scholarly journals Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives

2018 ◽  
Vol 27 (1) ◽  
pp. 100-108
Author(s):  
Hassan ALi ◽  
Mohammed H. Mohammed ◽  
Sajida H. Ismeal
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Phthalic Anhydride ◽  
Inhibitory Activity ◽  
Functional Group ◽  
Aliphatic Amine ◽  
Inhibition Activity ◽  
End Products ◽  
Ic50 Values ◽  
Carboxyl Functional Group ◽  
Alpha Glucosidase

 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as the end products (5a-j) while  the compounds (5k-o) required further reaction to deprotect aliphatic amine this achieved by treating the compounds with TFA to remove tert-Butoxycarbonyl group (6a-e). The alpha glucosidase inhibitory activity of some synthesized compounds (5a, 5f, 6a) were tested by using  -glucosidase from Saccharomyces cerevisiae, p-nitrophenol glucopyranoside (pNPG)  used as substrate and acarbose used as standard. All these test compounds shows   excellent inhibitory activity according to IC50 values which is ranging from (4.61-7.32).

scholarly journals ALPHA AMYLASE AND ALPHA GLUCOSIDASE INHIBITION ACTIVITY OF SELECTED EDIBLE SEAWEEDS FROM SOUTH COAST AREA OF INDIA

2017 ◽  
Vol 9 (6) ◽  
pp. 64 ◽  
Author(s):  
P. Reka ◽  
Thahira Banu A. ◽  
M. Seethalakshmi
Keyword(s):  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Alpha Amylase ◽  
Postprandial Blood Glucose ◽  
Inhibition Activity ◽  
Gracilaria Edulis ◽  
Edible Seaweeds ◽  
Daily Diet ◽  
Postprandial Blood Glucose Level ◽  
Alpha Glucosidase

Objective: The present work was to investigate the alpha amylase and alpha-glucosidase inhibitory activity of the selected edible seaweeds.Methods: The seaweeds namely Acanthophora spicifera, Gracilaria corticata, Gracilaria edulis, Ulva lactuca and Ulva reticulata were selected for this study. Six and eight hours of ethanol and aqueous extract were used for the estimation of alpha amylase using DNS method and alpha-glucosidase inhibition activity.Results: The study reported that the solvent from ethanol and aqueous in eight hours of extraction showed a higher inhibitory activity than six hours of extraction. Maximum of 89.1±0.96 and 79.55±3.08 percent of alpha-amylase and alpha-glucosidase inhibition activity were detected in the eight hours of aqueous extract (0.5 ml) of Ulva reticulata and Gracilaria edulis respectively. All the selected edible seaweeds had significant differences (p<0.05) in alpha amylase and alpha glucosidase inhibition activity between the selected seaweeds with different extracts.Conclusion: It was concluded that all the selected edible seaweeds have the potential to act as a potent inhibitor of the carbohydrate hydrolyzing enzyme. Thus, it was clear from the study that seaweeds incorporated in small amounts in the dishes consumed in the daily diet can bring a control on postprandial blood glucose level.

scholarly journals IN VITRO ALPHA-GLUCOSIDASE INHIBITORY ACTIVITY OF EGYPTIAN PLANT EXTRACTS AS AN INDICATION FOR THEIR ANTIDIABETIC ACTIVITY

2018 ◽  
Vol 11 (7) ◽  
pp. 360 ◽  
Author(s):  
May A El-manawaty ◽  
Lamiaa Gohar
Keyword(s):  
Plant Extracts ◽  
Inhibitory Activity ◽  
The Body ◽  
Antidiabetic Activity ◽  
Pinus Roxburghii ◽  
Systematic Screening ◽  
Ic50 Values ◽  
Rich Flora ◽  
Alpha Glucosidase

Objective: Diabetes mellitus is a highly prevalent chronic disease in Egypt leading to high socioeconomic problems, especially in the cities due to the unhealthy life style. Although many drugs are available, they have many side effects. Furthermore, the body arouses resistance after a while for the drug so it should be changed every once in a while. Plants could be a good source for drugs. In Egypt, we have a rich flora which has not been subjected to systematic screening for antidiabetic activity.Methods: The aim of this work was to screen 264 plant extracts for their in vitro α-glucosidase inhibitory activity. Those extracts which gave more than 70% inhibition were screened on different concentrations and their inhibitory concentrations giving 50% activity (IC50) were calculated.Results: Out of all the tested extracts, 63 gave more than or equal 70% inhibition on α-glucosidase at the tested concentration (25 ppm). After the calculation of the IC50 values, 10 extracts were chosen for further study having 5 ppm and less IC50.Conclusion: The most active plant extract is Pinus roxburghii Sarg. branches (IC50 is 2.47 ppm).

