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
in English
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Oleanolic Acid
/
Nitroreductases
/
Prodrugs
/
Colitis
/
Mesalamine
Limits:
Animals
Language:
English
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2021
Type:
Article
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