scholarly journals GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4183
Author(s):  
Dasha Mihaylova ◽  
Ivelina Desseva ◽  
Aneta Popova ◽  
Ivayla Dincheva ◽  
Radka Vrancheva ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Amylase Activity ◽  
Principal Component ◽  
Hierarchical Cluster ◽  
New Approach ◽  
Natural Agents ◽  
Patients With Diabetes ◽  
Inhibitory Activities ◽  
Inhibitory Potential

The inhibition of certain digestive enzymes by target food matrices represents a new approach in the treatment of socially significant diseases. Proving the ability of fruits to inhibit such enzymes can support the inclusion of specific varieties in the daily diets of patients with diabetes, obesity, Alzheimer’s disease, etc., providing them with much more than just valuable micro- and macromolecules. The current study aimed atidentifying and comparing the GC-MS metabolic profiles of eight peach varieties (“Filina”, “Ufo 4, “Gergana”, “Laskava”, “July Lady”, “Flat Queen”, “Evmolpiya”, and “Morsiani 90”) grown in Bulgaria (local and introduced) and to evaluate the inhibitory potential of their extracts towards α-glucosidase, α-amylase, lipase, and acetylcholinesterase. In order to confirm samples’ differences or similarities, principal component analysis (PCA) and hierarchical cluster analysis (HCA) were also applied to the identified metabolites. The results provide important insights into the metabolomic profiles of the eight peach varieties and represent a first attempt to characterize the peels of the peach varieties with respect to α-glucosidase-, α-amylase-, lipase-, and acetylcholinesterase-inhibitory activities. All of the studied peach extracts displayed inhibitory activity towards α-glucosidase (IC50: 125–757 mg/mL) and acetylcholinesterase (IC50: 60–739 mg/mL), but none of them affected α-amylase activity. Five of the eight varieties showed inhibitory activity towards porcine pancreatic lipase (IC50: 24–167 mg/mL). The obtained results validate the usefulness of peaches and nectarines as valuable sources of natural agents beneficial for human health, although further detailed investigation should be performed in order to thoroughly identify the enzyme inhibitors responsible for each activity.

scholarly journals Natural plant enzyme inhibitors. Characterization of an unusual α-amylase/trypsin inhibitor from ragi (Eleusine coracana Geartn.)

1981 ◽  
Vol 193 (1) ◽  
pp. 29-36 ◽  
Author(s):  
B Shivaraj ◽  
T N Pattabiraman
Keyword(s):  
Trypsin Inhibitor ◽  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Complete Recovery ◽  
Alpha Amylase ◽  
Protein Factor ◽  
Wide Ph Range ◽  
Arginine Residues ◽  
Inhibitory Activities ◽  
Antitryptic Activity

An inhibitor I-1, capable of acting on both alpha-amylase and trypsin, was purified to homogeneity from ragi (finger-millet) grains. The factor was found to be stable to heat treatment at 100 degrees C for 1 h in the presence of NaCl and also was stable over the wide pH range 1-10. Pepsin and Pronase treatment of inhibitor I-1 resulted in gradual loss of both the inhibitory activities. Formation of trypsin-inhibitor I-1 complex, amylase-inhibitor I-1 complex and trypsin-inhibitor I-1-amylase trimer complex was demonstrated by chromatography on a Bio-Gel P-200 column. This indicated that the inhibitor is ‘double-headed’ in nature. The inhibitor was retained on a trypsin-Sepharose 4B column at pH 7.0. Elution at acidic pH resulted in almost complete recovery of amylase-inhibitory and trypsin-inhibitory activities. alpha-Amylase was retained on a trypsin-Sepharose column to which inhibitor I-1 was bound, but not on trypsin-Sepharose alone. Modification of amino groups of the inhibitor with 2,4,6-trinitrobenzenesulphonic acid resulted in complete loss of amylase-inhibitory activity but only 40% loss in antitryptic activity. Modification of arginine residues by cyclohexane-1,2-dione led to 85% loss of antitryptic activity after 5 h, but no effect on amylase-inhibitory activity. The results show that a single bifunctional protein factor is responsible for both amylase-inhibitory and trypsin-inhibitory activities with two different reactive sites.

scholarly journals Evaluation of Xanthine Oxidase Inhibitory Activities in vitro of Gomphrena CelosiodesMart

2017 ◽  
Vol 33 (2) ◽  
Author(s):  
Dang Kim Thu ◽  
Vu Thi Hoa ◽  
Chu Ngoc Khanh ◽  
Bui Thanh Tung
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Final Stage ◽  
Enzyme Inhibitors ◽  
The Body ◽  
Prevention And Treatment ◽  
Etoac Fraction ◽  
Inhibitory Activities

