scholarly journals Phenolics Profiling of Carpobrotus edulis (L.) N.E.Br. and Insights into Molecular Dynamics of Their Significance in Type 2 Diabetes Therapy and Its Retinopathy Complication

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4867
Author(s):  
Saheed Sabiu ◽  
Fatai O. Balogun ◽  
Stephen O. Amoo
Keyword(s):  
Type 2 Diabetes ◽  
Phenolic Compounds ◽  
Aldose Reductase ◽  
Alpha Amylase ◽  
Diabetes Therapy ◽  
Carpobrotus Edulis ◽  
Phenolic Extract ◽  
Alpha Glucosidase

Adverse effects associated with synthetic drugs in diabetes therapy has prompted the search for novel natural lead compounds with little or no side effects. Effects of phenolic compounds from Carpobrotus edulis on carbohydrate-metabolizing enzymes through in vitro and in silico methods were assessed. Based on the half-maximal inhibitory concentrations (IC50), the phenolic extract of the plant had significant (p < 0.05) in vitro inhibitory effect on the specific activity of alpha-amylase (0.51 mg/mL), alpha-glucosidase (0.062 mg/mL) and aldose reductase (0.75 mg/mL), compared with the reference standards (0.55, 0.72 and 7.05 mg/mL, respectively). Molecular interactions established between the 11 phenolic compounds identifiable from the HPLC chromatogram of the extract and active site residues of the enzymes revealed higher binding affinity and more structural compactness with procyanidin (−69.834 ± 6.574 kcal/mol) and 1,3-dicaffeoxyl quinic acid (−42.630 ± 4.076 kcal/mol) as potential inhibitors of alpha-amylase and alpha-glucosidase, respectively, while isorhamnetin-3-O-rutinoside (−45.398 ± 4.568 kcal/mol) and luteolin-7-O-beta-d-glucoside (−45.102 ± 4.024 kcal/mol) for aldose reductase relative to respective reference standards. Put together, the findings are suggestive of the compounds as potential constituents of C. edulis phenolic extract responsible for the significant hypoglycemic effect in vitro; hence, they could be exploited in the development of novel therapeutic agents for type-2 diabetes and its retinopathy complication.

Novel polydatin-loaded chitosan nanoparticles for safe and efficient type 2 diabetes therapy: In silico, in vitro and in vivo approaches

2020 ◽  
Vol 154 ◽  
pp. 1496-1504 ◽  
Author(s):  
Adel Abdel-Moneim ◽  
Ahmed El-Shahawy ◽  
Ahmed Ismail Yousef ◽  
Sanaa Mahmoud Abd El-Twab ◽  
Zienab Essam Elden ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
In Silico ◽  
Chitosan Nanoparticles ◽  
Diabetes Therapy ◽  
Efficient Type

Exploration of Diosmin to control diabitis and its complications-an in vitro and in silico approach

2020 ◽  
Vol 16 ◽  
Author(s):  
Kushagra Dubey ◽  
Raghvendra Dubey ◽  
Revathi Gupta ◽  
Arun Gupta
Keyword(s):  
Molecular Docking ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Blood Lipid ◽  
Docking Studies ◽  
Alpha Amylase ◽  
Lipid Lowering ◽  
Molecular Docking Studies ◽  
Alpha Glucosidase

