enhance insulin secretion and glucose uptake activity. Molecular docking results revealing that phlorizin binds strongly with α-glucosidase, DPP (IV) and Insulin receptor (IR) enzymes with achieving the lowest binding energy value. The present work suggests several of the compounds have the potential that contribute towards inhibiting α-glucosidase and DPP (IV) and thus effective in lowering post-prandial hyperglycaemia.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/isolation & purification; Glycoside Hydrolase Inhibitors/pharmacology*; Glycoside Hydrolase Inhibitors/chemistry
  14. Growth inhibition of human liver carcinoma HepG2 cells and α-glucosidase inhibitory activity of Murdannia bracteata (C.B. Clarke) Kuntze ex J.K. Morton extracts
    Ooi KL, Loh SI, Tan ML, Muhammad TS, Sulaiman SF
    J Ethnopharmacol, 2015 Mar 13;162:55-60.
    PMID: 25554642 DOI: 10.1016/j.jep.2014.12.030
    The juice of the entire fresh herb and infusion of dried sample of Murdannia bracteata are consumed to treat liver cancer and diabetes in Malaysia. However, no scientific evidence of these bioactivities has been reported.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology*
  15. Vitexin and isovitexin from the Leaves of Ficus deltoidea with in-vivo α-glucosidase inhibition
    Choo CY, Sulong NY, Man F, Wong TW
    J Ethnopharmacol, 2012 Aug 1;142(3):776-81.
    PMID: 22683902 DOI: 10.1016/j.jep.2012.05.062
    The leaves of Ficus deltoidea are used as a traditional medicine by diabetes patients in Malaysia.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors*
  16. Cytotoxic, apoptotic and anti-α-glucosidase activities of 3,4-di-O-caffeoyl quinic acid, an antioxidant isolated from the polyphenolic-rich extract of Elephantopus mollis Kunth
    Ooi KL, Muhammad TS, Tan ML, Sulaiman SF
    J Ethnopharmacol, 2011 Jun 1;135(3):685-95.
    PMID: 21497647 DOI: 10.1016/j.jep.2011.04.001
    The decoction of the whole plant of Elephantopus mollis Kunth. is traditionally consumed to treat various free radical-mediated diseases including cancer and diabetes.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors*
  17. Fulltext Metabolite profiling, antioxidant, and α-glucosidase inhibitory activities of germinated rice: nuclear-magnetic-resonance-based metabolomics study
    Pramai P, Abdul Hamid NA, Mediani A, Maulidiani M, Abas F, Jiamyangyuen S
    J Food Drug Anal, 2018 01;26(1):47-57.
    PMID: 29389588 DOI: 10.1016/j.jfda.2016.11.023
    In an attempt to profile the metabolites of three different varieties of germinated rice, specifically black (GBR), red, and white rice, a 1H-nuclear-magnetic-resonance-based metabolomics approach was conducted. Multivariate data analysis was applied to discriminate between the three different varieties using a partial least squares discriminant analysis (PLS-DA) model. The PLS model was used to evaluate the relationship between chemicals and biological activities of germinated rice. The PLS-DA score plot exhibited a noticeable separation between the three rice varieties into three clusters by PC1 and PC2. The PLS model indicated that α-linolenic acid, γ-oryzanol, α-tocopherol, γ-aminobutyric acid, 3-hydroxybutyric acid, fumaric acid, fatty acids, threonine, tryptophan, and vanillic acid were significantly correlated with the higher bioactivities demonstrated by GBR that was extracted in 100% ethanol. Subsequently, the proposed biosynthetic pathway analysis revealed that the increased quantities of secondary metabolites found in GBR may contribute to its nutritional value and health benefits.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology*; Glycoside Hydrolase Inhibitors/chemistry
  18. 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: Glycoside Hydrolase Inhibitors/analysis; Glycoside Hydrolase Inhibitors/pharmacology*
  19. Multidirectional insights into the biochemical and toxicological properties of Bougainvillea glabra (Choisy.) aerial parts: A functional approach for bioactive compounds
    Saleem H, Zengin G, Ahmad I, Lee JTB, Htar TT, Mahomoodally FM, et al.
    J Pharm Biomed Anal, 2019 Jun 05;170:132-138.
    PMID: 30921647 DOI: 10.1016/j.jpba.2019.03.027
    The current research work was conducted in order to probe into the biochemical and toxicological characterisation of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (Choisy.) aerial parts. Biological fingerprints were assessed for in vitro antioxidant, key enzyme inhibitory and cytotoxicity potential. Total bioactive contents were determined spectrophotometrically and the secondary metabolite components of methanol extract was assessed by UHPLC mass spectrometric analysis. The antioxidant capabilities were evaluated via six different in vitro antioxidant assays namely DPPH, ABTS (free radical scavenging), FRAP, CUPRAC (reducing antioxidant power), phosphomolybdenum (total antioxidant capacity) and ferrous chelating activity. Inhibition potential against key enzymes urease, α-glucosidase and cholinesterases were also determined. Methanol extract exhibited higher phenolic (24.01 mg GAE/g extract) as well as flavonoid (41.51 mg QE/g extract) contents. Phytochemical profiling of methanol extract identified a total of twenty secondary metabolites and the major compounds belonged to flavonoids, phenolics and alkaloid derivatives. The findings of antioxidant assays revealed the methanol extract to exhibit stronger antioxidant (except phosphomolybdenum) activities. Similarly, the methanol extract showed highest butyrylcholinesterase and urease inhibition. The DCM extract was most active for phosphomolybdenum and α-glucosidase inhibition assays. Moreover, both extracts exhibited significant cytotoxic potential against five (MCF-7, MDA-MB-231, CaSki, DU-145, and SW-480) human carcinoma cell lines with half maximal inhibitory concentration values of 22.09 to 257.2 μg/mL. Results from the present study highlighted the potential of B. glabra aerial extracts to be further explored in an endeavour to discover novel phytotherapeutics as well as functional ingredients.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/chemistry
  20. Fulltext Phytochemical screening and enzymatic and antioxidant activities of Erythrina suberosa (Roxb) bark
    Ahmed Z, Aziz S, Hanif M, Mohiuddin SG, Ali Khan SH, Ahmed R, et al.
    J Pharm Bioallied Sci, 2020 04 10;12(2):192-200.
    PMID: 32742119 DOI: 10.4103/jpbs.JPBS_222_19
    Background: This study aimed to evaluate the phytochemicals screening of Erythrina suberosa (Roxb) bark and to analyze the enzymatic activities of its various organic fractions.

