Displaying publications 1 - 20 of 131 in total

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  1. Vyas K, Prabaker S, Prabhu D, Sakthivelu M, Rajamanikandan S, Velusamy P, et al.
    Int J Biol Macromol, 2024 Feb;259(Pt 1):129222.
    PMID: 38185307 DOI: 10.1016/j.ijbiomac.2024.129222
    The substantial nutritional content and diversified biological activity of plant-based nutraceuticals are due to polyphenolic chemicals. These chemicals are important and well-studied plant secondary metabolites. Their protein interactions are extensively studied. This relationship is crucial for the logical development of functional food and for enhancing the availability and usefulness of polyphenols. This study highlights the influence of protein types and polyphenols on the interaction, where the chemical bindings predominantly consist of hydrophobic interactions and hydrogen bonds. The interaction between polyphenolic compounds (PCs) and digestive enzymes concerning their inhibitory activity has not been fully studied. Therefore, we have examined the interaction of four digestive enzymes (α-amylase, pepsin, trypsin, and α-chymotrypsin) with four PCs (curcumin, diosmin, morin, and 2',3',4'-trihydroxychalcone) through in silico and in vitro approaches. In vitro plate assays, enzyme kinetics, spectroscopic assays, molecular docking, and simulations were performed. We observed all these PCs have significant docking scores and preferable interaction with the active site of the digestive enzymes, resulting in the reduction of enzyme activity. The enzyme-substrate binding mechanism was determined using the Lineweaver Burk plot, indicating that the inhibition occurred competitively. Among four PCs diosmin and morin has the highest interaction energy over digestive enzymes with IC50 value of 1.13 ± 0.0047 and 1.086 ± 0.0131 μM. Kinetic studies show that selected PCs inhibited pepsin, trypsin, and chymotrypsin competitively and inhibited amylase in a non-competitive manner, especially by 2',3',4'-trihydroxychalcone. This study offers insights into the mechanisms by which the selected PCs inhibit the enzymes and has the potential to enhance the application of curcumin, diosmin, morin, and 2',3',4'-trihydroxychalcone as natural inhibitors of digestive enzymes.
    Matched MeSH terms: alpha-Glucosidases/metabolism
  2. Ahda M, Jaswir I, Khatib A, Ahmed QU, Mahfudh N, Ardini YD, et al.
    Sci Rep, 2023 Oct 09;13(1):17012.
    PMID: 37813908 DOI: 10.1038/s41598-023-43251-2
    Ocimum aristatum, commonly known as O. stamineus, has been widely studied for its potential as an herbal medicine candidate. This research aims to compare the efficacy of water and 100% ethanolic extracts of O. stamineus as α-glucosidase inhibitors and antioxidants, as well as toxicity against zebrafish embryos. Based on the study findings, water extract of O. stamineus leaves exhibited superior inhibition activity against α-glucosidase, ABTS, and DPPH, with IC50 values of approximately 43.623 ± 0.039 µg/mL, 27.556 ± 0.125 µg/mL, and 95.047 ± 1.587 µg/mL, respectively. The major active compounds identified in the extract include fatty acid groups and their derivates such as linoleic acid, α-eleostearic acid, stearic acid, oleanolic acid, and corchorifatty acid F. Phenolic groups such as caffeic acid, rosmarinic acid, 3,4-Dihydroxybenzaldehyde, norfenefrine, caftaric acid, and 2-hydroxyphenylalanine and flavonoids and their derivates including 5,7-Dihydroxychromone, 5,7-Dihydroxy-2,6-dimethyl-4H-chromen-4-one, eupatorin, and others were also identified in the extract. Carboxylic acid groups and triterpenoids such as azelaic acid and asiatic acid were also present. This study found that the water extract of O. stamineus is non-toxic to zebrafish embryos and does not affect the development of zebrafish larvae at concentrations lower than 500 µg/mL. These findings highlight the potential of the water extract of O. stamineus as a valuable herbal medicine candidate, particularly for its potent α-glucosidase inhibition and antioxidant properties, and affirm its safety in zebrafish embryos at tested concentrations.
