| 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. | |
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MedLine Citation:
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PMID: 23347011 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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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. |
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Authors:
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Hai-Long Wang; Li-Chuan Wang; Jiann-Wu Wei |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: The Chinese journal of physiology Volume: 56 ISSN: 0304-4920 ISO Abbreviation: Chin J Physiol Publication Date: 2013 Feb |
Date Detail:
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Created Date: 2013-01-25 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7804502 Medline TA: Chin J Physiol Country: China (Republic : 1949- ) |
Other Details:
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Languages: eng Pagination: xxx Citation Subset: IM |
Affiliation:
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Institute of Neuroscience, National Yang Ming University, Shih-Pai, Beitou Taipei 112, Taiwan, R.O.C. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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