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Identification of a new azoreductase driven prodrug from bardoxolone methyl and 5-aminosalicylate for the treatment of colitis in mice.
Qiao, Xin; Gong, Yan; Mou, Yi; Zhang, Yi-Hua; Huang, Zhang-Jian; Wen, Xiao-Dong.
Afiliación
  • Qiao X; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
  • Gong Y; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, China Pharmaceutical University, Nanjing 210009, China.
  • Mou Y; College of Pharmacy and Chemistry & Chemical Engineering, Taizhou University, Taizhou 225300, China.
  • Zhang YH; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, China Pharmaceutical University, Nanjing 210009, China.
  • Huang ZJ; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, China Pharmaceutical University, Nanjing 210009, China. Electronic address: cpudahuang@163.com.
  • Wen XD; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China. Electronic address: xiaodongwen@cpu.edu.cn.
Chin J Nat Med ; 19(7): 545-550, 2021 Jul.
Article en En | MEDLINE | ID: mdl-34247779
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácido Oleanólico / Profármacos / Colitis / Mesalamina Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: Chin J Nat Med Año: 2021 Tipo del documento: Article País de afiliación: China Pais de publicación: China
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácido Oleanólico / Profármacos / Colitis / Mesalamina Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: Chin J Nat Med Año: 2021 Tipo del documento: Article País de afiliación: China Pais de publicación: China