    Matched MeSH terms: alpha-Glucosidases
  3. El Omari N, Mrabti HN, Benali T, Ullah R, Alotaibi A, Abdullah ADI, et al.
    Front Biosci (Landmark Ed), 2023 Sep 27;28(9):229.
    PMID: 37796709 DOI: 10.31083/j.fbl2809229
    BACKGROUND: Screening new natural molecules with pharmacological and/or cosmetic properties remains a highly sought-after area of research. Moreover, essential oils and volatile compounds have recently garnered significant interest as natural substance candidates. In this study, the volatile components of Pistacia lentiscus L. essential oils (PLEOs) isolated from the fruit and its main compounds, alpha-pinene, and limonene, are investigated for antioxidant, antidiabetic, and dermatoprotective activities.

    METHODS: In vitro antioxidant activity was investigated using 2,2'-diphenyl-1-picrylhydrazyl (DPPH), fluorescence recovery after photobleaching (FRAP), and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. The antidiabetic and dermatoprotective effects were studied using enzyme inhibitory activities.

    RESULTS: Antioxidant tests showed that PLEO has the best activity (ranging from 29.64 ± 3.04 to 73.80 ± 3.96 µg/mL) compared to its main selected molecules (ranging from 74 ± 3.72 to 107.23 ± 5.03 µg/mL). The α-glucosidase and α-amylase assays demonstrated that the elements tested have a promising antidiabetic potential with IC50values ranging from 78.03 ± 2.31 to 116.03 ± 7.42 µg/mL and 74.39 ± 3.08 to 112.35 ± 4.92 µg/mL for the α-glucosidase and α-amylase assays, respectively, compared to the standard drug. For the tyrosinase test, we found that the EOs (IC50 = 57.72 ± 2.86 µg/mL) followed by limonene (IC50 = 74.24 ± 2.06 µg/mL) and α-pinene (IC50 = 97.45 ± 5.22 µg/mL) all exhibited greater inhibitory effects than quercetin (IC50 = 246.90 ± 2.54 µg/mL).

    CONCLUSIONS: Our results suggest that the biological activities of PLEO, as well as its main compounds, make them promising candidates for the development of new strategies aimed at improving dermatoprotection and treating diseases associated with diabetes mellitus and oxidative stress.

    Matched MeSH terms: alpha-Glucosidases
  4. 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
  5. El Hachlafi N, Benkhaira N, Al-Mijalli SH, Mrabti HN, Abdnim R, Abdallah EM, et al.
    Biomed Pharmacother, 2023 Aug;164:114937.
    PMID: 37267633 DOI: 10.1016/j.biopha.2023.114937
    Mentha suaveolens, Lavandula stoechas, and Ammi visnaga are widely used in Moroccan folk medicine against several pathological disorders, including diabetes and infectious diseases. This work was designed to determine the chemical profile of M. suaveolens (MSEO), L. stoechas (LSEO), and A. visnaga (AVEO) essential oils and assess their antimicrobial, antioxidant, and antidiabetic effects. The volatile components of LSEO, AVEO, and MSEO were analyzed using Gas Chromatography-Mass Spectrometry (GC-MS). The in vitro antidiabetic activity was assessed using α-amylase and α-glucosidase enzymes, while DPPH, FRAP, and β-carotene/linoleic acid methods were used to determine the antioxidant capacity. The antimicrobial activities were investigated using disc diffusion and broth-microdilution assays. GC-MS investigation revealed that the main components were fenchone (29.77 %) and camphor (24.9 %) for LSEO, and linalool (38.29 %) for AVEO, while MSEO was mainly represented by piperitenone oxide (74.55 %). The results of the antimicrobial evaluation showed that all examined essential oils (EOs) had noticeable antimicrobial activity against both bacteria and yeast, especially Micrococcus luteus and Bacillus subtilis. The MIC, MBC, and MFC values were ranged from 0.015 % to 0.5 %. The MBC/MIC and MFC/MIC ratios were less than or equal to 4.0 % (v/v), indicating their noticeable bactericidal and candidacidal efficacy. Moreover, the three EOs showed significant inhibitory effects on α-amylase and α-glucosidase (p 
    Matched MeSH terms: alpha-Glucosidases
  6. 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
  7. Munawaroh HSH, Pratiwi RN, Gumilar GG, Aisyah S, Rohilah S, Nurjanah A, et al.
    Int J Biol Macromol, 2023 Mar 15;231:123248.
