The marine product petrosaspongiolide M is a novel inhibitor of phospholipase A(2) (PLA(2)), showing selectivity for secretory PLA, Versus cytosolic PLA(2), with a potency on the human synovial enzyme (group II) similar to that of manoalide. This compound was more potent than manoalide on bee venom PLA, (group III) and had no effect on group I enzymes (Naja naja and porcine pancreatic PLA(2)). Inhibition of PLA(2) was also observed in vivo in the zymosan-injected rat air pouch, on the secretory enzyme accumulated in the pouch exudate. Petrosaspongiolide M decreased carrageenan paw edema in mice after the oral administration of 5, 10, or 20 mg/kg. This marine metabolite (0.01-1.0 mu mol/pouch) induced a dose-dependent reduction in the levels of prostaglandin (PG)E-2, leukotriene B-4, and tumor necrosis factor-alpha in the mouse air pouch injected with zymosan 4 h after the stimulus. It also had a weaker effect on cell migration. The inflammatory response of adjuvant arthritis was reduced by petrosaspongiolide M, which also inhibited leukotriene B-4 levels in serum and PGE(2) levels in paw homogenates. In contrast with indomethacin, this marine compound did not reduce PGE(2) levels in stomach homogenates. Petrosaspongiolide M is a new inhibitor of secretory PLA(2) in vitro and in vivo, with anti-inflammatory properties in acute and chronic inflammation.

Effects of Petrosaspongiolide M, a Novel Human Synovial Phospholipase A2 Inhibitor, on Acute and Chronic Inflammation / P., GARCIA PASTOR; Randazzo, Antonio; LUIGI GOMEZ, Paloma; MARIA J., Alcaraz; M., Paya. - In: THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. - ISSN 0022-3565. - STAMPA. - 289:1(1999), pp. 166-172.

Effects of Petrosaspongiolide M, a Novel Human Synovial Phospholipase A2 Inhibitor, on Acute and Chronic Inflammation

RANDAZZO, ANTONIO;
1999

Abstract

The marine product petrosaspongiolide M is a novel inhibitor of phospholipase A(2) (PLA(2)), showing selectivity for secretory PLA, Versus cytosolic PLA(2), with a potency on the human synovial enzyme (group II) similar to that of manoalide. This compound was more potent than manoalide on bee venom PLA, (group III) and had no effect on group I enzymes (Naja naja and porcine pancreatic PLA(2)). Inhibition of PLA(2) was also observed in vivo in the zymosan-injected rat air pouch, on the secretory enzyme accumulated in the pouch exudate. Petrosaspongiolide M decreased carrageenan paw edema in mice after the oral administration of 5, 10, or 20 mg/kg. This marine metabolite (0.01-1.0 mu mol/pouch) induced a dose-dependent reduction in the levels of prostaglandin (PG)E-2, leukotriene B-4, and tumor necrosis factor-alpha in the mouse air pouch injected with zymosan 4 h after the stimulus. It also had a weaker effect on cell migration. The inflammatory response of adjuvant arthritis was reduced by petrosaspongiolide M, which also inhibited leukotriene B-4 levels in serum and PGE(2) levels in paw homogenates. In contrast with indomethacin, this marine compound did not reduce PGE(2) levels in stomach homogenates. Petrosaspongiolide M is a new inhibitor of secretory PLA(2) in vitro and in vivo, with anti-inflammatory properties in acute and chronic inflammation.
1999
Effects of Petrosaspongiolide M, a Novel Human Synovial Phospholipase A2 Inhibitor, on Acute and Chronic Inflammation / P., GARCIA PASTOR; Randazzo, Antonio; LUIGI GOMEZ, Paloma; MARIA J., Alcaraz; M., Paya. - In: THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. - ISSN 0022-3565. - STAMPA. - 289:1(1999), pp. 166-172.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/205488
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