Xanthine oxidase (XO) is an enzyme that has an improtant role in the synthesis of uric acid. XO is an enzyme allowscatalyzing the hydroxylation of hypoxanthine to xanthine and xanthine to uric acid. These are two reactions in the final stage of metabolism of the purines in the body. Offal, XO enzyme inhibitors reduce biosynthesis of uric acid have been used to prevent and treat gout. In this study, Gompherena celosiodes is extracted by ultrasonic with ethanol 80 % (EtOH)solvents and fractionated with n-hexane, ethyl acetate (EtOAc) and n-butanol (n-BuOH) solvents. These fractions were evaluated xanthine oxidase inhibitory activities in vitro. The results show that n-BuOH fraction from roots bark had the strongest XO enzyme inhibitory activity (IC50: 27,39 ± 0,31µg/mL), followed by EtOH fraction (IC50: 47,37 ± 0,26 µg/mL) and EtOAc fraction (IC50: 33,36 ± 0,51µg/mL) and the lowest is n-hexan fraction (IC50: 81,59 ± 0,21µg/mL). The research results indicated that the n-BuOH fraction and the EtOAc fraction from tree-hatched soil have a potential in the prevention and treatment of gout.

scholarly journals Dalbergia ecastaphyllum leaf extracts: in vitro inhibitory potential against enzymes related to metabolic syndrome, inflammation and neurodegenerative diseases

2019 ◽  
Vol 41 ◽  
pp. e46622
Author(s):  
Daniel Vieira de Morais ◽  
Manuela Maria Moreira ◽  
Fabiane de Lima Silva ◽  
Maria Angélica Pereira de Carvalho Costa ◽  
Cristina Delerue-Mato ◽  
...  
Keyword(s):  
Hemolytic Activity ◽  
Inhibitory Activity ◽  
High Performance ◽  
Leaf Extracts ◽  
Photodiode Array Detection ◽  
Photodiode Array ◽  
Array Detection ◽  
Inhibitory Activities ◽  
Inhibitory Potential

For the first time, the anti-hemolytic activity and the enzyme inhibitory activities of Dalbergia ecastaphyllum leaves extracts were tested against α-amylase, α-glucosidase, lipase, acetylcholinesterase, butyrylcholinesterase, tyrosinase and hyaluronidase. The phenolic profile of the obtained extracts was also investigated by high-performance liquid chromatography with photodiode array detection (HPLC-PAD). The extracts showed inhibitory activity against all enzymes evaluated, with the highest inhibitory activity reported for the enzyme hyaluronidase (28.28 ± 2.43 to 72.19 ± 1.40 μg mL-1). The obtained extracts also demonstrate anti-hemolytic activity (52.22 ± 1.62 to 71.17 ± 1.82%). Among the phenolic compounds identified, protocatechuic, vanillic and β-resorcylic acids were the most abundant (1.13 ± 0.06 to 2.53 ± 0.06, 0.90 ± 0.06 to 2.19 ± 0.06 and 1.03 ± 1.62 to 22.11 ± 1.62 mg L-1, respectively). In the statistical analysis, a significant correlation was found between the flavonoids content and all enzymes inhibitory activities. The present study showed that D. ecastaphyllum leaves extracts may have the potential to be used in the therapeutic treatment of several diseases such as Alzheimer, Parkinson, type 2 diabetes mellitus, hyperglycemia, and pigmentation, as well as those associated with oxidative stress.

scholarly journals A New Approach for Provenance Studies of Archaeological Finds: Inferences from Trace Elements in Carbonate Minerals of Alpine White Marbles by a Bench-to-Top μ-XRF Spectrometer

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Gloria Vaggelli ◽  
Margherita Serra ◽  
Roberto Cossio ◽  
Alessandro Borghi
Keyword(s):  
Principal Component ◽  
Hierarchical Cluster ◽  
Western Alps ◽  
Metamorphic Rocks ◽  
Carbonate Minerals ◽  
Data Set ◽  
New Approach ◽  
Provenance Studies ◽  
Individual Observation ◽  
Geological Units