    PMID: 36642356 DOI: 10.1016/j.ijbiomac.2023.123248
    Gelatin hydrogel is widely employed in various fields, however, commercially available gelatin hydrogels are mostly derived from mammalian which has many disadvantages due to the supply and ethical issues. In this study, the properties of hydrogels from fish-derived collagen fabricated with varying Glutaraldehyde (GA) determined. The antidiabetic properties of salmon gelatin (SG) and tilapia gelatin (TG) was also evaluated against α-glucosidase. Glutaraldehyde-crosslinked salmon gelatin and tilapia gelatin were used, and compared with different concentrations of GA by 0.05 %, 0.1 %, and 0.15 %. Water absorbency, swelling, porosity, pore size and water retention of the hydrogels were dependent on the degree of crosslinking. The synthesis of hydrogels was confirmed by FTIR study. Scanning electron microscope (SEM) observation showed that all hydrogels have a porous structure with irregular shapes and heterogeneous morphology. Performance tests showed that gelatin-GA 0.05 % mixture had the best performance. Antidiabetic bioactivity in vitro and in silico tests showed that the active peptides of SG and TG showed a high binding affinity to α-glucosidase enzyme. In conclusion, SG and TG cross-linked GA 0.05 % have the potential as an antidiabetic agent and as a useful option over mammalian-derived gelatin.
    Matched MeSH terms: alpha-Glucosidases
  8. 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
  9. 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: alpha-Glucosidases/metabolism
  10. 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: alpha-Glucosidases/chemistry
  11. Wee AS, Nhu TD, Khaw KY, Tang KS, Yeong KY
    Curr Neuropharmacol, 2023;21(10):2036-2048.
    PMID: 36372924 DOI: 10.2174/1570159X21999221111102343
    Alzheimer's disease (AD) and type 2 diabetes mellitus (DM) are more prevalent with ageing and cause a substantial global socio-economic burden. The biology of these two conditions is well elaborated, but whether AD and type 2 DM arise from coincidental roots in ageing or are linked by pathophysiological mechanisms remains unclear. Research findings involving animal models have identified mechanisms shared by both AD and type 2 DM. Deposition of β-amyloid peptides and formation of intracellular neurofibrillary tangles are pathological hallmarks of AD. Type 2 DM, on the other hand, is a metabolic disorder characterised by hyperglycaemia and insulin resistance. Several studies show that improving type 2 DM can delay or prevent the development of AD, and hence, prevention and control of type 2 DM may reduce the risk of AD later in life. Alpha-glucosidase is an enzyme that is commonly associated with hyperglycaemia in type 2 DM. However, it is uncertain if this enzyme may play a role in the progression of AD. This review explores the experimental evidence that depicts the relationship between dysregulation of glucose metabolism and AD. We also delineate the links between alpha-glucosidase and AD and the potential role of alpha-glucosidase inhibitors in treating AD.
    Matched MeSH terms: alpha-Glucosidases/metabolism
  12. Kasim N, Afzan A, Mediani A, Low KH, Ali AM, Mat N, et al.
    Phytochem Anal, 2022 Dec;33(8):1235-1245.
    PMID: 36192845 DOI: 10.1002/pca.3175
    INTRODUCTION: Ficus deltoidea Jack (Moraceae) is a plant used in Malaysia to treat various ailments, including diabetes. The presence of several varieties raises essential questions regarding which is the potential bioactive variety and what are the bioactive metabolites.

