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Planta Med 2011; 77(13): 1504-1511
DOI: 10.1055/s-0030-1270762
Biological and Pharmacological Activity
Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

Effects of Flavonoids on Prostaglandin E2 Production and on COX-2 and mPGES-1 Expressions in Activated Macrophages

Mari Hämäläinen1 , Riina Nieminen1 , M. Zaini Asmawi1 , 2 , Pia Vuorela3 , Heikki Vapaatalo4 , Eeva Moilanen1
  • 1The Immunopharmacology Research Group, University of Tampere, School of Medicine and Tampere University Hospital, Tampere, Finland
  • 2School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia
  • 3Pharmaceutical Sciences, Department of Biosciences, Åbo Akademi University, Turku, Finland
  • 4Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland
Further Information

Publication History

received May 28, 2010 revised January 19, 2011

accepted January 21, 2011

Publication Date:
21 February 2011 (online)

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Abstract

Prostaglandin E2 (PGE2) has a central role in inflammation and both cyclooxygenase-2 (COX-2) and prostaglandin E synthases are critical enzymes in its synthesis. In inflammation, bacterial products and cytokines enhance the expression of COX-2 and inducible microsomal prostaglandin E synthase-1 (mPGES-1) which are functionally coupled to result in increased PGE2 formation in macrophages and tissue cells. In the present study, we systematically investigated the effects of 26 naturally occurring flavonoids on PGE2 production and on COX-2 and mPGES-1 expression in activated macrophages. Twelve flavonoids, i.e., flavone, luteolin-7-glucoside, kaempferol, isorhamnetin, morin, quercetin, naringenin, taxifolin, pelargonidin, daidzein, genistein, and genistin effectively inhibited lipopolysaccharide (LPS)–induced PGE2 production. Four flavonoids (flavone, isorhamnetin, daidzein, and genistein) inhibited significantly LPS-induced COX-2 expression, while mPGES-1 expression was downregulated by kaempferol and isorhamnetin. The present study characterizes the effects of flavonoids on PGE2 production and on COX-2 and mPGES-1 expression in activated macrophages. The results add to our knowledge of the anti-inflammatory actions of flavonoids and introduce kaempferol and isorhamnetin as compounds capable of downregulating the expression of mPGES-1.

Key words

flavonoids - prostaglandin E2 - cyclooxygenase-2 - prostaglandin E synthase - inflammation - macrophages

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Prof. Eeva Moilanen

The Immunopharmacology Research Group
School of Medicine
University of Tampere

33014 Tampere

Finland

Phone: +35 83 35 51 67 41

Fax: +35 83 35 51 80 82

Email: eeva.moilanen@uta.fi

    www.thieme-connect.de/ejournals/toc/plantamedica
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