scholarly journals ALPHA-GLUCOSIDASE INHIBITORY LIMONOIDS FROM THE LEAVES OF AZADIRACHTA INDICA A. JUSS GROWN IN NINH THUAN PROVINCE

2011 ◽  
Vol 14 (2) ◽  
pp. 36-42
Author(s):  
Nhi Thi Y Nguyen ◽  
Qui Kim Tran ◽  
Quan Le Tran
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Azadirachta Indica ◽  
Spectroscopic Methods ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Alpha Glucosidase

Two new limonoids, named nimbandiol A (1) and azadirachtolid E (2) were isolated from the leaves of Azadirachta indica, along with deoxyazadirachtolid (3), a known compound. Their structures were determined by spectroscopic methods and compared with literatures. Three compounds (1-3) showed moderate a-glucosidase inhibitory activities against Saccharomyces cerevisiae a-glucosidase with IC50 values of 38.7 mM, 85.76 mM and 48.24 mM, respectively.

scholarly journals Alpha-Glucosidase and Alpha-Amylase Inhibitory Activities, Molecular Docking, and Antioxidant Capacities of Salvia aurita Constituents

Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1149
Author(s):  
Ninon G. E. R. Etsassala ◽  
Jelili A. Badmus ◽  
Jeanine L. Marnewick ◽  
Emmanuel I. Iwuoha ◽  
Felix Nchu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Antidiabetic Drugs ◽  
Alpha Amylase ◽  
Ic50 Values ◽  
Trolox Equivalent ◽  
Inhibitory Activities ◽  
Abietane Diterpenes ◽  
Alpha Glucosidase

Diabetes mellitus (DM) is one of the most dangerous metabolic diseases with a high rate of mortality worldwide. It is well known that insulin resistance and deficiency in insulin production from pancreatic β-cells are the main characteristics of DM. Due to the detrimental side effects of the current treatment, there is a considerable need to develop new effective antidiabetic drugs, especially alpha-glucosidase and alpha-amylase inhibitors with lesser adverse effects. These inhibitors are known to be directly involved in the delay of carbohydrate digestion, resulting in a reduction of glucose absorption rate and, consequently, reducing the postprandial rise of plasma glucose, which can reduce the risk of long-term diabetes complications. Furthermore, natural products are well-known sources for the discovery of new bioactive compounds that can serve as scaffolds for drug discovery, including that of new antidiabetic drugs. The phytochemical investigation of Salvia aurita collected from Hogobach Pass, Eastern Cape Province, South Africa (SA), yielded four known abietane diterpenes namely carnosol (1), rosmanol (2), 7-methoxyrosmanol (3), 12-methoxycarnosic acid (4), and one flavonoid named 4,7-dimethylapigenin (5). Structural characterization of these isolated compounds was conducted using 1 and 2D NMR, in comparison with reported spectroscopic data. These compounds are reported for the first time from S. aurita. The biological evaluation of the isolated compound against alpha-glucosidase exhibited strong inhibitory activities for 3 and 2 with the half maximal inhibitory concentration (IC50) values of 4.2 ± 0.7 and 16.4 ± 1.1 µg/mL respectively, while 4 and 1 demonstrated strong alpha-amylase inhibitory activity amongst the isolated compounds with IC50 values of 16.2 ± 0.3 and 19.8 ± 1.4 µg/mL. Molecular docking analysis confirms the strong inhibitory activity of 3 against alpha-glucosidase. Additionally, excellent antioxidant capacities were displayed by 2, 1, and 3, respectively, with oxygen radical absorbance capacity (ORAC) (25.79 ± 0.01; 23.96 ± 0.01; 23.94 ± 0.02) mM Trolox equivalent (TE)/g; 1 and 2 as ferric-ion reducing antioxidant power (FRAP) (3.92 ± 0.002; 1.52 ± 0.002) mM ascorbic acid equivalent (AAE)/g; 5 and 2 as Trolox equivalent absorbance capacity (TEAC) (3.19 ± 0.003; 2.06 ± 0.003) mM TE/g. The methanolic extract of S. aurita is a rich source of abietane diterpenes with excellent antioxidant and antidiabetic activities that can be useful to modulate oxidative stress and might possibly be excellent candidates for the management of diabetes. This is the first scientific report on the phytochemical isolation and biological evaluation of the alpha-glucosidase and alpha-amylase inhibitory activities of Salvia aurita.

