scholarly journals Purification, Preliminary Structural Characterization, and In Vitro Inhibitory Effect on Digestive Enzymes by β-Glucan from Qingke (Tibetan Hulless Barley)

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Jialiang Hu ◽  
Yue Wu ◽  
Huifang Xie ◽  
Wanyin Shi ◽  
Zhiyuan Chen ◽  
...  
Keyword(s):  
Column Chromatography ◽  
Structural Characterization ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Hordeum Vulgare L ◽  
Spectra Analysis ◽  
Hulless Barley ◽  
Ft Ir ◽  
Tibetan Hulless Barley

Background and Objective. Qingke (Tibetan hulless barley, Hordeum vulgare L.) contains a high content of β-glucan among all the cereal varieties. Although β-glucan has multiple physiological functions, the physiological function of qingke β-glucan was few studied. In this study, the β-glucan was isolated, purified, determined the structural characterization, and measured the inhibitory activity to enzymes correlating blood sugar and lipid. Methods. β-Glucan was isolated from enzymatic aqueous extract of qingke by using deproteinization, decolorization, DEAE-52 column chromatography, and sepharose CL-4B agarose gel column chromatography. The structure of the β-glucan was determined using FT-IR and 13C-NMR spectra analysis, and molecular mass by use of HPSEC-dRI-LS. The kinematic viscosity was measured. The inhibitory effects of this β-glucan on four enzymes were investigated. Results. This β-glucan had a uniform molecular weight of 201,000 Da with β-(1⟶4) as the main chain and β-(1⟶3) as a side chain. The β-glucan presented a relatively strong inhibitory activity on α-glucosidase, moderate inhibition on invertase, and a weak inhibition on α-amylase, whereas it did not inhibit lipase. Conclusion. The study indicates that the enzymatic β-glucan from qingke has the potential as natural auxiliary hypoglycemic additives in functional medicine or foods.

scholarly journals Development of mouthwash with Rosmarinus officinalis extract

2014 ◽  
Vol 50 (4) ◽  
pp. 851-858 ◽  
Author(s):  
Isabela Moreira Baumgratz de Paula ◽  
Flávia Costa Moraes ◽  
Orlando Vieira de Souza ◽  
Célia Hitomi Yamamoto
Keyword(s):  
Sodium Fluoride ◽  
Inhibitory Activity ◽  
Raw Materials ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Rosmarinus Officinalis ◽  
Hexane Fraction ◽  
Diffusion Method ◽  
Oral Infections

Rosmarinus officinalis, which belongs to the Lamiaceaefamily, is a species of medicinal flora with therapeutic properties. In order to exploit the benefits of these properties, a mouthwash formulation was developed, with careful selection of raw materials to meet pharmacotechnical requirements. Extracts of the plant were incorporated into a mouthwash, which was shown to have inhibitory action in vitro against the micro-organisms commonly found in periodontics. Controls for assessing the quality of the drugs were carried out, quantifying phenols and flavonoids as chemical markers. Mouthwash solutions were formulated containing 0.1, 5 and 10% ethanol extract of R. officinalis; and 0.05, 5 and 10% of the hexane fraction of R. officinalis. In order to evaluate synergism, ethanol extract and hexane fraction were also added to formulations containing 0.05% sodium fluoride and 0.12% chlorhexidine digluconate. These formulations were assessed for inhibitory effect against the specific microorganisms involved in the process of bacterial plaque formation, S. mutans(ATCC25175) and C. albicans(ATCC 10231), frequently found in cases of oral infections. The agar diffusion method was used to evaluate the inhibitory activity of extracts and formulations. All mouthwash solutions displayed inhibitory activity having higher sensitivity to S. mutansfor the 5% ethanol extract+0.05% sodium fluoride, and greater sensitivity to C. albicansfor the 10% hexane fraction. Results were characterized by the appearance of a growth inhibition halo, justifying the utilization and association of extracts of R. officinalis.

scholarly journals In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Colorimetric Assay ◽  
Hypotensive Effect ◽  
Ace Inhibition ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Total Phenolic ◽  
Before And After

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

scholarly journals Inhibition of prolyl oligopeptidase by flavonoids isolated from the roots of Allexis obanensis (Baker f.) Melch

2021 ◽  
Vol 1 (2) ◽  
pp. 39-44
Author(s):  
Olivier Ndogo Eteme ◽  
Nkwengoua Tchouboun Zondegoumba Ernestine ◽  
Soh Desire ◽  
Oladimeji Taiwo Babatunde ◽  
Barthelemy Nyasse
Keyword(s):  
Neurodegenerative Diseases ◽  
Column Chromatography ◽  
Inhibitory Activity ◽  
High Performance ◽  
High Performance Liquid Chromatographic ◽  
Chromatographic Technique ◽  
Carboxy Terminus ◽  
Prolyl Oligopeptidase ◽  
Liquid Chromatographic

