Activity landscape modeling of PPAR ligands with dual-activity difference maps

2012 ◽  
Vol 20 (11) ◽  
pp. 3523-3532 ◽  
Author(s):  
Oscar Méndez-Lucio ◽  
Jaime Pérez-Villanueva ◽  
Rafael Castillo ◽  
José L. Medina-Franco
Keyword(s):  
Landscape Modeling ◽  
Activity Difference ◽  
Ppar Ligands

774: Improvement of Anti-Angiogenic and Anti-Tumorigenic Efficacy of Thrombospondin-1 by PPAR┌ Ligands in Bladder Cancer

2007 ◽  
Vol 177 (4S) ◽  
pp. 259-259
Author(s):  
Thomas Nelius ◽  
Hanua Huang ◽  
Stephanie Filleur ◽  
Steven C. Campbell ◽  
Werner de Riese ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Thrombospondin 1 ◽  
Ppar Ligands

PPAR ligands: Potential therapies for metabolic syndrome

2005 ◽  
Vol 5 (1) ◽  
pp. 45-52 ◽  
Author(s):  
Taro E. Akiyama ◽  
Peter T. Meinke ◽  
Joel P. Berger
Keyword(s):  
Metabolic Syndrome ◽  
Ppar Ligands

The effect of PPAR?? ligands on the proliferation and apoptosis of human melanoma cells

2003 ◽  
Vol 13 (5) ◽  
pp. 447-456 ◽  
Author(s):  
Wojciech Placha ◽  
Dorota Gil ◽  
Aldona Dembi??ska-Kie?? ◽  
Piotr Laidler
Keyword(s):  
Melanoma Cells ◽  
Human Melanoma ◽  
Human Melanoma Cells ◽  
Proliferation And Apoptosis ◽  
Ppar Ligands

Challenges of forest landscape modeling—Simulating large landscapes and validating results

2011 ◽  
Vol 100 (4) ◽  
pp. 400-402 ◽  
Author(s):  
Hong S. He ◽  
Jian Yang ◽  
Stephen R. Shifley ◽  
Frank R. Thompson
Keyword(s):  
Forest Landscape ◽  
Landscape Modeling ◽  
Forest Landscape Modeling

Shelf Life and Moisture Transfer Predictions in a Composite Food Product: Impact of Preservation Techniques

2008 ◽  
Vol 4 (4) ◽  
Author(s):  
Elisabeth Roca ◽  
Dorothée Adeline ◽  
Valérie Guillard ◽  
Stéphane Guilbert ◽  
Nathalie Gontard
Keyword(s):  
Shelf Life ◽  
Water Activity ◽  
Food System ◽  
Moisture Transfer ◽  
Food Product ◽  
Moisture Diffusivity ◽  
Point Of View ◽  
Effective Moisture Diffusivity ◽  
Effective Moisture ◽  
Activity Difference

Three techniques to prevent moisture transfer in a multidomain food system constituted by a cookie in contact with a moist filling were investigated: reducing the water activity difference between components, reducing the effective moisture diffusivity of the cereal-based component, and applying an edible moisture barrier at the interface between components. Shelf-life of the food product was extended by 6 days by decreasing the water activity of the moist filling in contact from 0.99 to 0.64 (cookie aw being 0.23, 20°C). Decreasing effective moisture diffusivity from 1.56 to 0.99*10-11 m²/s by the addition of 2.35 g of fat in the formulation of the cookie was limited by technological and organoleptic considerations and allowed an extension of shelf-life of 2 more days. From a technical and nutritional point of view, the application of a sprayed edible barrier at the surface of the cookie was the more effective solution increasing shelf life of almost 8 days for only 1.7 g of fat per cookie.

scholarly journals Comparison of PPAR Ligands as Modulators of Resolution of Inflammation, via Their Influence on Cytokines and Oxylipins Release in Astrocytes

2020 ◽  
Vol 21 (24) ◽  
pp. 9577
Author(s):  
Dmitry V. Chistyakov ◽  
Alina A. Astakhova ◽  
Sergei V. Goriainov ◽  
Marina G. Sergeeva
Keyword(s):  
Interleukin 10 ◽  
Mitogen Activated Protein Kinase ◽  
Cytochrome P450 Monooxygenases ◽  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
P450 Monooxygenases ◽  
Pparγ Agonist ◽  
Inflammatory Stimuli ◽  
Anti Inflammatory ◽  
Ppar Ligands

Neuroinflammation is a key process of many neurodegenerative diseases and other brain disturbances, and astrocytes play an essential role in neuroinflammation. Therefore, the regulation of astrocyte responses for inflammatory stimuli, using small molecules, is a potential therapeutic strategy. We investigated the potency of peroxisome proliferator-activated receptor (PPAR) ligands to modulate the stimulating effect of lipopolysaccharide (LPS) in the primary rat astrocytes on (1) polyunsaturated fatty acid (PUFAs) derivative (oxylipins) synthesis; (2) cytokines TNFα and interleukin-10 (IL-10) release; (3) p38, JNK, ERK mitogen-activated protein kinase (MAPKs) phosphorylation. Astrocytes were exposed to LPS alone or in combination with the PPAR ligands: PPARα (fenofibrate, GW6471); PPARβ (GW501516, GSK0660); PPARγ (rosiglitazone, GW9662). We detected 28 oxylipins with mass spectrometry (UPLC-MS/MS), classified according to their metabolic pathways: cyclooxygenase (COX), cytochrome P450 monooxygenases (CYP), lipoxygenase (LOX) and PUFAs: arachidonic (AA), docosahexaenoic (DHA), eicosapentaenoic (EPA). All tested PPAR ligands decrease COX-derived oxylipins; both PPARβ ligands possessed the strongest effect. The PPARβ agonist, GW501516 is a strong inducer of pro-resolution substances, derivatives of DHA: 4-HDoHE, 11-HDoHE, 17-HDoHE. All tested PPAR ligands decreased the release of the proinflammatory cytokine, TNFα. The PPARβ agonist GW501516 and the PPARγ agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFα) was more for GW501516. The PPARβ ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. Overall, our data revealed that the PPARβ ligands are a potential pro-resolution and anti-inflammatory drug for targeting glia-mediated neuroinflammation.

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