Inhibitory Effect of Three Diketopiperazines from Marine-derived Bacteria on Secretory Group IIA Phospholipase A2
| Autor: | Sae-Kwang Ku, Jong-Sup Bae, Hyukjae Choi |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Lipopolysaccharides
Male 0301 basic medicine Marine sponges Spla2 iia Diketopiperazines Plant Science Red algae Group II Phospholipases A2 Mice 03 medical and health sciences Phospholipase A2 Sepsis Drug Discovery Human Umbilical Vein Endothelial Cells Animals Humans Phosphorylation Inhibitory effect Pharmacology Mice Inbred ICR Bacteria 030102 biochemistry & molecular biology biology Chemistry General Medicine biology.organism_classification Gorgonian Complementary and alternative medicine Biochemistry biology.protein Mitogen-Activated Protein Kinases |
| Zdroj: | Natural Product Communications. 11:1934578X1601100 |
| ISSN: | 1555-9475 1934-578X |
| DOI: | 10.1177/1934578x1601100919 |
| Popis: | Diketopiperazines, natural products found in bacteria, fungi, marine sponges, gorgonian and red algae, are cyclic dipeptides possessing relatively simple and rigid structures with chiral nature and various side chains. The compounds in this structure class have been known to possess diverse bioactivities including antibiotic activity, anti-cancer activity, neuroprotective activity, and anti-inflammatory activity. The expression of secretory group IIA phospholipase A2 (sPLA2-IIA) is enhanced by development of inflammatory disorders. Aim of this study is to determine the effects of diketopiperazines on the secretion and activity of sPLA2-IIA by lipopolysaccharide (LPS) in human umbilical vein endothelial cells (HUVECs). To do this, sPLA2-IIA expression was induced in the LPS-stimulated HUVECs and mice to evaluate the effect of diketopiperazines. Results showed that diketopiperazines remarkably suppressed the LPS-mediated protein expression and activity of sPLA2-IIA via inhibition of phosphorylation of cytosolic phospholipase A2 (cPLA2) and extracellular signal-regulated kinase (ERK) 1/2. These results demonstrated that diketopiperazines might play an important role in the modulation of sPLA2-IIA expression and activity in response to the inflammatory diseases. |
| Databáze: | OpenAIRE |
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