Induction of prostaglandin endoperoxide synthase‐2 in human monocytes associated with cyclo‐oxygenase‐dependent F2‐isoprostane formation

Article date: July 1996

By: Paola Patrignani, Giovanna Santini, Maria R. Panara, Maria G. Sciulli, Anita Greco, Maria T. Rotondo, Maria Giamberardino, Jacques Maclouf, Giovanni Ciabattoni, Carlo Patrono, in Volume 118, Issue 5, pages 1285-1293

The isoprostane 8‐epi‐prostaglandin (PG)F is produced by free radical‐catalyzed peroxidation of arachidonic acid. It may also be formed as a minor product of the cyclo‐oxygenase activity of platelet PGH synthase (PGHS)‐1. We investigated 8‐epi‐PGF production associated with induction of the human monocyte PGHS‐2 and its pharmacological modulation.

Heparinized whole blood samples were drawn from healthy volunteers, 48 h following oral dosing with aspirin 300 mg to suppress platelet cyclo‐oxygenase activity. One ml aliquots were incubated with lipopolysaccharide (LPS: 0.1–50 μg ml−1) for 0–24 h at 37°C. PGE2 and 8‐epi‐PGF were measured in separated plasma by radioimmunoassay and enzyme immunoassay techniques.

Levels of both eicosanoids were undetectable (i.e. < 60 pg ml−1) at time 0. LPS induced the formation of PGE2 and 8‐epi‐PGF in a time‐ and concentration‐dependent fashion, coincident with the induction of PGHS‐2 detected by Western blot analysis of monocyte lysates. After 24 h at 10 μg ml−1 LPS, immunoreactive PGE2 and 8‐epi‐PGF averaged 10,480 ± 4,643 and 295 ± 140 pg ml−1 (mean ± s.d., n = 6), respectively.

Dexamethasone and 5‐methanesulphonamido‐6‐(2, 4‐difluorothiophenyl)‐1‐indanone (L‐745,337), a selective inhibitor of the cyclo‐oxygenase activity of PGHS‐2, reduced PGE2 and 8‐epi‐PGF production in response to LPS.

Isolated monocytes produced PGE2 and 8‐epi‐PGF in response to LPS (10 μg ml−1) in a time‐dependent fashion. Monocyte PGE2 and 8‐epi‐PGF production was largely prevented by dexamethasone (2 μm) and cycloheximide (10 μg ml−1) in association with suppression of PGHS‐2 but not of PGHS‐1 expression.

We conclude that the induction of PGHS‐2 in human monocytes is associated with cyclo‐oxygenase‐dependent generation of the vasoconstrictor and platelet‐agonist 8‐epi‐PGF.

The isoprostane 8‐epi‐prostaglandin (PG)F is produced by free radical‐catalyzed peroxidation of arachidonic acid. It may also be formed as a minor product of the cyclo‐oxygenase activity of platelet PGH synthase (PGHS)‐1. We investigated 8‐epi‐PGF production associated with induction of the human monocyte PGHS‐2 and its pharmacological modulation.

Heparinized whole blood samples were drawn from healthy volunteers, 48 h following oral dosing with aspirin 300 mg to suppress platelet cyclo‐oxygenase activity. One ml aliquots were incubated with lipopolysaccharide (LPS: 0.1–50 μg ml−1) for 0–24 h at 37°C. PGE2 and 8‐epi‐PGF were measured in separated plasma by radioimmunoassay and enzyme immunoassay techniques.

Levels of both eicosanoids were undetectable (i.e. < 60 pg ml−1) at time 0. LPS induced the formation of PGE2 and 8‐epi‐PGF in a time‐ and concentration‐dependent fashion, coincident with the induction of PGHS‐2 detected by Western blot analysis of monocyte lysates. After 24 h at 10 μg ml−1 LPS, immunoreactive PGE2 and 8‐epi‐PGF averaged 10,480 ± 4,643 and 295 ± 140 pg ml−1 (mean ± s.d., n = 6), respectively.

Dexamethasone and 5‐methanesulphonamido‐6‐(2, 4‐difluorothiophenyl)‐1‐indanone (L‐745,337), a selective inhibitor of the cyclo‐oxygenase activity of PGHS‐2, reduced PGE2 and 8‐epi‐PGF production in response to LPS.

Isolated monocytes produced PGE2 and 8‐epi‐PGF in response to LPS (10 μg ml−1) in a time‐dependent fashion. Monocyte PGE2 and 8‐epi‐PGF production was largely prevented by dexamethasone (2 μm) and cycloheximide (10 μg ml−1) in association with suppression of PGHS‐2 but not of PGHS‐1 expression.

We conclude that the induction of PGHS‐2 in human monocytes is associated with cyclo‐oxygenase‐dependent generation of the vasoconstrictor and platelet‐agonist 8‐epi‐PGF.

DOI: 10.1111/j.1476-5381.1996.tb15535.x

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