scholarly journals Anti-diabetic potential of crude extracts of medicinal plants used as substitutes for Swertia chirayita using in vitro assays

1970 ◽  
Vol 7 ◽  
pp. 48-55 ◽  
Author(s):  
Susanna Phoboo ◽  
Prasanta C Bhowmik ◽  
Pramod Kumar Jha ◽  
Kalidas Shetty
Keyword(s):  
Type 2 Diabetes ◽  
Antioxidant Activity ◽  
Early Stage ◽  
Andrographis Paniculata ◽  
Total Phenolic ◽  
Swertia Chirayita ◽  
Inhibitory Potential ◽  
Swertia Species

Swertia chirayita is a highly traded medicinal plant of Nepal widely used for its anti-diabetic potential. In this study, two herbs (Swertia nervosa and Andrographis paniculata) often used as adulterants and substitutes of Swertia chirayita were analyzed for their antioxidant activity, α-glucosidase inhibitory potential and total phenolic content and compared with that of Swertia chirayita. Aqueous and 12% ethanolic extracts of the three herbs showed moderate to high antioxidant activity and moderate α-glucosidase inhibitory potential. HPLC/ DAD revealed the presence of swertiamarin and mangiferin in all the Swertia species, while Andrographis paniculata contained cinnamates such as cinnamic acid, p-coumaric acid and chlorogenic acid. The antioxidant activity and α-glucosidase inhibitory potential was evident in the two herbs indicating their relevance as substitutes for Swertia chirayita for potential early stage management of type-2 diabetes and related complications. Key-words: Andrographis paniculata; antioxidant activity; cinnamates; mangiferin; Swertia nervosa; swertiamarin; α-glucosidase; type-2 diabetes. DOI: 10.3126/botor.v7i0.4373Botanica Orientalis – Journal of Plant Science (2010) 7: 48-55

Hyperglycemia and hyperlipidemia are associated with endothelial dysfunction during the development of type 2 diabetes

2007 ◽  
Vol 85 (5) ◽  
pp. 562-567 ◽  
Author(s):  
Elena B. Okon ◽  
Ada W.Y. Chung ◽  
Hongbin Zhang ◽  
Ismail Laher ◽  
Cornelis van Breemen
Keyword(s):  
Type 2 Diabetes ◽  
Endothelial Dysfunction ◽  
Endothelial Function ◽  
Plasma Levels ◽  
Early Stage ◽  
Cardiovascular Complications ◽  
Older Age ◽  
Metabolic Markers

Diabetes mellitus impairs endothelial function, which can be considered as the hallmark in the development of cardiovascular diseases. Hyperglycemia, hyperinsulinemia, and hyperlipidemia are believed to contribute to endothelial dysfunction. In the present study, we investigated the possible links among these plasma metabolic markers and endothelial function in a mouse model during the development of type 2 diabetes. C57BL/6J-Lepob/ob mice at 8, 12, and 16 weeks were used to study endothelial function during the establishment of type 2 diabetes. Endothelial function was accessed in vitro in the thoracic aorta by measuring acetylcholine (ACh)-stimulated vasodilatation. Blood plasma was obtained for the measurements of glucose, insulin, triglycerides, and cholesterol levels. Correlation and multiple regression analysis revealed strong negative associations between the ACh responsiveness and the plasma levels of glucose, insulin, and lipid profiles at the age of 8 weeks. Associations were observed at neither older age nor in C57BL/6J mice. In conclusion, the increase in plasma levels of glucose, insulin, and lipids is associated with the impairment of the endothelial function during the early stage of the development of type 2 diabetes. The loss of correlation at an older age suggests multifactorial regulation of endothelial function and cardiovascular complications at later stages of the disease.

Phenolic bioactives from developmental stages of highbush blueberry (Vaccinium corymbosum) for hyperglycemia management using in vitro models

2015 ◽  
Vol 95 (4) ◽  
pp. 653-662 ◽  
Author(s):  
Susan Cheplick ◽  
Dipayan Sarkar ◽  
Prasanta Bhowmik ◽  
Kalidas Shetty
Keyword(s):  
Type 2 Diabetes ◽  
Antioxidant Activity ◽  
Inhibitory Activity ◽  
Developmental Stages ◽  
Vaccinium Corymbosum ◽  
In Vitro Models ◽  
In Vitro Assays ◽  
Highbush Blueberry

Cheplick, S., Sarkar, D., Bhowmik, P. and Shetty, K. 2015. Phenolic bioactives from developmental stages of highbush blueberry (Vaccinium corymbosum) for hyperglycemia management using in vitro models. Can. J. Plant Sci. 95: 653–662. Blueberry is a rich source of soluble phenolics as well as human health relevant antioxidants. Phenolic-linked bioactive functionality of blueberry for type 2 diabetes management was screened during fruit maturation, especially from green to ripening stages using in vitro assays. Green fruit showed the highest total soluble phenolic content, whereas all three developmental stages of blueberry fruit exhibited high total antioxidant activity. Overall, ripe fruit had higher α-amylase and α-glucosidase inhibitory activity than green or green/pink fruit, and showed significant potential to improve glucose metabolism through in vitro assays. High phenolic-linked antioxidant activity along with moderate to high α-amylase and α-glucosidase inhibitory activity in ripe blueberry indicated its potential relevance as part of diet-based prevention and management of early stages of hyperglycemia associated with development of type 2 diabetes. This in vitro screening study provides a biochemical rationale and dietary strategy to develop the right blueberry cultivar and stage of fruit development for further validation in animal and clinical studies.

In vitro antioxidant and inhibitory potential of Terminalia bellerica and Emblica officinalis fruits against LDL oxidation and key enzymes linked to type 2 diabetes

2011 ◽  
Vol 49 (1) ◽  
pp. 125-131 ◽  
Author(s):  
Suresh V. Nampoothiri ◽  
A. Prathapan ◽  
Ozhathil Lijo Cherian ◽  
K.G. Raghu ◽  
V.V. Venugopalan ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Ldl Oxidation ◽  
Emblica Officinalis ◽  
Key Enzymes ◽  
Terminalia Bellerica ◽  
Inhibitory Potential

scholarly journals Synthesis, In Vitro Evaluation and Molecular Docking of the 5-Acetyl-2-aryl-6-hydroxybenzo[b]furans against Multiple Targets Linked to Type 2 Diabetes

Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 418 ◽  
Author(s):  
Malose J. Mphahlele ◽  
Yee Siew Choong ◽  
Marole M. Maluleka ◽  
Samantha Gildenhuys
Keyword(s):  
Type 2 Diabetes ◽  
Antioxidant Activity ◽  
Molecular Docking ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Protein Tyrosine Phosphatase 1B

The 5-acetyl-2-aryl-6-hydroxybenzo[b]furans 2a–h have been evaluated through in vitro enzymatic assay against targets which are linked to type 2 diabetes (T2D), namely, α-glucosidase, protein tyrosine phosphatase 1B (PTP1B) and β-secretase. These compounds have also been evaluated for antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging method. The most active compounds against α-glucosidase and/or PTP1B, namely, 4-fluorophenyl 2c, 4-methoxyphenyl 2g and 3,5-dimethoxyphenyl substituted 2h derivatives were also evaluated for potential anti-inflammatory properties against cyclooxygenase-2 activity. The Lineweaver-Burk and Dixon plots were used to determine the type of inhibition on compounds 2c and 2h against α-glucosidase and PTP1B receptors. The interactions were investigated in modelled complexes against α-glucosidase and PTP1B via molecular docking.

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.

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