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Iranian Journal of Basic Medical Sciences، جلد ۲۲، شماره ۱۲، صفحات ۱۴۵۲-۱۴۶۱
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| عنوان فارسی |
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| چکیده فارسی مقاله |
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| کلیدواژه‌های فارسی مقاله |
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| عنوان انگلیسی |
Synthesis and evaluation of a prodrug of 5-aminosalicylic acid for the treatment of ulcerative colitis |
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| چکیده انگلیسی مقاله |
Objective(s): This study is aimed to design and synthesize a prodrug of 5-aminosalicylic acid and evaluate its ameliorative effect on experimental ulcerative colitis (UC).Materials and Methods: 5-Aminosalicylic acid-alanine (5-ASA-ALA) was synthesized and characterized. Its stability study was conducted in rat plasma and in the gastrointestinal tract environment, its transport characteristic was assessed using the Caco-2 cells. Its colon-targeting property was evaluated by the pharmacokinetic study, and incubation studies. A series of indicators were used to investigate its therapeutic effect on experimental colitis, including the survival rate and body weight of mice, the disease activity index (DAI), the colonic damage score and colon index, the myeloperoxidase (MPO) activity and the levels of malondialdehyde (MDA), total superoxide dismutase (SOD), glutathione (GSH) and glutathione peroxidase (GSH-Px) in colonic tissues.Results: 5-ASA-ALA was barely absorbed in the Caco-2 monolayer or into the rat blood. It was remarkably stable when incubated in the upper gastrointestinal tract, while gradually hydrolyzed in the colon of rats. When orally administered to mice, 5-ASA-ALA had significantly greater therapeutic effect on colitis than the positive control. Conclusion: 5-ASA-ALA is demonstrated to be a promising oral colon-targeting prodrug of 5-ASA and has potential application in UC treatment. |
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| کلیدواژه‌های انگلیسی مقاله |
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| نویسندگان مقاله |
| Yan Yan
School of Pharmacy, Xi’an Jiaotong University, Xi’an, Shaanxi, China
| FengLing Ren
School of Public Health, Xi’an Jiaotong University, Xi’an, Shaanxi, China
| Pengchong Wang
School of Pharmacy, Xi’an Jiaotong University, Xi’an, Shaanxi, China
| Ying Sun
School of Pharmacy, Xi’an Jiaotong University, Xi’an, Shaanxi, China
| Jianfeng Xing
School of Pharmacy, Xi’an Jiaotong University, Xi’an, Shaanxi, China
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| نشانی اینترنتی |
http://ijbms.mums.ac.ir/article_13991.html |
| فایل مقاله |
اشکال در دسترسی به فایل - ./files/site1/rds_journals/87/article-87-2060560.pdf |
| کد مقاله (doi) |
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| زبان مقاله منتشر شده |
en |
| موضوعات مقاله منتشر شده |
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| نوع مقاله منتشر شده |
Original Article |
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