    OBJECTIVES: Here, we explored the phytochemical diversity of the seven varieties from Peninsular Malaysia using Nuclear Magnetic Resonance (NMR) and Liquid Chromatography-Mass Spectrometry (LC-MS) analyses and correlated it with the α-glucosidase inhibitory activity.

    METHODOLOGY: The Nuclear Overhauser Effect Spectroscopy (NOESY) One-Dimensional (1D)-NMR and LC-MS data were processed, annotated, and correlated with in vitro α-glucosidase inhibitory using multivariate data analysis.

    RESULTS: The α-glucosidase results demonstrated that different varieties have varying inhibitory effects, with the highest inhibition rate being F. deltoidea var. trengganuensis and var. kunstleri. Furthermore, diverse habitats and plant ages could also influence the inhibitory rate. The heat map from NMR and LC-MS profiles showed unique patterns according to varying levels of α-glucosidase inhibition rate. The Partial Least Squares (PLS) model constructed from both NMR and LC-MS further confirmed the correlation between the α-glucosidase inhibition rate of F. deltoidea varieties and its metabolite profiles. The Variable Influence on Projection (VIP) and correlation coefficient (p(corr)) values values were used to determine the highly relevant metabolites for explaining the anticipated inhibitory action.

    CONCLUSION: NMR and LC-MS annotations allow the identification of flavan-3-ols and proanthocyanidins as the key bioactive factors. Our current results demonstrated the value of multivariate data analysis to predict the quality of herbal materials from both biological and chemical aspects.

    Matched MeSH terms: alpha-Glucosidases
  13. Suroowan S, Llorent-Martínez EJ, Zengin G, Dall'Acqua S, Sut S, Buskaran K, et al.
    Molecules, 2022 Sep 10;27(18).
    PMID: 36144622 DOI: 10.3390/molecules27185886
    Artemisia verlotiorum Lamotte is recognized medicinally given its long-standing ethnopharmacological uses in different parts of the world. Nonetheless, the pharmacological properties of the leaves of the plant have been poorly studied by the scientific community. Hence, this study aimed to decipher the phytochemicals; quantify through HPLC-ESI-MS analysis the plant’s biosynthesis; and evaluate the antioxidant, anti-tyrosinase, amylase, glucosidase, cholinesterase, and cytotoxicity potential on normal (NIH 3T3) and human liver and human colon cancer (HepG2 and HT 29) cell lines of this plant species. The aqueous extract contained the highest content of phenolics and phenolic acid, methanol extracted the most flavonoid, and the most flavonol was extracted by ethyl acetate. The one-way ANOVA results demonstrated that all results obtained were statistically significant at p < 0.05. A total of 25 phytoconstituents were identified from the different extracts, with phenolic acids and flavonoids being the main metabolites. The highest antioxidant potential was recorded for the aqueous extract. The best anti-tyrosinase extract was the methanolic extract. The ethyl acetate extract of A. verlotiorum had the highest flavonol content and hence was most active against the cholinesterase enzymes. The ethyl acetate extract was the best α-glucosidase and α-amylase inhibitor. The samples of Artemisia verlotiorum Lamotte in both aqueous and methanolic extracts were found to be non-toxic after 48 h against NIH 3T3 cells. In HepG2 cells, the methanolic extract was nontoxic up to 125 µg/mL, and an IC50 value of 722.39 µg/mL was recorded. The IC50 value exhibited in methanolic extraction of A. verlotiorum was 792.91 µg/mL in HT29 cells. Methanolic extraction is capable of inducing cell cytotoxicity in human hepatocellular carcinoma without damaging normal cells. Hence, A. verlotiorum can be recommended for further evaluation of its phytochemical and medicinal properties.
    Matched MeSH terms: alpha-Glucosidases/chemistry
  14. Liu Y, Kong KW, Wu DT, Liu HY, Li HB, Zhang JR, et al.
    Food Chem, 2022 Apr 16;374:131635.
