scholarly journals α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells

Biomolecules ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 275
Author(s):  
Anastasia Psarra ◽  
Maria A. Theodoropoulou ◽  
Martin Erhardt ◽  
Marina Mertiri ◽  
Christiana Mantzourani ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Mesangial Cells ◽  
Cellular Level ◽  
Interleukin 1Β ◽  
Novel Agents

Prostaglandin E2 (PGE2) is a key mediator of inflammation, and consequently huge efforts have been devoted to the development of novel agents able to regulate its formation. In this work, we present the synthesis of various α-ketoheterocycles and a study of their ability to inhibit the formation of PGE2 at a cellular level. A series of α-ketobenzothiazoles, α-ketobenzoxazoles, α-ketobenzimidazoles, and α-keto-1,2,4-oxadiazoles were synthesized and chemically characterized. Evaluation of their ability to suppress the generation of PGE2 in interleukin-1β plus forskolin-stimulated mesangial cells led to the identification of one α-ketobenzothiazole (GK181) and one α-ketobenzoxazole (GK491), which are able to suppress the PGE2 generation at a nanomolar level.

Endocytosis by cultured mesangial cells and associated changes in prostaglandin E2 synthesis

1987 ◽  
Vol 252 (4) ◽  
pp. F627-F634
Author(s):  
P. C. Singhal ◽  
G. H. Ding ◽  
S. DeCandido ◽  
N. Franki ◽  
R. M. Hays ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Cytochalasin B ◽  
Mesangial Cells ◽  
Pge2 Production ◽  
Receptor Interaction ◽  
Coated Pits ◽  
Pge2 Synthesis ◽  
Gold Particles ◽  
Fresh Serum ◽  
Stimulation Of

The mechanism of macromolecule uptake by cultured mesangial cells was studied by use of transmission electron microscopy. In parallel, we investigated the effect of macromolecular uptake on prostaglandin E2 (PGE2) formation. Cultured rat mesangial cells were studied in their third passage. As model molecules, we used colloidal gold particles (10 nm diameter) coated either with polyethylene glycol (PEG) or fresh serum (SCG). Mesangial cells were incubated from 1 to 60 min and up to 12 h with either PEG or SCG particles. Endocytosis of SCG significantly exceeded that of PEG particles. The mechanism involved binding to coated pits, followed by formation of coated vesicles (endosomes), and eventually delivery of particles to lysosomes. Pretreatment with cytochalasin B virtually prevented endocytosis of SCG particles, indicating active participation of the cytoskeleton. Determination of PGE2 production in parallel showed that SCG significantly stimulated PGE2 synthesis within minutes, whereas PEG-coated gold had no effect. When gold particles were coated with decomplemented serum instead of fresh serum, the stimulation of PGE2 was partially, but not completely, prevented, indicating that complement may be one, but not the only ligand responsible for enhanced PGE2 production. Stimulation of PGE2 synthesis by SCG was not dependent on actual endocytosis, as it was not altered by cytochalasin B pretreatment. Thus, surface ligand-receptor interaction may be sufficient to trigger PGE2 synthesis. The interaction between mesangial endocytosis and PGE2 production may be important for glomerular pathophysiology.

scholarly journals Suppression by cyclosporin A of interleukin 1β -induced expression of group II phospholipase A2 in rat renal mesangial cells

1997 ◽  
Vol 121 (4) ◽  
pp. 787-793 ◽  
Author(s):  
Gaby Walker ◽  
Dieter Kunz ◽  
Werner Pignat ◽  
Henk van den Bosch ◽  
Josef Pfeilschifter
Keyword(s):  
Phospholipase A2 ◽  
Cyclosporin A ◽  
Mesangial Cells ◽  
Interleukin 1Β ◽  
Induced Expression ◽  
Group Ii

The involvement of prostaglandin E2 in interleukin-1β evoked anorexia is strain dependent

2017 ◽  
Vol 60 ◽  
pp. 27-31 ◽  
Author(s):  
Anna Nilsson ◽  
Louise Elander ◽  
Martin Hallbeck ◽  
Unn Örtegren Kugelberg ◽  
David Engblom ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Interleukin 1Β ◽  
Strain Dependent ◽  
Is Strain

scholarly journals Activation of phospholipase C and prostaglandin synthesis by [arginine]vasopressin in cultures

1984 ◽  
Vol 223 (3) ◽  
pp. 855-859 ◽  
Author(s):  
J Pfeilschifter ◽  
A Kurtz ◽  
C Bauer
Keyword(s):  
Arachidonic Acid ◽  
Phosphatidic Acid ◽  
Prostaglandin E2 ◽  
Phospholipase C ◽  
Arginine Vasopressin ◽  
Mesangial Cells ◽  
Significant Loss ◽  
Prostaglandin Synthesis ◽  
Phosphatidylinositol 4 ◽  
In Cells

[Arginine]vasopressin (AVP) stimulates maximal prostaglandin E2 production in cultured rat renal mesangial cells within 2 min. As early as 10s after addition of AVP (10(-6)M) a significant loss of radioactivity from phosphatidylinositol 4,5-bisphosphate but not from phosphatidylinositol 4-phosphate and phosphatidylinositol was observed in cells prelabelled with 32Pi. Cells labelled with [14C]arachidonic acid showed an increase of label in 1,2-diacylglycerol after 15 s and in phosphatidic acid after 30 s upon stimulation with AVP. Pretreatment of the cells with indomethacin (10(-5)M) did not abolish the effect of AVP on the increased labelling of phosphatidic acid.

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