The metamorphic rocks outcropping in the Western Alps are characterised by a great variety of white marbles which have been used since the antiquity. This variety mostly includes nine historical Piedmont white marbles (Ornavasso, Candoglia, Crevola, Pont Canavese, Foresto, Chianocco, Prali, Brossasco, and Garessio marbles) coming from well-known quarry sites and belonging to different metamorphic geological units of the Western Alps. The petrographical, minerochemical, and C–O isotopic data of these white marbles have been integrated with CaO and trace element (Fe, Mn, and Sr) concentration determined on single crystals of carbonate minerals (i.e., calcite and/or dolomite) by means of a bench-to-top µ-XRF spectrometer. Principal component analysis and hierarchical cluster analysis were performed on a data set of 178 observations containing CaO, Fe, Mn, and Sr concentration as well as the maximum grain size (MGS), δ18O and δ13C. The use of only five selected variables (CaO, Fe, Mn, Sr, and δ18O) has provided the correct allocation of each individual observation to its relevant class. Therefore, this approach based mostly on a noninvasive µ-XRF determination will be useful to define the provenance of unknown marbles of alpine origin used in antiquity for cultural heritage.

2,4-Dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic Acid Derivatives: In Vitro Antidiabetic Activity, Molecular Modeling and In silico ADMET Screening

2019 ◽  
Vol 15 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Samridhi Thakral ◽  
Vikramjeet Singh
Keyword(s):  
Molecular Docking ◽  
Benzoic Acid ◽  
Inhibitory Activity ◽  
In Silico ◽  
Computational Study ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Benzoic Acid Derivatives ◽  
In Silico Admet ◽  
Inhibitory Potential

Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl] benzoic acid derivatives and evaluate α-glucosidase and α-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential α-glucosidase and α-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-dichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against α-amylase and 5 times inhibitory activity against α-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against α-glucosidase and α-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.

Screening of Actinomycetes For α-amylase Inhibitors Production

2019 ◽  
Vol 15 (1) ◽  
pp. 41-45
Author(s):  
Shivabai Chandwad ◽  
Sudhakar Gutte
Keyword(s):  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Spectroscopic Method ◽  
Solid Material ◽  
Soil Samples ◽  
Assay Method ◽  
Novel Drugs ◽  
Pre Treatment ◽  
Diabetic Treatment ◽  
Amylase Inhibitors

Background:Diabetes mellitus is the most common and fastest growing disease in the world. One of the therapies to treat diabetes is the inhibition of α-amylase activity by inhibitors from microbial and plant source. Actinomycetes are potential sources of enzyme inhibitors, drugs, amino acids, vitamins etc.Objective:Our work mainly highlights the isolation of actinomycetes from soil samples of different habitats and screening of α -amylase inhibitors.Methods:Actinomycetes were isolated from soil samples of different habitats by different methods; these include a variety of pre-treatment of soil samples in combination with an appropriate supplement medium with selective antibacterial agents. Isolated actinomycetes grown in fermentation condition and metabolites were extracted with Isopropyl alcohol and concentrated to obtain solid material. The extract of each isolate was tested for α -amylase inhibition using starch Iodine plate method and DNS- spectroscopic method.Results:Total 110 actinomycetes strains were isolated from various sources. Among 110 extracts of actinomycetes, eight extracts have shown positive results for α-amylase inhibition in starch Iodine plate assay method. Extracts selected from primary results were used for the confirmation of inhibitory activity using DNS- spectroscopic method. Out of eight extracts, six extracts showed Porcine pancreatic α -amylase inhibitory activity ranging from 40-86%. The actinomycetes strains that produce α -amylase inhibitory activity are A-24, A-29, B-5, B-18, C-15 and D-24.Conclusion:These results show that actinomycetes are a potential source for α -amylase inhibitors, which may lead to valuable novel drugs for diabetic treatment.

Quality evaluation of tugaksheeree samples by ATR-FTIR spectroscopy using multicomponent analysis

2020 ◽  
Vol 10 ◽  
Author(s):  
Nikunj D. Patel ◽  
Niranjan S. Kanaki
Keyword(s):  
Principal Component Analysis ◽  
Cluster Analysis ◽  
Quality Evaluation ◽  
Principal Component ◽  
Hierarchical Cluster ◽  
Attenuated Total Reflectance ◽  
Chemometric Methods ◽  
Total Reflectance ◽  
Fingerprint Region ◽  
Ftir Technique