scholarly journals Phytochemical screening and in vitro evaluation of alpha amylase, alpha glucosidase and beta galactosidase inhibition by aqueous and organic Atractylis gummifera L. extracts

2018 ◽  
Vol 5 (3) ◽  
pp. 103-112 ◽  
Author(s):  
Khadija Bouabid ◽  
Fatima Lamchouri ◽  
Hamid Toufik ◽  
Karima Sayah ◽  
Yahia Cherrah ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Alpha Amylase ◽  
Phytochemical Screening ◽  
Phytochemical Study ◽  
Organic Extracts ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Alpha Glucosidase ◽  
Beta Galactosidase

Diabetes is a chronic condition which is increasingly progressing throughout the world. To treat it, several methods are used, among which is medicinal plants that still have an unknown mechanism of action. The objective of this work is to evaluate the in vitro hypoglycemic effect of the extracts of the underground part of Atractylis gummifera, a member of Asteraceae used in traditional Moroccan medicine. A phytochemical study of the aqueous extracts (decocted, infused and macerated) and organic extracts (methanol, methanol macerate, chloroformic, ethyl acetate and petroleum ether), and a phytochemical screening of the different secondary metabolites was done. The antidiabetic power of the extracts of A. gummifera by testing the inhibitory activity of ?-amylase, ?-glucosidase and ?-galactosidase, which are enzymes responsible for the digestion of polysaccharides was determined. The extracts of A. gummifera are very rich in flavonoids and tannins, and are inhibitory to?-amylase and ?-glucosidase, mainly the macerate of methanol with IC50 values of 0.557 ± 0.013 and 0.743 ± 0.017 mg / mL respectively. Higher ?-galactosidase inhibitory potential than quercetin was observed for aqueous macerates and methanol with IC50 values of 2.23 ± 0.012 and 2.443 ± 0.071 mg / mL respectively. The extracts of A. gummifera possess a significant inhibitory activity of the alpha amylase and alpha glucosidase and beta-galactosidase enzymes, in particular the macerate of methanol followed by the aqueous macerate, among the eight extracts tested.

scholarly journals In vitro α-glucosidase inhibitory activity of compounds isolated from mangrove Lumnitzera littorea leaves

2019 ◽  
Vol 22 (1) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Thuy Thi Pham ◽  
Poul Erik Hansen ◽  
Phung Kim Phi Nguyen
Keyword(s):  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Mangrove Forest ◽  
2D Nmr ◽  
Positive Control ◽  
Spectroscopic Methods ◽  
Corosolic Acid ◽  
Ic50 Values ◽  
Alpha Glucosidase

Introduction: Lumnitzera littorea grown at CanGio Mangrove Forest has been investigated. The present study reports the isolation, characterization and evaluation of the alpha-glucosidase inhibitory activity of isolated compounds from Lumnitzera littorea leaves. Methods: Their structures were elucidated by spectroscopic methods (including MS, 1D and 2D–NMR) and comparison with values from the literature. From the n-hexane extract, nine compounds including lupeol (1), betulin (2), betulinic acid (3), oleanolic acid (4), corosolic acid (5), -sitosterol (6), beta-sitosterol 3-O- beta-D-glucopyranoside (7), stigmast-5-ene-3beta-O-(6-O-hexadecanoyl-beta-D-glucopyranoside) (8), and stigmast-4-ene-3-one (9) were isolated and identified. Results: The results of the alpha-glucosidase inhibitory activity showed thatcorosolic acid (5) and oleanolic acid (4) were the most potent, with IC50 values of 17.86 +/- 0.42 and 18.82 +/- 0.59 ug/mL, respectively. Five of the other seven compounds exhibited inhibitory activity with IC50 values below 100 ug/mL, and higher than the positive control acarbose (127.64 +/- 0.64 ug/mL).  

