scholarly journals First Identification of α-Glucosidase Inhibitors from Okra (Abelmoschus Esculentus) Seeds

2013 ◽  
Vol 8 (8) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Wannisa Thanakosai ◽  
Preecha Phuwapraisirisan
Keyword(s):  
Diabetes Mellitus ◽  
Kinetic Study ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Significant Decline ◽  
Hypoglycemic Effect ◽  
Competitive Behavior ◽  
Active Components ◽  
Glucose Residue ◽  
Glucosidase Inhibitors

Infusion of roasted okra seeds has long been consumed in Turkey for diabetes mellitus therapy. Previous reports of a hypoglycemic effect observed in rats administrated with okra seed extract indicated a possible connection with inhibition of intestinal α-glucosidase. An attempt to identify active components was first herein conducted using α-glucosidase-inhibition-guided isolation, yielding two major flavonol glucosides named isoquercetin (2) and quercetin-3- O-β-glucopyranosyl-(1″′ →6″)-glucoside (3). They selectively inhibited rat intestinal maltase and sucrase, in which isoquercetin (2) was 6–10 times more potent than its related diglucoside 3. This result suggested that an increase in hydrophilicity by the additional glucose residue in 3 led to a significant decline in the inhibitory effect and raised the possible involvement of the free 3-OH in exerting the inhibition. Our postulation was evaluated by examining α-glucosidase inhibition of quercetin (1), and the aglycone of 2 and 3, whose 3-OH is free from any glucose moiety. Interestingly, 1 displayed a broad inhibitory effect toward rat intestinal and baker's yeast α-glucosidases, with improved potency. A kinetic study of 1 indicated that it inhibited maltase by two distinct mechanisms, in competitive ( K i 462 μM) and noncompetitive ( K i 2153 μM) manners, whereas the mechanism underlying the inhibition of sucrase was verified as being of a competitive behavior ( K i 218 μM).

scholarly journals Hypoglycemic effect of katakakhadiradi kashayam by alleviating the oxidative damage in experimentally induced diabetic rats

2021 ◽  
Vol 12 (2) ◽  
pp. 1306-1310
Author(s):  
Angelie Jessica Subbiah ◽  
Kavimani M ◽  
Mukilan Ramadoss ◽  
Prabhu K
Keyword(s):  
Diabetes Mellitus ◽  
Oxidative Damage ◽  
Good Alternative ◽  
Pancreatic Tissue ◽  
Diabetic Rats ◽  
Blood Glucose Measurement ◽  
Biologically Active ◽  
Hypoglycemic Effect ◽  
Glucose Measurement ◽  
Active Components

At present, herbal plants and their biologically active components have acquired importance in diabetes mellitus (DM) management, which has spread worldwide. The current study was carried out to analyse the antidiabetic action of  Katakakhadiradi kashayam in streptozotocin administered diabetic rats. The study was done in wistar rats by inducing diabetes using streptozotocin and nicotinamide. Diabetic rats were given katakakhadiradi kashayam with various doses of 100, 200 and 300 mg/kg/b.wt for 14 days, and its efficacy was compared with glibenclamide drug. The hypoglycemic effect of this katakakhadiradi kashayam was tested by taking blood glucose measurement in experimental rats. The oxidative damage caused by streptozotocin was analysed by LPO levels and the antioxidants status was assessed by GSH levels, GPx, SOD and CAT activities in pancreatic tissues. The antidiabetic study of katakakhadiradi kashayam showed reduction in hyperglycemia by reducing the oxidative damage in pancreatic tissue and improving the antioxidants. Overall, the reports of the study showed that katakakhadiradi kashayam could be used to improve management of diabetic rats. The acquired data suggest the hypoglycemic efficacy of katakakhadiradi kashayam, which is practically a safe herbal formulation and may be used as a good alternative to cure diabetes mellitus.

scholarly journals Modes of Inhibition ofα-Amylase andα-Glucosidase by Aqueous Extract ofMorinda lucidaBenth Leaf

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
M. I. Kazeem ◽  
J. O. Adamson ◽  
I. A. Ogunwande
Keyword(s):  
Diabetes Mellitus ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Leaf Extracts ◽  
Glucosidase Inhibitors ◽  
Ethanolic Extracts ◽  
Insulin Secretagogues ◽  
Percentage Yield ◽  
Oral Hypoglycemic Drugs

Diabetes mellitus is a metabolic disorder of glucose metabolism. The management of blood glucose level is the hallmark in the treatment of this disease. This may be achieved through the use of oral hypoglycemic drugs such as biguanides, insulin secretagogues, andα-glucosidase inhibitors. The purpose of the present study was to investigate the inhibitory effect ofMorinda lucidaleaf extracts on the activities ofα-amylase andα-glucosidase. This was performed usingα-amylase fromAspergillus oryzaeandα-glucosidase fromSaccharomyces cerevisiae.Aqueous extract ofMorinda lucidagave the highest percentage yield (9.99%) of the plant out of the three extracts (compared to acetone and ethanolic extracts) and possesses the highest inhibitory activity againstα-amylase (IC50value of 2.30 mg/mL) andα-glucosidase (IC50value of 2.00 mg/mL). Kinetic analysis revealed that the aqueous extract of this plant leaf inhibited theα-amylase competitively but displayed mixed noncompetitive mode of inhibition towardsα-glucosidase. It can be concluded that aqueous extract ofMorinda lucidaexhibited the best inhibitory activity on the two enzymes studied and the presence of phytochemicals like flavonoids, saponins, and tannins may have contributed greatly to the inhibitory activity of the plant extract.

