Flemming, Marcel and Kraus, Birgit and Rascle, Anne and Juergenliemk, Guido and Fuchs, Simone and Fuerst, Robert and Heilmann, Joerg (2015) Revisited anti-inflammatory activity of matricine in vitro: Comparison with chamazulene. FITOTERAPIA, 106. pp. 122-128. ISSN 0367-326X, 1873-6971
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The proazulene matricine (1) is present in chamomile flower heads and has been proven to exhibit strong in vivo anti-inflammatory activity. In contrast to other secondary metabolites in chamomile preparations like its degradation product chamazulene (2), no plausible targets have been found to explain this activity. Therefore we revisited 1 regarding its in vitro anti-inflammatory activity in cellular and molecular studies. Using ICAM-1 as a marker for NF-kappa B activation, it was shown that ICAM-1 protein expression induced by TNF-alpha and LPS, but not by IFN-gamma, was remarkably inhibited by 1 in endothelial cells (HMEC-1). Inhibition was concentration-dependent in a micromolar range (10-75 mu M) and did not involve cytotoxic effects. At 75 mu M expression of the adhesion molecule ICAM-1 was down to 52.7 +/- 3.3% and 20.4 +/- 1.8% of control in TNF-alpha and LPS-stimulated HMEC-1, respectively. In contrast, 2 showed no activity. Quantitative RT-PCR experiments revealed that TNF-alpha-induced expression of the ICAM-1 gene was also reduced by 1 in a concentration-dependent manner, reaching 32.3 +/- 62% of control at 100 mu M matricine. Additional functional assays (NF-kappa B promotor activity and cytoplasm to nucleus translocation) confirmed the inhibitory effect of 1 on NF-kappa B signaling. Despite the fact that 1 lacks an alpha,beta-unsaturated carbonyl and is thus not able to act via a Michael reaction with electron rich SH groups of functional biological molecules, data gave strong evidence that 1 inhibits NF-kappa B transcriptional activity in endothelial cells by an hitherto unknown mechanism and this may contribute to its well-known anti-inflammatory activity in vivo. (C) 2015 Elsevier B.V. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NF-KAPPA-B; PHARMACOLOGICAL INVESTIGATIONS; SESQUITERPENE LACTONES; ADHESION MOLECULES; ICAM-1 EXPRESSION; ENDOTHELIAL-CELLS; BISABOLOL-OXIDES; TRANSCRIPTION; CHAMOMILE; (-)-ALPHA-BISABOLOL; Matricaria recutita; Matricine; Chamazulene; Anti-inflammatory activity; ICAM-1; NF-kappa B |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Medicine > Lehrstuhl für Immunologie Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 06 Jun 2019 10:21 |
| Last Modified: | 06 Jun 2019 10:21 |
| URI: | https://pred.uni-regensburg.de/id/eprint/4716 |
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