In vitro inhibition of human polymorphonuclear cell function by cloricromene

F. Bertocchi, F. Breviario, P. Proserpio, Ji Ming Wang, P. Ghezzi, R. A. Travagh, M. Prosdocimi, E. Dejana

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Abstract

Cloricromene, a coumarin derivative with antiaggregating and vasodilating properties, was tested in vitro on polymorphonuclear cell (PMN) adhesion to the endothelium, superoxide anion generation and chemotaxis. PMN adhesion was measured using cultured human umbilical vein endothelial cells (EC) either untreated or previously activated with interleukin-1 (IL-1). Cloricromene (5-50 μM) induced dose-related inhibition of PMN adhesion to untreated and IL-1 treated EC. Cloricromene also inhibited PMN superoxide generation induced by the tumor promoter 12-O-tetradecanoyl-phorbol-13-acetate (TPA) or by N-formyl-methionyl-leucyl-phenylalanine (FMLP). PMN and monocyte chemotaxis was evaluated by a modification of the Boyden chamber technique. Cloricromene inhibited both types of cell motility induced by FMLP in a concentration-dependent fashion. The major cloricromene metabolite (cloricromene acid) had no effect on any of the biological parameters studied up to a concentration of 500μM. HPLC measurement showed that cloricromene accumulated in PMN within a few minutes and levels of the drug were still high after 60 min. In contrast its acid metabolite was not taken up in a significant amount during incubation periods up to 60 min. We conclude that cloricromene inhibits a series of PMN activities in vitro. This effect might be of pharmacological interest in view of the role of PMN activation in different pathophysiological conditions.

Original languageEnglish (US)
Pages (from-to)697-703
Number of pages7
JournalNaunyn-Schmiedeberg's Archives of Pharmacology
Volume339
Issue number6
DOIs
StatePublished - Jun 1989

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Cell Adhesion
Chemotaxis
Interleukin-1
Superoxides
methionyl-leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine
Coumarins
Acids
In Vitro Techniques
cloricromen
Inhibition (Psychology)
Human Umbilical Vein Endothelial Cells
Tetradecanoylphorbol Acetate
Carcinogens
Endothelium
Cell Movement
Monocytes
Endothelial Cells
High Pressure Liquid Chromatography
Pharmacology

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Bertocchi, F. ; Breviario, F. ; Proserpio, P. ; Wang, Ji Ming ; Ghezzi, P. ; Travagh, R. A. ; Prosdocimi, M. ; Dejana, E. / In vitro inhibition of human polymorphonuclear cell function by cloricromene. In: Naunyn-Schmiedeberg's Archives of Pharmacology. 1989 ; Vol. 339, No. 6. pp. 697-703.
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abstract = "Cloricromene, a coumarin derivative with antiaggregating and vasodilating properties, was tested in vitro on polymorphonuclear cell (PMN) adhesion to the endothelium, superoxide anion generation and chemotaxis. PMN adhesion was measured using cultured human umbilical vein endothelial cells (EC) either untreated or previously activated with interleukin-1 (IL-1). Cloricromene (5-50 μM) induced dose-related inhibition of PMN adhesion to untreated and IL-1 treated EC. Cloricromene also inhibited PMN superoxide generation induced by the tumor promoter 12-O-tetradecanoyl-phorbol-13-acetate (TPA) or by N-formyl-methionyl-leucyl-phenylalanine (FMLP). PMN and monocyte chemotaxis was evaluated by a modification of the Boyden chamber technique. Cloricromene inhibited both types of cell motility induced by FMLP in a concentration-dependent fashion. The major cloricromene metabolite (cloricromene acid) had no effect on any of the biological parameters studied up to a concentration of 500μM. HPLC measurement showed that cloricromene accumulated in PMN within a few minutes and levels of the drug were still high after 60 min. In contrast its acid metabolite was not taken up in a significant amount during incubation periods up to 60 min. We conclude that cloricromene inhibits a series of PMN activities in vitro. This effect might be of pharmacological interest in view of the role of PMN activation in different pathophysiological conditions.",
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Bertocchi, F, Breviario, F, Proserpio, P, Wang, JM, Ghezzi, P, Travagh, RA, Prosdocimi, M & Dejana, E 1989, 'In vitro inhibition of human polymorphonuclear cell function by cloricromene', Naunyn-Schmiedeberg's Archives of Pharmacology, vol. 339, no. 6, pp. 697-703. https://doi.org/10.1007/BF00168664

In vitro inhibition of human polymorphonuclear cell function by cloricromene. / Bertocchi, F.; Breviario, F.; Proserpio, P.; Wang, Ji Ming; Ghezzi, P.; Travagh, R. A.; Prosdocimi, M.; Dejana, E.

In: Naunyn-Schmiedeberg's Archives of Pharmacology, Vol. 339, No. 6, 06.1989, p. 697-703.

Research output: Contribution to journalArticle

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T1 - In vitro inhibition of human polymorphonuclear cell function by cloricromene

AU - Bertocchi, F.

AU - Breviario, F.

AU - Proserpio, P.

AU - Wang, Ji Ming

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AU - Travagh, R. A.

AU - Prosdocimi, M.

AU - Dejana, E.

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