    PMID: 34823934 DOI: 10.1016/j.foodchem.2021.131635
    The pomegranate peel is a by-product of pomegranate fruit rich in polyphenols. In this study, pomegranate peel polyphenols were explored using LC-MS/MS, and punicalagin was the most abundant compound. The highest yield (505.89 ± 1.73 mg/g DW) of punicalagin was obtained by ultrasonic-assisted extraction (UAE) with the ethanol concentration of 53%, sample-to-liquid ratio of 1:25 w/v, ultrasonic power of 757 W, and extraction time of 25 min. Punicalagin was further purified by the macroporous resin D101 and prep-HPLC, reaching the purity of 92.15%. The purified punicalagin had the IC50 of 82 ± 0.02 µg/mL against α-glucosidase, similar to the punicalagin standard with IC50 of 58 ± 0.014 µg/mL, both exhibiting a mixed inhibitory mechanism. Molecular docking further revealed that a steric hindrance with the intermolecular energy of -7.99 kcal/mol was formed between punicalagin and α-glucosidase. Overall, pomegranate peel is a promising source of punicalagin to develop anti-diabetic functional foods.
    Matched MeSH terms: alpha-Glucosidases
  15. Jamil W, Shaikh J, Yousuf M, Taha M, Khan KM, Shah SAA
    J Biomol Struct Dyn, 2022;40(23):12723-12738.
    PMID: 34514955 DOI: 10.1080/07391102.2021.1975565
    This study reports synthesis of flavone hydrazide Schiff base derivatives with diverse functionalities for the cure of diabetic mellitus and their a-glucosidase inhibitor and in silico studies. In this regard, Flavone derivatives 1-20 has synthesized and characterized by various spectroscopic techniques. These compounds showed significant potential towards a-glucosidase enzyme inhibition activity and found to be many fold better active than the standard Acarbose (IC50 = 39.45 ± 0.11 µM). The IC50values ranges 1.02-38.1 µM. Among these, compounds 1(IC50 = 4.6 ± 0.23 µM), 2(IC50 = 1.02 ± 0.2 µM), 3(IC50 = 7.1 ± 0.11 µM), 4(IC50 = 8.3 ± 0.34 µM), 5(IC50 = 7.4 ± 0.15 µM), 6(IC50 = 8.5 ± 0.27 µM) and 18 (IC50 = 1.09 ± 0.26 µM) showed highest activity. It was revealed that the analogues having -OH substitution have higher activity than their look likes. The molecular docking analysis revealed that these molecules have high potential to interact with the protein molecule and have high ability to bind with the enzyme. Furthermore, in silico pharmacokinetics, physicochemical studies were also performed for these derivatives. The bioavailability radar analysis explored that of all these compounds have excellent bioavailability for five (5) descriptors, however, the sixth descriptor of instauration is slightly increased in all compounds.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: alpha-Glucosidases/chemistry
  16. Akinyede KA, Oyewusi HA, Hughes GD, Ekpo OE, Oguntibeju OO
    Molecules, 2021 Dec 28;27(1).
    PMID: 35011387 DOI: 10.3390/molecules27010155
    Diabetes mellitus (DM) is a chronic metabolic condition that can lead to significant complications and a high fatality rate worldwide. Efforts are ramping up to find and develop novel α-glucosidase and α-amylase inhibitors that are both effective and potentially safe. Traditional methodologies are being replaced with new techniques that are less complicated and less time demanding; yet, both the experimental and computational strategies are viable and complementary in drug discovery and development. As a result, this study was conducted to investigate the in vitro anti-diabetic potential of aqueous acetone Helichrysum petiolare and B.L Burtt extract (AAHPE) using a 2-NBDG, 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-2-deoxy-d-glucose uptake assay. In addition, we performed molecular docking of the flavonoid constituents identified and quantified by liquid chromatography-mass spectrometry (LC-MS) from AAHPE with the potential to serve as effective and safe α-amylase and α-glucosidase inhibitors, which are important in drug discovery and development. The results showed that AAHPE is a potential inhibitor of both α-amylase and α-glucosidase, with IC50 values of 46.50 ± 6.17 (µg/mL) and 37.81 ± 5.15 (µg/mL), respectively. This is demonstrated by a significant increase in the glucose uptake activity percentage in a concentration-dependent manner compared to the control, with the highest AAHPE concentration of 75 µg/mL of glucose uptake activity being higher than metformin, a standard anti-diabetic drug, in the insulin-resistant HepG2 cell line. The molecular docking results displayed that the constituents strongly bind α-amylase and α-glucosidase while achieving better binding affinities that ranged from ΔG = -7.2 to -9.6 kcal/mol (compared with acarbose ΔG = -6.1 kcal/mol) for α-amylase, and ΔG = -7.3 to -9.0 kcal/mol (compared with acarbose ΔG = -6.3 kcal/mol) for α-glucosidase. This study revealed the potential use of the H. petiolare plant extract and its phytochemicals, which could be explored to develop potent and safe α-amylase and α-glucosidase inhibitors to treat postprandial glycemic levels in diabetic patients.
