New mechanisms of action of 5-aminosalicylic acid: PPARy: how it decreases inflammation and cancer

摘要

The oldest of the drugs used in ulcerative colitis (UC) therapy, sulfasalazine (5-aminosalicylic acid (5-ASA) linked to sulfapyridine by an azo bond), was for many years the standard therapy after pivotal induction of remission and maintenance trials in the 1960s . However, up to one-third of patients are intolerant of sulfasalazine, the most common adverse effects being nausea, vomiting, dyspepsia, malaise or headaches. Less common effects include blood dyscrasias, male infertility and skin rashes. These adverse effects are considered to be due to the sulfapyridine moiety. This has become apparent since it was recognized in 1977 that the therapeutic effect of sulfasalazine is due to the release of the 5-ASA moiety (Figure 1) into the lumen by the action of gut flora in the distal ileum and colon.