Is N-acetylation of 5-aminosalicylic acid reversible in man?

Inhibitory effect of flavonoids on N-acetylation of 5-aminosalicylic acid in cultured rat hepatocytes.

5-Aminosalicylic acid (5-ASA) is an effective drug for the treatment of ulcerative colitis and Crohn's disease. A large group of flavonoids was investigated for their inhibitory effects on the N-acetyl-conjugation of 5-ASA in rat hepatocytes and subcellular preparations. When added to cultured hepatocytes, some flavonoids inhibited the production of N-acetyl-5-aminosalicylic acid (5-AcASA) with...

Electrochemical Synthesis of 5-Aminosalicylic Acid from 5- Nitrosalicylic Acid in Alkaline Media

5-Aminosalicylic acid (5-ASA) is currently prepared by electrochemical reduction of 5-nitrosalicylic acid (5-NSA) in acidic media. In this work, electrolytic reduction of 5-NSA in alkaline media is presented. Reactionconditions and parameters such as anode and cathode electrodes, electrolyte type, reaction time, temperature,current, and the pH for isolation of product are investigated. The yiel...

Identification and functional characterization of arylamine N-acetyltransferases in eubacteria: evidence for highly selective acetylation of 5-aminosalicylic acid.

Arylamine N-acetyltransferase activity has been described in various bacterial species. Bacterial N-acetyltransferases, including those from bacteria of the gut flora, may be involved in the metabolism of xenobiotics, thereby exerting physiopathological effects. We characterized these enzymes further by steady-state kinetics, time-dependent inhibition, and DNA hybridization in 40 species, mostl...

aminosalicylic acid to 5-aminosalicylic acid in topical treatment of ulcerative colitis. Digestion

Nephrotoxic lesions from 5-aminosalicylic Acid.

5-Aminosalicylic acid given to rats as a single intravenous injection led to necrosis of the proximal convoluted tubules and of the renal papilla. These two lesions developed at the same time and the cortical lesions did not appear to be a consequence of the renal papillary necrosis. Since the compound possesses the molecular structure both of a phenacetin derivative and of a salicylate these o...