AI Article Synopsis
- A mutual azo prodrug of 5-aminosalicylic acid and l-tyrosine was created to deliver medication specifically to inflamed gut tissue in conditions like inflammatory bowel disease.
- The structure of the prodrug was confirmed using methods like elemental analysis and spectroscopy techniques (IR and NMR).
- In tests with rat feces, the prodrug showed a rapid release of 5-aminosalicylic acid and demonstrated a therapeutic effect similar to the standard drug sulfasalazine in treating induced colitis in rats.
Article Abstract
Mutual azo prodrug of 5-aminosalicylic acid with l-tyrosine was synthesized by coupling l-tyrosine with salicylic acid, for targeted drug delivery to the inflamed gut tissue in inflammatory bowel disease. The structure was confirmed by elemental analysis, IR and NMR spectroscopy. In vitro kinetic studies in rat fecal matter showed 87.18% release of 5-aminosalicylic acid with a half-life of 140.28min, following first order kinetics. Therapeutic efficacy of the carrier system and the mitigating effect of the azo conjugate were evaluated in trinitrobenzenesulfonic acid-induced experimental colitis model. Myeloperoxidase activity was determined by the method of Krawisz et al. The synthesized prodrug was found to produce comparable mitigating effect as that of sulfasalazine on colitis in rats.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2006.11.017 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Designing for medication adherence in inflammatory bowel disease: multi-disciplinary approaches for self-administrable biotherapeutics.
EClinicalMedicine
November 2024
Division of Gastroenterology, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA, USA.
Biotherapeutics are among the therapeutics that have revolutionized standard inflammatory bowel disease (IBD) treatment, which was previously limited to mesalamine, 5-aminosalicylic acid, corticosteroids, and classical immunosuppressants. Self-administrable biotherapeutics for IBD would enable home-based treatment and reduce the burden on medical infrastructure. Self-administration is made possible through subcutaneous injectable, oral, and rectal dosage forms.
View Article and Find Full Text PDFRole of 5-aminosalicylic acid in ulcerative colitis management in 8 Asian territories: a physician survey.
Intest Res
January 2025
Department of Medicine, School of Clinical Medicine, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong, China.
Clinical guidelines typically endorse conventional therapies such as 5-aminosalicylic acid (5-ASA) as the mainstay of ulcerative colitis management. However, the degree of adoption and application of guideline recommendations by physicians within Asia remains unclear. This study aims to understand the prescribing patterns of 5-ASA and implementation of current guideline recommendations across Asian clinical practice.
View Article and Find Full Text PDFAromatic compounds and organic acids identified from Ganoderma formosanum exhibit synergistic anti-melanogenic effects.
J Food Drug Anal
December 2024
Institute of Food Science Technology, National Taiwan University, No. 1, Sec. 4, Roosevelt Rd., Taipei, Taiwan, R.O.C.
This study reveals the anti-tyrosinase activity of Ganoderma formosanum extracts, pinpointing compounds including gluconic acid, mesalamine, L-pyroglutamic acid, esculetin, 5-hydroxyindole, and salicylic acid, as effective melanin production inhibitors in melanoma cells and zebrafish embryos. Furthermore, multiple molecular docking simulations provided insights into interactions between the identified compounds and tyrosinase, increasing binding affinity up to -16.36 kcal/mol.
View Article and Find Full Text PDFPrior Anti-TNF Exposure Is Associated with an Increased Risk of Short- and Long-Term Colectomy in Acute Severe Ulcerative Colitis.
Dig Dis Sci
January 2025
The Henry D. Janowitz Division of Gastroenterology, Department of Medicine, Icahn School of Medicine at Mount Sinai, 1 Gustave L. Levy Place, New York, NY, 10029, USA.
Background: Acute severe ulcerative colitis (ASUC) affects up to 25% of patients with UC and is associated with an increased risk of colectomy. Despite improvements in medical management, individual patient prognostication and risk stratification in ASUC remains challenging. We explored clinical, biochemical, and endoscopic factors as potential predictors for colectomy in patients hospitalized with ASUC.
View Article and Find Full Text PDFHealth-related quality of life, work productivity, and persisting challenges in treated ulcerative colitis patients: a Japanese National Health and Wellness Survey.
Intest Res
January 2025
Bristol Myers Squibb, Tokyo, Japan.
Article Synopsis
- The study highlights the ongoing challenges faced by ulcerative colitis (UC) patients in Japan despite existing treatments, focusing on their health-related quality of life (HRQoL) and productivity losses.
- About 83.6% of participants were on non-biologic treatments, with a significant portion reporting persistent symptoms and a notable percentage experiencing anxiety and depression, which negatively impacted their work productivity by an average of 29.3%.
- The results emphasize the need for new interventions to improve treatment outcomes as many patients still experience high disease burden and indirect costs.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!