Synthesis and Insulin-sensitizing Activity of a Series of 2-Benzyl-1,3-dicarbonyl Derivatives

2010 ◽  
Vol 21 (4) ◽  
pp. 365-368
Author(s):  
Tang Lei ◽  
Leng Ying ◽  
Wang Huo-Quan ◽  
Feng Ying ◽  
Yang Yu-She ◽  
...  
2020 ◽  
Vol 4 (5) ◽  
pp. 2070051
Author(s):  
Kun Chen ◽  
Hongli Jia ◽  
Yuan Liu ◽  
Panchao Yin ◽  
Yongge Wei

2011 ◽  
pp. OR23-6-OR23-6
Author(s):  
Neves Francisco de Assis Rocha ◽  
Senepathy Rajagopalan ◽  
Bruno M Carvalho ◽  
Mario JA Saad ◽  
Marie Togashi ◽  
...  

2009 ◽  
Vol 123 (2) ◽  
pp. 288-292 ◽  
Author(s):  
Hao-Shu Wu ◽  
Di-Feng Zhu ◽  
Chang-Xin Zhou ◽  
Chu-Rui Feng ◽  
Yi-Jia Lou ◽  
...  

Author(s):  
Narendar Koyagura ◽  
I M Nagendra Nayak ◽  
M G Jamadar ◽  
Ashok M Patil ◽  
Sanjit Anand

<p>ABSTRACT<br />Objective: This study was undertaken to evaluate the preventive effect of heartwood of P. marsupium in dexamethasone-induced hyperinsulinemia<br />and hyperglycemia and compare it with that of pioglitazone.<br />Methods: Male albino wistar rats were divided into five groups (n=6). Plain control group received gum acacia (2%) orally from d 1 to d 12. Dexa<br />control group received gum acacia (2%) orally for d 1 to d 12 and Dexa (8 mg/kg) intraperitoneal (i.p.) from d 7 to d 12, during the study period.<br />Two test groups received ethanolic extract of Pterocarpus marsupium heartwood (PME) (1 and 2 g/kg/) per oral (PO), and standard control group<br />received pioglitazone (60 mg/kg/PO) from d 1 to d 12. During the 12-d study period, the two test groups and standard control group received Dexa<br />(8 mg/kg/i.p.) from d 7 to d 12. On last day of the study, the blood samples were collected by retro-orbital sinus punctureand used for estimation of<br />serum insulin and glucose levels. Homeostatic Model Assessment (HOMA) method was employed to calculate the degree of insulin resistance(IR).<br />Results were analyzed by using one-way analysis of variance followed by Scheffe’s multiple comparison test (p&lt;0.05).<br />Results: Treatment with ethanolic extract of P. marsupium and pioglitazone significantly (p&lt;0.05) reduced the elevated insulin and glucose levels as<br />well as HOMA-IR and HOMA-IS values in dexa treated animals.<br />Conclusion: Ethanolic extract of P. marsupium heartwood effectively countered dexamethasone-induced hyperinsulinemia and hyperglycemia.<br />Insulin-sensitizing activity of P. marsupium heartwood was found to be more effective than pioglitazone.<br />Keywords: Pterocarpus marsupium, Insulin resistance, Hyperinsulinemia, Hyperglycemia.</p>


2003 ◽  
Vol 13 (20) ◽  
pp. 3437-3440 ◽  
Author(s):  
Lei Tang ◽  
Juanhong Yu ◽  
Ying Leng ◽  
Ying Feng ◽  
Yushe Yang ◽  
...  

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 275 ◽  
Author(s):  
Sungjin Ahn ◽  
Dong Man Jang ◽  
Sung Chul Park ◽  
Seungchan An ◽  
Jongheon Shin ◽  
...  

Adiponectin is an adipocyte-derived cytokine having an insulin-sensitizing activity. During the phenotypic screening of secondary metabolites derived from the marine fungus Aspergillus terreus, a poly cyclin-dependent kinase (CDK) inhibitor butyrolactone I affecting CDK1 and CDK5 was discovered as a potent adiponectin production-enhancing compound in the adipogenesis model of human bone marrow-derived mesenchymal stem cells (hBM-MSCs). CDK5 inhibitors exhibit insulin-sensitizing activities by suppressing the phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ). However, the adiponectin production-enhancing activities of butyrolactone I have not been correlated with the potency of CDK5 inhibitor activities. In a target identification study, butyrolactone I was found to directly bind to PPARγ. In the crystal structure of the human PPARγ, the ligand-binding domain (LBD) in complex with butyrolactone I interacted with the amino acid residues located in the hydrophobic binding pockets of the PPARγ LBD, which is a typical binding mode of the PPARγ partial agonists. Therefore, the adiponectin production-enhancing effect of butyrolactone I was mediated by its polypharmacological dual modulator activities as both a CDK5 inhibitor and a PPARγ partial agonist.


2020 ◽  
Vol 4 (5) ◽  
pp. 1900281
Author(s):  
Kun Chen ◽  
Hongli Jia ◽  
Yuan Liu ◽  
Panchao Yin ◽  
Yongge Wei

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