Background: Diosmin is a flavonoid obtained from the citrus fruits of the plants. Diosmin has blood lipid lowering activities, antioxidant activity, enhances venous tone and microcirculation, protects capillaries, mainly by reducing systemic oxidative stress. Objective: The present study demonstrates the potential of Diosmin against the enzymes aldose reductase, α-glucosidase, and α-amylase involved in diabetes and its complications by in vitro evaluation and reverse molecular docking studies. Method: The assay of aldose reductase was performed by using NADPH as starting material and DL-Glyceraldehyde as a substrate. DNS method was used for alpha amylase inhibition and in alpha glucosidase inhibitory activity p-nitrophenyl glucopyranoside (pNPG) was used as substrate. The reverse molecular docking studies was performed by using Molegro software (MVD) with grid resolution of 30 Å. Result: Diosmin shows potent inhibitory effect against aldose reductase (IC50:333.88±0.04 µg/mL), α-glucosidase (IC50:410.3±0.01 µg/mL) and α-amylase (IC50: 404.22±0.02 µg/mL) respectively. The standard drugs shows moderate inhibitory activity for enzymes. The MolDock Score of Diosmin was -224.127 against aldose reductase, -168.17 against α-glucosidase and -176.013 against α-amylase respectively, which was much higher than standard drugs. Conclusion: From the result it was concluded that diosmin was a potentially inhibitor of aldose reductase, alpha amylase and alpha glucosidase enzymes then the standard drugs and it will be helpful in the management of diabetes and its complications. This will also be benevolent to decrease the socio economical burden on the middle class family of the society.

scholarly journals Effect of Avarai Kudineer on α- Amylase and α- Glucosidase Inhibition: A Preclinical Antidiabetic Study

2021 ◽  
pp. 818-825
Author(s):  
K. Rajalakshmi ◽  
P. Shanmugapriya ◽  
G. J. Christian ◽  
R. Jeeva Gladys
Keyword(s):  
Diabetes Mellitus ◽  
Preparation Method ◽  
Maximum Activity ◽  
Alpha Amylase ◽  
Test Drug ◽  
Standard Drug ◽  
Polyherbal Formulation ◽  
Alpha Glucosidase

In recent years there has been a mounting interest towards the traditional medicine globally for the treatment of type 2 diabetes. Avarai Kudineer (AK) is a Siddha classical polyherbal formulation that has been indicated for the management of Diabetes mellitus in Siddha literature. The goal of the present study is to provide an in-vitro evidence for the  antidiabetic potential of Avarai Kudineer in terms of  inhibiting the carbohydrate digesting enzymes alpha amylase and alpha glucosidase. Aavirai Kudineer (1/4) was prepared by boiling the ingredients weighed 20g in 80ml and reduced to 20ml and filtered according to the decoction preparation method as indicted in the Siddha literature. The filtrate was dissolved in DMSO to make stock solution and serially diluted to make different concentrations ranging from 10,20,40,80 and 100 µg/ml. The triplicates (n=3) were maintained. The invitro alpha amylase and alpha glucosidase enzyme inhibition of AK sample was compared with standard drug acarbose and the IC 50 value was calculated.The data was statistically analysed and expressed as Mean ± SD (n=3). The results showed that AK had maximum activity towards the inhibition of the enzyme alpha amylase (59.83± 7.10) and alpha glucosidase (71.94 ± 1.22) when compared with the standard acarbose81.42± 5.51 and 91.59 ±12.79respectively. The results reveal that the test drug AK has appreciable alpha amylase and alpha glucosidase inhibitory activity.

Integrate Incretins Into Type 2 Diabetes Therapy

2008 ◽  
Vol 38 (10) ◽  
pp. 18-19
Author(s):  
MARY ELLEN SCHNEIDER
Keyword(s):  
Type 2 Diabetes ◽  
Diabetes Therapy

Recent Developments in Alpha-Glucosidase Inhibitors for Management of Type-2 Diabetes: An Update

2019 ◽  
Vol 25 (23) ◽  
pp. 2510-2525 ◽  
Author(s):  
Bashir Usman ◽  
Neha Sharma ◽  
Saurabh Satija ◽  
Meenu Mehta ◽  
Manish Vyas ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Patient Compliance ◽  
Postprandial Hyperglycemia ◽  
Diabetic Patients ◽  
Poor Patient ◽  
Glucosidase Inhibitors ◽  
Poor Patient Compliance ◽  
Recent Developments ◽  
Alpha Glucosidase

The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes of drugs are available for the management of type 2 diabetes but were having certain limitations of their safety. Alphaglucosidase is a family of enzyme originated from the pancreas which plays a role in the anabolism of 80-90% of carbohydrate consumed into glucose. This glucose is absorbed into the blood and results in frank postprandial hyperglycemia and worsens the conditions of diabetic patients which precipitate complications. Inhibition of these enzymes helps to prevent postprandial hyperglycemia and the formation of glycated end products. Alphaglucosidase inhibitors are reported to be more important in adequate control of type 2, but marketed drugs have various side effects, such as poor patient compliance and also expensive. This proves the needs for other class of drugs with better efficacy, safety, patient compliance and economic. In this review, we have emphasized the recent advances in the field of new alpha-glucosidase inhibitors with improved safety and pharmacological profile.

