Synthesis of 2-phenyl-1H-imidazo[4,5-b]pyridine as type 2 diabetes inhibitors and molecular docking studies

2017 ◽  
Vol 26 (5) ◽  
pp. 916-928 ◽  
Author(s):  
Muhammad Taha ◽  
Nor Hadiani Ismail ◽  
Syahrul Imran ◽  
Izzatul Ainaa ◽  
Manikandan Selvaraj ◽  
...  
Author(s):  
Tushar Kumar

Diabetes is the becoming one of the most common problem all over the world. About 1 in 10 persons are suffering from diabetes and most from type 2 diabetes. It occurs due to problem in pancreas which further results defect in the insulin secretion, as insulin maintains blood glucose level. The effect of Alpha-Amyrin Acetate, Myrcene and Vasicine compounds against Islet Amyloid polypeptide (IAPP) protein was seen through molecular docking studies. IAPP acts as complementary to insulin in regulating the sugar level for the treatment of diabetes disease by virtual screening. Different tools and software used in this research were Uniprot, Pubchem, Swiss ADMS, PyRx, Auto dock Vina/MGL tool and PyMOL.


2020 ◽  
Vol 96 ◽  
pp. 103579 ◽  
Author(s):  
Antony Stalin ◽  
Subramani Kandhasamy ◽  
Balakrishnan Senthamarai Kannan ◽  
Rama Shanker Verma ◽  
Savarimuthu Ignacimuthu ◽  
...  

2014 ◽  
Vol 85 (4) ◽  
pp. 439-446 ◽  
Author(s):  
Ram N. Kushwaha ◽  
Rohit Srivastava ◽  
Akansha Mishra ◽  
Arun K. Rawat ◽  
Arvind K. Srivastava ◽  
...  

Life Sciences ◽  
2016 ◽  
Vol 153 ◽  
pp. 100-117 ◽  
Author(s):  
Antony Stalin ◽  
Santiagu Stephen Irudayaraj ◽  
Gopalsamy Rajiv Gandhi ◽  
Kedike Balakrishna ◽  
Savarimuthu Ignacimuthu ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5306
Author(s):  
Beiyun Shen ◽  
Xinchen Shangguan ◽  
Zhongping Yin ◽  
Shaofu Wu ◽  
Qingfeng Zhang ◽  
...  

The inhibition of α-glucosidase is a clinical strategy for the treatment of type 2 diabetes mellitus (T2DM), and many natural plant ingredients have been reported to be effective in alleviating hyperglycemia by inhibiting α-glucosidase. In this study, the α-glucosidase inhibitory activity of fisetin extracted from Cotinus coggygria Scop. was evaluated in vitro. The results showed that fisetin exhibited strong inhibitory activity with an IC50 value of 4.099 × 10−4 mM. Enzyme kinetic analysis revealed that fisetin is a non-competitive inhibitor of α-glucosidase, with an inhibition constant value of 0.01065 ± 0.003255 mM. Moreover, fluorescence spectrometric measurements indicated the presence of only one binding site between fisetin and α-glucosidase, with a binding constant (lgKa) of 5.896 L·mol−1. Further molecular docking studies were performed to evaluate the interaction of fisetin with several residues close to the inactive site of α-glucosidase. These studies showed that the structure of the complex was maintained by Pi-Sigma and Pi-Pi stacked interactions. These findings illustrate that fisetin extracted from Cotinus coggygria Scop. is a promising therapeutic agent for the treatment of T2DM.


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