Background: Prolyl oligopeptidase is a cytosolic serine peptidase that hydrolyzes peptides containing proline at the carboxy terminus of proline residues. It has been associated with several neurodegenerative diseases. Therefore, it is a target in the management of these disease conditions. Methods: Allexis obanensis was taken through cold extraction, subjected to column chromatography and flavonoids isolated via high-performance liquid chromatographic technique. The flavonoids obtained were investigated for their in vitro prolyl oligopeptidase inhibitory activity. Results: The flavonoids isolated include: 4.4'''- dimethoxylophirone A [1] and 7-hydroxy-3-(3-hydroxy-4 méthoxyphenyl)-5- méthoxy-4H chromen-4-one [2]. They inhibited prolyl oligopeptidase at low IC50 concentrations of 7.201±3.021 µM and 6.223±2.002 µM respectively. Conclusion: The results obtained from this study proves the potential of these flavonoids as prolyl oligopeptidase inhibitors, by inference, their potentiality in the management of neuropsychiatric disorders.

IN VITRO STUDIES OF SOME EDIBLE SPICES ON PANCREATIC LIPASE INHIBITORY ACTIVITY

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 62-68
Author(s):  
S Mhatre ◽  
◽  
A. Bhagit ◽  
R. P Yadav
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Syzygium Aromaticum ◽  
High Potency ◽  
Good Source ◽  
Zanthoxylum Armatum ◽  
Methanolic Extracts ◽  
Cinnamomum Tamala

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.

scholarly journals Phenolic Acids from Lycium barbarum Leaves: In Vitro and In Silico Studies of the Inhibitory Activity against Porcine Pancreatic α-Amylase

Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1388
Author(s):  
Luna Pollini ◽  
Alessandra Riccio ◽  
Cristina Juan ◽  
Carmela Tringaniello ◽  
Federica Ianni ◽  
...  
Keyword(s):  
Phenolic Acids ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Lycium Barbarum ◽  
Plant Materials ◽  
Vitro Assay ◽  
In Silico Studies

Nowadays, bioactive compounds from vegetable food and waste are of great interest for their inhibitory potential against digestive enzymes. In the present study, the inhibitory activity of methanolic extract from Lycium barbarum leaves on porcine pancreas α-amylase has been studied. The α-amylase inhibitory activity of the constituent phenolic acids was also investigated. The leaves were extracted by ultrasound-assisted method, one of the most efficient techniques for bioactive extraction from plant materials, and then the phenolic acids were identified by Accurate-Mass Quadrupole Time-of-Flight (Q-TOF) Liquid Chromatography/Mass Spectrometry (LC/MS). Chlorogenic and salicylic acids were the most abundant phenolic acids in L. barbarum leaf extract. The inhibitory effect against α-amylase, determined for individual compounds by in vitro assay, was higher for chlorogenic, salicylic, and caffeic acids. L. barbarum leaf extract showed an appreciable α-amylase inhibitory effect in a concentration-dependent manner. Docking studies of the considered phenolic acids into the active site of α-amylase suggested a conserved binding mode that is mainly stabilized through H-bonds and π-π stacking interactions.

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

2017 ◽  
Vol 41 (1) ◽  
pp. 30-35 ◽  
Author(s):  
Laleh Faraji ◽  
Shiva Shahkarami ◽  
Hamid Nadri ◽  
Alireza Moradi ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Inhibitory Effect ◽  
Ring System ◽  
Benzothiazole Derivatives ◽  
Ache Inhibitory Activity ◽  
Group A

A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.

scholarly journals Collagenase inhibition by water-pepper (Polygonum hydropiper L.) sprout extract

2019 ◽  
Vol 8 (2) ◽  
pp. 114-119 ◽  
Author(s):  
Tomoaki Kawaguchi ◽  
Kaori Nagata
Keyword(s):  
Column Chromatography ◽  
Inhibitory Activity ◽  
High Performance ◽  
Inhibitory Effect ◽  
Skin Aging ◽  
Dependent Manner ◽  
Dermal Matrix ◽  
Polygonum Hydropiper ◽  
Concentration Dependent Manner ◽  
Hplc Fraction