Novel coumarin containing dithiocarbamate derivatives as potent α-glucosidase inhibitors for management of type 2 diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Marjan Mollazadeh ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Yousef Valizadeh ◽  
Afsaneh Zonouzi ◽  
Mohammad Ali Faramarzi ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Kinetic Study ◽  
Active Site ◽  
Docking Study ◽  
Secondary Amines ◽  
Molecular Docking Study ◽  
Glucosidase Inhibitors ◽  
Dithiocarbamate Derivatives

Background: α-Glucosidase is a hydrolyze enzyme that plays a crucial role in degradation of carbohydrates and starch to glucose. Hence, α-glucosidase is an important target in the carbohydrate mediated diseases such as diabetes mellitus. Objective: In this study, novel coumarin containing dithiocarbamate derivatives 4a-n were synthesized and evaluated against α-glucosidase in vitro and in silico. Methods: These compounds were obtained of reaction between 4-(bromomethyl)-7-methoxy-2H-chromen-2-one 1, carbon disulfide 2, and primary or secondary amines 3a-n in the presence potassium hydroxide and ethanol at room temperature. In vitro α-glucosidase inhibition and kinetic study of these compounds were performed. Furthermore, docking study of the most potent compounds was also performed by Auto Dock Tools (version 1.5.6). Results: Obtained results showed that all the synthesized compounds exhibited prominent inhibitory activities (IC50 = 85.0 ± 4.0-566.6 ± 8.6 μM) in comparison to acarbose as standard inhibitor (IC50 = 750.0 ± 9.0 µM). Among them, secondary amine derivative 4d with pendant indole group was the most potent inhibitor. Enzyme kinetic study of the compound 4d revealed that this compound compete with substrate to connect to the active site of α-glucosidase and therefore is a competitive inhibitor. Also, molecular docking study predicted that this compound as well interacted with α-glucosidase active site pocket. Conclusion: Our results suggest that the coumarin-dithiocarbamate scaffold can be a promising lead structure for design potent α-glucosidase inhibitors for treatment of type 2 diabetes.

Modification of pea dietary fiber by ultrafine grinding and hypoglycemic effect in diabetes mellitus mice

2021 ◽  
Author(s):  
Meng Wang ◽  
Xuanhong Chen ◽  
Leichao Dong ◽  
Xijun Nan ◽  
Wei Ji ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Dietary Fiber ◽  
Hypoglycemic Effect ◽  
Ultrafine Grinding

scholarly journals Assessment of the Aromatase Inhibitory Activity of Ma-Huang-Tang (MHT) and Its Active Compounds

2019 ◽  
Vol 2019 ◽  
pp. 1-9
Author(s):  
Dong Ho Jung ◽  
Joo Tae Hwang ◽  
Bo-Jeong Pyun ◽  
Song Yi Yu ◽  
Byoung Seob Ko
Keyword(s):  
Herbal Medicines ◽  
Inhibitory Effect ◽  
Aromatase Activity ◽  
Cytochrome P450 Enzyme ◽  
Active Components ◽  
Glycyrrhizae Radix ◽  
Potent Inhibition ◽  
P450 Enzyme ◽  
Medicine Prescription ◽  
Ma Huang

Aromatase, a cytochrome P450 enzyme that converts androgens into estrogens, is an important drug target for hormone-dependent diseases. The purpose of this study was to elucidate the aromatase inhibitory effects of Ma-Huang-Tang (MHT), a traditional Korean herbal medicine prescription, and to identify its active ingredients. In this study, the inhibitory effect of MHT on aromatase activity was observed using dibenzylfluorescein (DBF) and KGN cells, and the dose-dependent effect of MHT was verified (IC50 values of 251 μg/mL and 246 μg/mL as determined by the two methods, respectively). Furthermore, among the six herbal medicines that constitute MHT, Ephedrae Herba, Cinnamomi Ramulus, and Glycyrrhizae Radix et Rhizoma showed the most potent inhibition of aromatase activity. Furthermore, upon identification of the active MHT compounds, three markers from Glycyrrhizae Radix et Rhizoma, liquiritin (5), liquiritin apioside (6), and liquiritigenin (7), were verified (IC50 values of 530 μM, 508 μM, and 1.611 mM and 499 μM, 522 μM, and 1.41 mM as determined by the two methods, respectively). In addition, their contents were confirmed to be 15.58, 19.80, and 2.22 mg/g, respectively, by HPLC/DAD analysis. These results indicate that the aromatase inhibitory effect of MHT results from the synergistic action of its active components and that MHT has potential as a preventive agent against aromatase activity.

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