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Titolo:
SECRETED AND INTRACELLULAR PHOSPHOLIPASES A(2) INHIBITION BY 1-DECYL 2-OCTYL-GLYCEROPHOSPHOCHOLINE IN RAT PERITONEAL-MACROPHAGES
Autore:
BOUCROT P; BOBINDUBIGEON C; ELKIHEL L; LETOURNEUX Y; JUGE M; GANDEMER G; PETIT JY;
Indirizzi:
FAC PHARM,LAB PHARMACOL & PHARMACOCINET,BP 1024 F-44035 NANTES 01 FRANCE FAC PHARM,LAB PHARMACOL & PHARMACOCINET F-44035 NANTES 01 FRANCE INRA,LAB ETUD INTERACT MOL ALIMENTAIRES F-44316 NANTES 03 FRANCE LAB SYNTH & ETUD SUBST NAT ACT BIOL F-17042 LA ROCHELLE 1 FRANCE
Titolo Testata:
Fundamental and clinical pharmacology
fascicolo: 4, volume: 12, anno: 1998,
pagine: 433 - 441
SICI:
0767-3981(1998)12:4<433:SAIPAI>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
POTENT COMPETITIVE INHIBITORS; ARACHIDONIC-ACID RELEASE; ALKYL-LYSOPHOSPHOLIPIDS; LIPOLYTIC ENZYMES; ETHER LIPIDS; ALVEOLAR MACROPHAGES; ACYLAMINO ANALOGS; GUINEA-PIG; FATTY-ACID; CELLS;
Keywords:
MACROPHAGE; PHOSPHOLIPASE A(2); INHIBITION; PHOSPHOLIPID ANALOG;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
P. Boucrot et al., "SECRETED AND INTRACELLULAR PHOSPHOLIPASES A(2) INHIBITION BY 1-DECYL 2-OCTYL-GLYCEROPHOSPHOCHOLINE IN RAT PERITONEAL-MACROPHAGES", Fundamental and clinical pharmacology, 12(4), 1998, pp. 433-441

Abstract

Compounds able to inhibit phospholipases A(2) can be considered as potential anti-inflammatory drugs. In this respect, the inhibitory effect of the phospholipid analogue 1-decyl 2-octyl-rac-glycero-3-phosphocholine (decyloctyl-GPC) added to the culture medium of rat peritoneal macrophages stimulated with ionophore A23187 was determined. (a) The substrate of phospholipase A(2) 1-octadecanoyl [C-14]eicosatetraenoyl-sn-glycero-3-phosphocholine ([C-14]20:4-GPC) was added to the culture medium. In macrophages + extracellular fluids, its hydrolysis at the 2-position, produced [C-14]non-phosphorous lipids which reached 12% of the dose at 0.14 mu M, 73% at 0.9 and > 90% at 1.6 mu M; in experiments where macrophages and extracellular fluids were analyzed separately, decyloctyl-GPC initially added at 4 mu M, significantly inhibited the release of [C-14]fatty acids and the eicosanoid synthesis, demonstrating its ability to inhibit secreted and/or intracellular phospholipases A(2). (b) Extracellular fluids were separated from the macrophages andincubated with [C-14]20:4-GPC: 48% of the dose was hydrolyzed by extracellular fluid-associated secreted phospholipase A(2) and decyloctyl-GPC at 3 mu M, reduced this hydrolysis by 50%. (c) [H-3]arachidonic acid ([H-3]20:4) was added to the culture medium and was esterified in the macrophage membrane phospholipids. Activation of intracellular phospholipase A(2) induced the release of [H-3] fatty acids and eicosanoidsynthesis. These releases were inhibited by 50% with decyloctyl-GPC added at 4 mu M. (d) [H-3]20:4 and [C-14]20:4-GPC were added to the culture medium of the macrophages. [3H] and [C-14] fatty acids and eicosanoids were released in macrophages or extracellular fluids. They were significantly reduced by the phospholipid analogue added at 4 mu M. Itis concluded that secreted and intracellular phospholipases A(2) wereboth inhibited by decyloctyl-GPC which extensively reduced the 20:4 release from exogenous and membrane phospholipids and therefore eicosanoid synthesis. (C) 1998 Elsevier, Paris.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/12/20 alle ore 14:30:44