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

Inhibition of methanogenic activity of starch-degrading granules by aromatic pollutants

1997 ◽  
Vol 35 (8) ◽  
pp. 247-253 ◽  
Author(s):  
Herbert H. P. Fang ◽  
Ivan W. C. Lau ◽  
Denis W. C. Chung
Keyword(s):  
Chemical Industry ◽  
Functional Group ◽  
Anaerobic Treatment ◽  
Upflow Anaerobic Sludge Blanket ◽  
Uasb Reactor ◽  
Anaerobic Sludge ◽  
Aromatic Pollutants ◽  
Methanogenic Activity ◽  
Phenolic Pollutants ◽  
Ic50 Values

The effects of nine common aromatic pollutants from chemical industry on the bioactivity of anaerobic granules were examined. The granules were obtained from an upflow anaerobic sludge blanket (UASB) reactor treating wastewater containing colloidal starch. The specific methanogenic activities (SMA) of granules were measured at 37°C in serum vials using 3000 mg/l of colloidal starch as substrate, plus individual pollutants at various concentrations. The toxicity was expressed by the IR50 and IC50 values, i.e. the toxicant/biomass ratio and concentration at which levels the granules exhibited only 50% of their original bioactivities. Results showed that in general the granules exhibited mild resistance to toxicity of aromatic pollutants, probably due to the granules' layered microstructure. The toxicities, which were dependent on the nature of chemical functional group, of the aromatic pollutants were in the following descending order: cresols &gt; phenol &gt; hydroxyphenols/phthalate &gt; benzoate. There was only marginal difference between the toxicity of the steric isomers. For the seven phenolic pollutants, the more hydrophobic the functional group the higher the toxicity. The granules' resistance to toxicity suggested the plausibility of anaerobic treatment of wastewater from the chemical industry.

scholarly journals Fine-Tuning the Biological Profile of Multitarget Mitochondriotropic Antioxidants for Neurodegenerative Diseases

Antioxidants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 329
Author(s):  
Daniel Chavarria ◽  
Ophelie Da Silva ◽  
Sofia Benfeito ◽  
Sandra Barreiro ◽  
Jorge Garrido ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Antioxidant Properties ◽  
Neuroblastoma Cells ◽  
Oxidation Potential ◽  
Fine Tuning ◽  
Mitochondrial Oxidative Stress ◽  
Electric Eel ◽  
Ic50 Values ◽  
System Extension ◽  
Inhibition Potency

Neurotransmitter depletion and mitochondrial dysfunction are among the multiple pathological events that lead to neurodegeneration. Following our previous studies related with the development of multitarget mitochondriotropic antioxidants, this study aims to evaluate whether the π-system extension on the chemical scaffolds of AntiOXCIN2 and AntiOXCIN3 affects their bioactivity and safety profiles. After the synthesis of four triphenylphosphonium (TPP+) conjugates (compounds 2–5), we evaluated their antioxidant properties and their effect on neurotransmitter-metabolizing enzymes. All compounds were potent equine butyrylcholinesterase (eqBChE) and moderate electric eel acetylcholinesterase (eeAChE) inhibitors, with catechols 4 and 5 presenting lower IC50 values than AntiOXCIN2 and AntiOXCIN3, respectively. However, differences in the inhibition potency and selectivity of compounds 2–5 towards non-human and human cholinesterases (ChEs) were observed. Co-crystallization studies with compounds 2–5 in complex with human ChEs (hChEs) showed that these compounds exhibit different binging modes to hAChE and hBChE. Unlike AntiOXCINs, compounds 2–5 displayed moderate human monoamine oxidase (hMAO) inhibitory activity. Moreover, compounds 4 and 5 presented higher ORAC-FL indexes and lower oxidation potential values than the corresponding AntiOXCINs. Catechols 4 and 5 exhibited broader safety windows in differentiated neuroblastoma cells than benzodioxole derivatives 2 and 3. Compound 4 is highlighted as a safe mitochondria-targeted antioxidant with dual ChE/MAO inhibitory activity. Overall, this work is a contribution for the development of dual therapeutic agents addressing both mitochondrial oxidative stress and neurotransmitter depletion.

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