    Materials and Methods: Crude methanolic fraction of E. suberosa (Roxb) bark and its respective fractions were screened for the presence of different phytochemicals with different reagents. On the basis of increasing order of polarity, different organic solvents were used to obtain different fractions. Enzymatic studies were performed on crude methanolic extract of the plant. All the assays were performed under standard in vitro conditions.

    Results: The phytochemical analysis shows the presence of alkaloids, phenols, triterpenoids, phytosterols, and flavonoids. Phenolic compounds and flavonoids are the major constituents of the plant. In anticholinesterase assay, the percent inhibition of standard drug (eserine) was 91.27 ± 1.17 and the half maximal inhibitory concentration (IC50) was 0.04 ± 0.0001. For α-glucosidase inhibition, the IC50 value for Dichloromethane fraction was 8.45 ± 0.13, for Methanol fraction it was 64.24 ± 0.15, and for aqueous fraction it was 42.62 ± 0.17 as compared with standard IC50 that is 37.42 (acarbose). Furthermore, results show that all fractions have potential against anti-urease enzyme, but DCM fraction of crude aqueous extract has significant IC50 value (45.26 ± 0.13) than other fractions.

    Conclusion: Keeping in view all the results, it is evident that the plant can be used in future for formulating effective drugs against many ailments. Secondary metabolites and their derivatives possess different biological activities, for example, .g. flavonoids in cancer, asthma, and Alzheimer. Furthermore, the extracts of this plant can be used in their crude form, which is an addition to the complementary and alternative treatment strategies.

    Matched MeSH terms: Glycoside Hydrolase Inhibitors
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