Development and Clinical Investigation of a Novel Natural Anti-inflammatory Product with Balanced Cox 1 and Cox 2 Activity

Vendor Workshop Sponsored by Metagenics, Inc. ~ Gastrointestinal toxicity of non-steroidal anti-inflammatory drugs (NSAIDs) is well documented, and a primary drawback in their long-term use. A common theme of NSAIDs efficacy is their non specific targeting of clycooxygenase (COX) enzymes resulting in inhibition and subsequent reduction in Prostaglandin H2 (PGH2) inflammatory derived eicosanoids. While inhibition of inflammatory cell (e.g., macrophage) COX enzyme activity to reduce PGH2 is desired, gastrointestinal cell COX enzyme inhibition is not, and results in the inability of GI cells to repair damage leading to ulceration and GI toxicity. In pursuit of a safer naturally derived anti-inflammatory agent, we designed a program to assess natural agents for selective and balanced Cox 2 vs. Cox 1 inhibition, and therefore anti-inflammatory efficacy with predicted low GI toxicity. Greater then 100 natural DSHEA ingredients with a history of safe use were screened for anti-inflammatory