Introduction: Collagenase plays an important role in the degradation of dermal matrix proteins leading to wrinkle formation. The objectives of this study were to evaluate the inhibitory effect of water-pepper (Polygonum hydropiper L.) sprout extract on the activity of collagenase and to identify the inhibitory compounds.Methods: Collagenase inhibitory activity was measured by spectrophotometric assay. Activity-guided fractionation was performed using liquid-liquid extraction of water and n-butanol and Diaion HP-20 column chromatography, followed by high-performance liquid chromatography (HPLC) fraction collection.Results: A methanolic extract of water-pepper sprout inhibited collagenase activity in a concentration-dependent manner with an IC50 value of 156.7 μg/mL. Collagenase inhibitory activity (IC50 = 23.5 μg/mL) was found in 50% methanol eluate from the HP-20 column chromatography of the n-butanol soluble fraction. The active compound (IC50 = 1.9 μg/mL) in the eluate was isolated by HPLC and identified as quercetin-3-O-galactoside (hyperoside) from comparing retention time, UV-Vis absorption, and mass spectra with those of the standard. Lineweaver-Burk plots revealed that hyperoside was an uncompetitive inhibitor against collagenase. Hyperoside was also the most abundant flavonoid present in the methanolic extract.Conclusion: These results suggest that water-pepper sprouts could be beneficial as a natural source of collagenase inhibitor which might be used for the treatment of skin aging.

scholarly journals α-Glucosidase Inhibitory Activity of Phenolic Rich Extracts Obtained from the Seeds of Melastoma saigonense (Kuntze) Merr.

2019 ◽  
Vol 31 (12) ◽  
pp. 2964-2968 ◽  
Author(s):  
Nutthamon Prajudtasri ◽  
Mongkol Nontakitticharoen ◽  
Sujint Anguravirutt
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Inhibitory Effect ◽  
Total Phenolic ◽  
Phytochemical Analysis ◽  
Antidiabetic Agent ◽  
Seed Extracts

The aim of this study was to perform a phytochemical analysis of Melastoma saigonense seed extracts and to determine their α-glucosidase inhibitory activity. The extracts from seeds of M. saigonense indicated that the total phenolic content was in the range between 233.46 and 967.22 mg GAE/g DE, whereas the flavonoids content was in the range between 359.96 and 850.84 mg QE/g DE. The present study of antidiabetic inhibitory activity by in vitro α-glucosidase revealed that the crude extracts using ethyl acetate (EA), butanol (BU) and final aqueous residue extracts (AQ) exhibited a strong α-glucosidase inhibitory effect (IC50 4.42-11.95 μg/mL). The ethyl acetate and butanol extracts of seeds of Melastoma saigonense (Kuntze) Merr. were further fractionated by silica gel column chromatography into four fractions (EAF1−EAF4) and five fractions (BUF1−BUF5), respectively and their bioactivities were investigated. The nine fractions exhibited significant α-glucosidase inhibitory activity (p < 0.05) with an IC50 between 3.42-34.77 μg/mL which is less than the IC50 for standard acarbose (IC50 = 507.26 μg/mL). Among all the fractions, BUF1 and EAF1 exhibited high inhibitory activity against α-glucosidase with BUF1 showing the highest inhibitory activity (IC50 = 3.42 μg/mL). The dominant phenolic acids were sinapic, gallic, ferrulic, syringic, gallic and caffeic acids and the prominent flavonoids were myricetin and quercetin. These findings suggest that the seeds of M. saigonense have potential as a source of antidiabetic agent (s).

scholarly journals Variability of Hordeum vulgare L. Cultivars in Yield, Antioxidant Potential, and Cholinesterase Inhibitory Activity

2020 ◽  
Vol 12 (5) ◽  
pp. 1938 ◽  
Author(s):  
Joanna Kobus-Cisowska ◽  
Piotr Szulc ◽  
Oskar Szczepaniak ◽  
Marcin Dziedziński ◽  
Daria Szymanowska ◽  
...  
Keyword(s):  
Hordeum Vulgare ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Antioxidant Potential ◽  
Aqueous Extracts ◽  
Hordeum Vulgare L ◽  
Barley Cultivars ◽  
Cholinesterase Inhibitory Activity ◽  
Barley Leaves ◽  
Barley Grains

Barley (Hordeum vulgare L.) is an annual plant cultivated in spring or autumn. Currently, over 70% of the cultivated barley grains are utilized for preparing fodder, while the rest is used for the production of malt and cereals in the food industry. The purpose of the present work was to evaluate the content of bioactive compounds, antioxidant potential, and cholinesterase inhibitory effect of the aqueous extracts of juvenile barley leaves. It was found that the barley cultivars differed in their content of the determined phytochemicals as well as their antioxidant potential and cholinesterase-inhibitory activity. The water extracts of young barley leaves contained phenolic acids as well as quercetin, rutin, and kaempferitrin. The extracts showed a higher inhibitory effect on 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) than on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. Based on the aqueous extracts analyzed, we found that winter cultivars were characterized by the highest iron-chelating activity. Furthermore, barley extracts showed a stronger inhibitory effect against acetylcholinesterase compared to butyrylcholinesterase. The results of the present work indicated that barley cultivars differed in their germination process. Among the tested samples, the highest cholinesterase inhibitory activity was shown by the Basic variety.

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