ArticleIranian journal of basic medical sciences2019
Synthesis and evaluation of a prodrug of 5-aminosalicylic acid for the treatment of ulcerative colitis.
Article in Iranian journal of basic medical sciences, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Application of Chinese Medicine in Treatment of Ulcerative Colitis and Elucidation of Relevant Mechanisms.Chinese journal of integrative medicine · 2026Review
- Network pharmacology and experimental verification in vivo reveal the mechanism of Zhushao Granules against ulcerative colitis.Biological procedures online · 2025Article
- An Overview of Colon Specific Drug Delivery: Approaches and Evaluation Aspects.Current drug research reviews · 2025Review
- A Comprehensive Review of Challenges in Oral Drug Delivery Systems and Recent Advancements in Innovative Design Strategies.Current pharmaceutical design · 2025Review
- Comparable Toxicity of Surface-Modified TiOAntioxidants (Basel, Switzerland) · 2024Article
- Protective roles of vitamin C and 5-aminosalicylic acid on reproduction in acrylamide intoxicated male mice.Saudi journal of biological sciences · 2023Article
- Protective effect and mechanism insight of purified Antarctic kill phospholipids against mice ulcerative colitis combined with bioinformatics.Natural products and bioprospecting · 2023Article
- Mucoadhesive Nanoparticles Enhance the Therapeutic Effect of Dexamethasone on Experimental Ulcerative Colitis by the Local Administration as an Enema.Drug design, development and therapy · 2023Article
- Preparation and Characterization of a Novel Multiparticulate Dosage Form Carrying Budesonide-Loaded Chitosan Nanoparticles to Enhance the Efficiency of Pellets in the Colon.Pharmaceutics · 2022Article
- Anti-inflammatory Effect of a Novel Pectin Polysaccharide FromFrontiers in nutrition · 2022Article
- Myeloperoxidase Inhibitory and Antioxidant Activities of (Pharmaceuticals (Basel, Switzerland) · 2021Article
- Flower extract ofIranian journal of basic medical sciences · 2021Article
- Synthesis of a novel PEGylated colon-specific azo-based 4- aminosalicylic acid prodrug.Iranian journal of basic medical sciences · 2020Article
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectivesThis 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
methods5-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.
results5-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.
conclusion5-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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