In vitro and ex vivo cyclooxygenase inhibition by a hops extract.
While there has been much research on botanical materials as potential pain-relieving Cox inhibitors, it has not yet been demonstrated that oral consumption of botanical agents can inhibit Cox-2 activity in humans. In particular it would be of interest to determine whether any botanical anti-inflammatory has Cox-1-sparing activity, in order to reduce the risk of gastrointestinal side effects. This two-stage study was designed to first screen a variety of botanicals in vitro, and then to select one or more promising agents to test in human volunteers. Method: Seventeen botanical agents, putative anti-inflammatories or pain-relievers all, were evaluated in vitro for Cox-1 and -2 inhibitory potency and selectivity using a caco-2 cell line with ibuprofen as an active control. A promising compound, a hops extract high in alpha acids, showed a Cox-2/Cox-1 IC50 selectivity ratio of 0.06, compared to 4.2 for ibuprofen. Two different formulations of a standardized hops extract (resin and powder) were compared with ibuprofen in a double-blind, randomized, ex vivo study. Subjects consumed hops powder extract, hops resin extract, or ibuprofen, and provided blood samples before and at intervals for 9 h following the first dose. Plasma was extracted and analyzed in a validated Cox-1 and -2 inhibition assay. Results: There were no differences between active treatments or ibuprofen control in Cox-2 inhibitory action, as indicated by 9-hour Cox-2 Area over the Inhibition Curve (AOC); however, hops powder or hops resin extract produced a 9-hour Cox-1 / Cox-2 AOC ratio of about 0.4 (i.e., some degree of Cox-1 sparing), compared to 1.5 for ibuprofen (i.e. no Cox-1 sparing). Conclusion: Hops exhibited Cox-2 inhibition over 9 hours equivalent to ibuprofen 400 mg but had significant Cox-1 sparing activity relative to ibuprofen. Hops extracts may represent a safe alternative to ibuprofen for non-prescription anti-inflammation.[1]References
- In vitro and ex vivo cyclooxygenase inhibition by a hops extract. Lemay, M., Murray, M.A., Davies, A., Roh-Schmidt, H., Randolph, R.K. Asia Pacific journal of clinical nutrition. (2004) [Pubmed]
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