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Original Paper

Investigations of Interactions of Chlormezanone Racemate and Its Enantiomers on Human Keratinocytes and Human Leucoytes in vitro

Wollina U.a · Hipler U.-C.b · Seeling A.c · Oelschläger H.c

Author affiliations

aDepartment of Dermatology, Academic Teaching Hospital Dresden-Friedrichstadt, Dresden; bDepartment of Dermatology and Dermatological Allergology and cInstitute of Pharmacy, Department of Pharmaceutical Chemistry, Friedrich-Schiller-University of Jena, Jena, Germany

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Skin Pharmacol Physiol 2005;18:132–138

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: May 11, 2004
Accepted: September 30, 2004
Published online: May 06, 2005
Issue release date: May – June

Number of Print Pages: 7
Number of Figures: 5
Number of Tables: 0

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: http://www.karger.com/SPP

Abstract

Chlormezanone is a centrally acting muscle relaxant introduced in human therapy as a racemic substance. The following investigation was performed in order to investigate whether the racemate and both enantiomers differ in their potential cytotoxicty in vitro. We investigated antiproliferative effects and cytotoxicity (PicoGreen and ATP assay) for human HaCaT keratinocytes, production of oxygen radicals (ROS) by human interleukin-3-stimulated leukocytes (Lucigenin assay) and production of sulfoleukotrienes (Cellular Antigen Stimulation Test – CAST) by human leukocytes. In the dosage range of 0.001 to 0.1 mg/ ml chlormezanone, no antiproliferative effects were measured with the racemate and both enantiomers. At 1.0 mg/ml, a decrease of proliferative activity was seen after 48 h incubation time of about 50% for the enantiomers and of about 80% for the racemate (PicoGreen) and 50% (enantiomers) or 21% (racemate) in the ATP assay, respectively. ROS production was significantly inhibited at concentrations ≤0.01 mg/ ml by the racemate and the (+)-enantiomer, whereas the (–)-enantiomer was less effective. There was no stimulation of sulfidoleukotrienes in human leukocytes by chlormezanone. Present data argue for absence of significant cytotoxicity against human HaCaT keratinocytes and a dose-dependent suppression of ROS production by human leukocytes that is not uniform among the racemate and its enantiomers.

© 2005 S. Karger AG, Basel


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: May 11, 2004
Accepted: September 30, 2004
Published online: May 06, 2005
Issue release date: May – June

Number of Print Pages: 7
Number of Figures: 5
Number of Tables: 0

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: http://www.karger.com/SPP


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