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.

scholarly journals Pharmaceutical hit of anti type 2 Diabetes mellitus on the phenolic extract of Malaka (Phyllanthus emblica L.) flesh

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Musri Musman ◽  
Mauli Zakia ◽  
Ratu Fazlia Inda Rahmayani ◽  
Erlidawati Erlidawati ◽  
Safrida Safrida
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Body Weight ◽  
Blood Glucose ◽  
Phyllanthus Emblica ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
Phenolic Extract

Abstract Background Ethnobotany knowledge in a community has shaped local wisdom in utilizing plants to treat diseases, such as the use of Malaka (Phyllanthus emblica) flesh to treat type 2 diabetes. This study presented evidence that the phenolic extract of the Malaka flesh could reduce blood sugar levels in the diabetic induced rats. Methods The phenolic extract of the P. emblica was administrated to the glucose-induced rats of the Wistar strain Rattus norvegicus for 14 days of treatment where the Metformin was used as a positive control. The data generated were analyzed by the two-way ANOVA Software related to the blood glucose level and by SAS Software related to the histopathological studies at a significant 95% confidence. Results The phenolic extract with concentrations of 100 and 200 mg/kg body weight could reduce blood glucose levels in diabetic rats. The post hoc Dunnet test showed that the administration of the extract to the rats with a concentration of 100 mg/kg body weight demonstrated a very significant decrease in blood glucose levels and repaired damaged cells better than administering the extract at a concentration of 200 mg/kg weight body. Conclusion The evidence indicated that the phenolic extract of the Malaka flesh can be utilized as anti type 2 Diabetes mellitus without damaging other organs.

scholarly journals Experimental Type 2 Diabetes Differently Impacts on the Select Functions of Bone Marrow-Derived Multipotent Stromal Cells

Cells ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 268
Author(s):  
Jonathan Ribot ◽  
Cyprien Denoeud ◽  
Guilhem Frescaline ◽  
Rebecca Landon ◽  
Hervé Petite ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Bone Marrow ◽  
Stromal Cells ◽  
Adipogenic Differentiation ◽  
Therapeutic Modality ◽  
Multipotent Stromal Cells ◽  
Cell Therapies

Bone marrow-derived multipotent stromal cells (BMMSCs) represent an attractive therapeutic modality for cell therapy in type 2 diabetes mellitus (T2DM)-associated complications. T2DM changes the bone marrow environment; however, its effects on BMMSC properties remain unclear. The present study aimed at investigating select functions and differentiation of BMMSCs harvested from the T2DM microenvironment as potential candidates for regenerative medicine. BMMSCs were obtained from Zucker diabetic fatty (ZDF; an obese-T2DM model) rats and their lean littermates (ZL; controls), and cultured under normoglycemic conditions. The BMMSCs derived from ZDF animals were fewer in number, with limited clonogenicity (by 2-fold), adhesion (by 2.9-fold), proliferation (by 50%), migration capability (by 25%), and increased apoptosis rate (by 2.5-fold) compared to their ZL counterparts. Compared to the cultured ZL-BMMSCs, the ZDF-BMMSCs exhibited (i) enhanced adipogenic differentiation (increased number of lipid droplets by 2-fold; upregulation of the Pparg, AdipoQ, and Fabp genes), possibly due to having been primed to undergo such differentiation in vivo prior to cell isolation, and (ii) different angiogenesis-related gene expression in vitro and decreased proangiogenic potential after transplantation in nude mice. These results provided evidence that the T2DM environment impairs BMMSC expansion and select functions pertinent to their efficacy when used in autologous cell therapies.

Sign in / Sign up

Export Citation Format

Share Document