Document Detail

Differential Inhibitory Effects of 2-Azafluorenones on PI-PLC Activation but not on PC-PLC- or PC-PLD-Activation Induced by Histamine, PAF, PMA or A23187 in C6 Glioma Cells.
MedLine Citation:
PMID:  23347011     Owner:  NLM     Status:  In-Data-Review    
In this study, C6 glioma cells were used to test the effects of 2-azafluorenone and its related compounds on membrane phosphatidylinositol (PI) and phosphatidylcholine (PC) turnover. An increase of [³H]-labeled inositol phosphate (IP1) formation by histamine (100 μM) or A23187 (100 nM) via the activation of phosphatidylinositol-specific phospholipase C (PI-PLC) to breakdown labeled substrate was observed, and this effect could be partially blocked by about half at 100 μM of 2-azafluorenones. Histamine induced the increase of IP1 formation, but failed to cause an increase in extracellularly releasing of [3H]choline metabolites, or intracellular accumulation of [³H]phosphscholine. However, platelet activation factor (PAF) from 0.2 to 1 μM, and phorbol 12-myristate-13-acetate (PMA) at 1 μM caused an increase in extracellularly releasing of [³H]choline metabolites, and intracellular accumulation of [³H]phosphocholine via the activation on phosphatidylcholine (PC)-PLC. These responses of PAF and PMA were not affected by 2-azafluorenone or 4-methyl-2-azafluorenone even at high concentration (10⁻⁴ M). A23187 induced an increase of intracellular [³H]choline release via the activation of PCphospholipase D (PLD). This increasing effect of 100 nM A23187 was not affected by 2-azafluorenone or 4-methyl-2-azafluorenone even at a high concentration of 10⁻⁴ M. In summary, the inhibitory effect of 2-azafluorenone and its related compound 4-methyl-2-azafluorenone was observed selectively on PIPLC, but not on PC-PLC or PC-PLD based on changes of products after the activation of these enzymes.
Hai-Long Wang; Li-Chuan Wang; Jiann-Wu Wei
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Chinese journal of physiology     Volume:  56     ISSN:  0304-4920     ISO Abbreviation:  Chin J Physiol     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-01-25     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804502     Medline TA:  Chin J Physiol     Country:  China (Republic : 1949- )    
Other Details:
Languages:  eng     Pagination:  xxx     Citation Subset:  IM    
Institute of Neuroscience, National Yang Ming University, Shih-Pai, Beitou Taipei 112, Taiwan, R.O.C.
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