| Citation: | XIE Tong, Liang- Yan, Hao-Hai-Beng, Xie- Lin, Wang-An-Ji. Advances in study of metabolic activation of carboxyl-acid containing drugs by UGTsJ. 药学学报, 2009,44(11): 1193-1199. |
The metabolic transformation of the drugs containing carboxylic acid groups can lead to the formation of acyl glucuronide metabolites through catalysis by glucuronosyltransferase, and produce pro-acyl glucuronide intermediate metabolites with electronic activity. Then, protein or DNA adducts appeared after a series of non-enzyme or enzyme reactions. These adducts would change the protein activity and potentially lead to idiosyncratic and genotoxicity. In this paper, we discussed the chemical activity, drug-induced mechanisms, distribution and toxicity resulting from this metabolic activation for these drugs, and stated the status and prospects of research in this field.