Identification of a new azoreductase driven prodrug from bardoxolone methyl and 5-aminosalicylate for the treatment of colitis in mice / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 545-550, 2021.
Article
Dans Anglais
| WPRIM
| ID: wpr-888784
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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Acide oléanolique
/
Nitroréductases
/
Promédicaments
/
Colite
/
Mésalazine
Limites du sujet:
Animaux
langue:
Anglais
Texte intégral:
Chinese Journal of Natural Medicines (English Ed.)
Année:
2021
Type:
Article
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