Background: Numerous Ayurvedic formulations contains tugaksheeree as key ingredient. Tugaksheereeis the starch gained from the rhizomes of two plants, Curcuma angustifoliaRoxb. (Zingiberaceae) and Marantaarundinacea (MA) Linn. (Marantaceae). Objective: The primary concerns in quality assessment of Tugaksheeree occur due to adulteration or substitution. Method: In current study, Fourier transform infrared (FTIR) technique with attenuated total reflectance (ATR) facility was used to evaluate tugaksheeree samples. Total 10 different samples were studied and transmittance mode was kept to record the spectra devoid of pellets of KBR. Further treatment was given with multi component tools by considering fingerprint region of the spectra. Multivariate analysis was performed by various chemometric methods. Result: Multi component methods like Principal Component Analysis (PCA), and Hierarchical Cluster Analysis (HCA)were used to discriminate the tugaksheeree samples using Minitab software. Conclusion: This method can be used as a tool to differentiate samples of tugaksheeree from its adulterants and substitutes.

scholarly journals Structural Characterization and Assessment of Anti-Inflammatory and Anti-Tyrosinase Activities of Polyphenols from Melastoma normale

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3913
Author(s):  
Rui-Jie He ◽  
Jun Li ◽  
Yong-Lin Huang ◽  
Ya-Feng Wang ◽  
Bing-Yuan Yang ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Enzyme Inhibitor ◽  
Structure Identification ◽  
No Production ◽  
Protective Effects ◽  
Successful Isolation ◽  
Ic50 Values ◽  
Development And Utilization ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Polyphenols, widely distributed in the genus Melastoma plants, possess extensive cellular protective effects such as anti-inflammatory, anti-tyrosinase, and anti-obesity, which makes it a potential anti-inflammatory drug or enzyme inhibitor. Therefore, the aim of this study is to screen for the anti-inflammatory and enzyme inhibitory activities of compounds from title plant. Using silica gel, MCI, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, the extract of Melastoma normale roots was separated. Four new ellagitannins, Whiskey tannin C (1), 1-O-(4-methoxygalloyl)-6-O-galloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (2), 1-O-galloyl-6-O-(3-methoxygalloyl)-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (3), and 1-O-galloyl-6-O-vanilloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (4), along with eight known polyphenols were firstly obtained from this plant. The structures of all isolates were elucidated by HRMS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW2 64.7 cells, we investigated the anti-inflammatory activities of compounds 1–4, unfortunately, none of them exhibit inhibit nitric oxide (NO) production, their IC50 values are all > 50 μM. Anti-tyrosinase activity assays was done by tyrosinase inhibition activity screening model. Compound 1 showed weak tyrosinase inhibitory activity with IC50 values of 426.02 ± 11.31 μM. Compounds 2–4 displayed moderate tyrosinase inhibitory activities with IC50 values in the range of 124.74 ± 3.12–241.41 ± 6.23 μM. The structure–activity relationships indicate that hydroxylation at C-3′, C-4′, and C-3 in the flavones were key to their anti-tyrosinase activities. The successful isolation and structure identification of ellagitannin provide materials for the screening of anti-inflammatory drugs and enzyme inhibitors, and also contribute to the development and utilization of M. normale.

scholarly journals Multivariate Statistical Approach for Nephrines in Women with Obesity

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1393
Author(s):  
Ralitsa Robeva ◽  
Miroslava Nedyalkova ◽  
Georgi Kirilov ◽  
Atanaska Elenkova ◽  
Sabina Zacharieva ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Metabolic Syndrome ◽  
Data Analysis ◽  
Stress Response ◽  
Exploratory Data Analysis ◽  
Principal Component ◽  
Hierarchical Cluster ◽  
Obese Women ◽  
Exploratory Data

Catecholamines are physiological regulators of carbohydrate and lipid metabolism during stress, but their chronic influence on metabolic changes in obese patients is still not clarified. The present study aimed to establish the associations between the catecholamine metabolites and metabolic syndrome (MS) components in obese women as well as to reveal the possible hidden subgroups of patients through hierarchical cluster analysis and principal component analysis. The 24-h urine excretion of metanephrine and normetanephrine was investigated in 150 obese women (54 non diabetic without MS, 70 non-diabetic with MS and 26 with type 2 diabetes). The interrelations between carbohydrate disturbances, metabolic syndrome components and stress response hormones were studied. Exploratory data analysis was used to determine different patterns of similarities among the patients. Normetanephrine concentrations were significantly increased in postmenopausal patients and in women with morbid obesity, type 2 diabetes, and hypertension but not with prediabetes. Both metanephrine and normetanephrine levels were positively associated with glucose concentrations one hour after glucose load irrespectively of the insulin levels. The exploratory data analysis showed different risk subgroups among the investigated obese women. The development of predictive tools that include not only traditional metabolic risk factors, but also markers of stress response systems might help for specific risk estimation in obesity patients.

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