{Reference Type}: Journal Article
{Title}: Identification of a new azoreductase driven prodrug from bardoxolone methyl and 5-aminosalicylate for the treatment of colitis in mice.
{Author}: Qiao X;Gong Y;Mou Y;Zhang YH;Huang ZJ;Wen XD;
{Journal}: Chin J Nat Med
{Volume}: 19
{Issue}: 7
{Year}: Jul 2021
{Factor}: 3.887
{DOI}: 10.1016/S1875-5364(21)60055-9
{Abstract}: For local treatment of ulcerative colitis, a new azoreductase driven prodrug CDDO-AZO from bardoxolone methyl (CDDO-Me) and 5-aminosalicylate (5-ASA) was designed, synthesized and biologically evaluated. It is proposed that orally administrated CDDO-AZO is stable before reaching the colon, while it can also be triggered by the presence of azoreductase in the colon to fragment into CDDO-Me and 5-ASA, generating potent anti-colitis effects. Superior to olsalazine (OLS, a clinically used drug for ulcerative colitis) and CDDO-Me plus 5-ASA, CDDO-AZO significantly attenuated inflammatory colitis symptoms in DSS-induced chronic colitis mice, which suggested that CDDO-AZO may be a promising anti-ulcerative colitis agent.