Selective inhibition of COX-2 by a standardized CO2 extract of Humulus lupulus in vitro and its activity in a mouse model of zymosan-induced arthritis

Planta medica
Sander HougeeMaarten A Hoijer

Abstract

A standardized CO(2) extract from Humulus lupulus L. (hop extract) was investigated for its selective COX-1/2 inhibitory properties. An in vitro model of inflammation using lipopolysaccharide (LPS)-stimulated human peripheral blood mononuclear cells (PBMC) was used as a model to investigate the effect of hop extract on PGE(2) production. COX-1/2 selective inhibition by the hop extract was investigated in a COX-1 whole blood assay (WBA) and a COX-2 WBA. To evaluate the in vivo activity of hop extract, it was administered orally to C57BL/6 mice in which inflammation of the right joint was induced by injecting zymosan intra-articularly. Ex vivo PGE(2) production of LPS-stimulated blood cells was determined. Also, the effect of hop extract on healthy and arthritic cartilage was investigated as well as effects on inflammatory joint swelling. Hop extract inhibited PGE(2) production by LPS-stimulated PBMC without compromising the metabolic activity of these cells. Furthermore, hop extract showed a decline in PGE(2) production in the COX-2 whole blood assay (WBA) with an IC(50) of 20.4 microg/mL, while in the COX-1 WBA no inhibition of PGE(2) production was observed. This indicates a COX-2 selective inhibition. The COX-1 inhibitor SC-5...Continue Reading

Citations

May 18, 2016·International Journal of Endocrinology·Maëlle LempereurDominique Gallo
May 23, 2015·Bioscience, Biotechnology, and Biochemistry·Yoshimasa TaniguchiMikio Katayama
Sep 30, 2016·Pharmacological Reviews·Birgit M DietzJudy L Bolton
Feb 10, 2009·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Naoto YamaguchiMitsunori Ono
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Mar 25, 2010·Journal of Agricultural and Food Chemistry·Ko CattoorArne Heyerick
Jul 3, 2021·Nutrients·Gustavo Ignacio Vazquez-CervantesBenjamín Pineda

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