    Matched MeSH terms: alpha-Glucosidases/chemistry
  17. 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: alpha-Glucosidases/metabolism
  18. Trang NTH, Tang DYY, Chew KW, Linh NT, Hoang LT, Cuong NT, et al.
    Mol Biotechnol, 2021 Nov;63(11):1004-1015.
    PMID: 34185249 DOI: 10.1007/s12033-021-00362-3
    Various studies showed that the suppression of α-glucosidase activity can impede the glucose absorption in our body, and therefore, it can be used to treat type 2 diabetes. Hence, the compounds with anti-α-glucosidase have gained considerable attention because of their potential application in diabetes treatment. In previous literature studies, these anti-α-glucosidase compounds were extracted from plants and fungus. Less studies are being conducted to identify the anti-α-glucosidase compounds in the microbial community. In this study, 23 marine bacterial strains were screened for their potential to suppress the α-glucosidase activity. The highest inhibitory activity was exhibited by isolated L06 which was identified as Oceanimonas smirnovii EBL6. The cultivation conditions, such as temperature and pH, were optimized to increase the production of α-glucosidase inhibitors by Oceanimonas smirnovii EBL6 strain. The result findings showed that the highest yield of α-glucosidase inhibitors can be obtained at the culture time of 120 h, fermentation temperature of 30 °C, and pH 4.6. Under these conditions, the inhibitory activity of α-glucosidase can reach 81%. The IC50 of n-butanol extract was 13.89 μg/ml, while standard acarbose was 31.16 μg/ml. Overall, these findings suggest that Oceanimonas smirnovii produces α-glucosidase inhibitors and could been applied in the biochemical and medicinal fields in the future.
    Matched MeSH terms: alpha-Glucosidases/metabolism; alpha-Glucosidases/chemistry*
  19. 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: alpha-Glucosidases/metabolism*
  20. Ado MA, Maulidiani M, Ismail IS, Ghazali HM, Shaari K, Abas F
    Nat Prod Res, 2021 Sep;35(17):2992-2996.
    PMID: 31631709 DOI: 10.1080/14786419.2019.1679138
    Phytochemical investigation on the soluble fractions of n-hexane and dichloromethane of methanolic leaves extract of the Callicarpa maingayi K. & G. led to the isolation of three triterpenoids [euscaphic acid (1), arjunic acid (2), and ursolic acid (3)] together with two flavones [apigenin (4) and acacetin (5)], two phytosterols [stigmasterol 3-O-β-glycopyranoside (6) and sitosterol 3-O-β-glycopyranoside (7)], and a fatty acid [n-hexacosanoic acid (8)]. Six (6) compounds (1, 2, 3, 4, 5, and 8) are reported for the first time from this species. Their structures were elucidated and identified by extensive NMR techniques, GC-MS and comparison with the previously reported literature. Compound 3 was found to displayed good inhibition against acetylcholinesterase with an IC50 value of 21.5 ± 0.022 μM, while 1 and 2 exhibited pronounced α-glucosidase inhibitory activity with IC50 values of 22.4 ± 0.016 μM and 24.9 ± 0.012 μM, respectively.
    Matched MeSH terms: alpha-Glucosidases
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