[The biotransformation of cui xing ning in the isolated perfused rat liver].

ABSTRACT

Similar to eserine, Cui Xing Ning [CXN),5-(1,3,3-trimethylindoline) N, N-dimethyl carbamate] is a choline esterase (ChE) inhibitor. The biotransformation of CXN, which had been studied in vivo and in vitro unsuccessfully, was studied by using isolated perfused rat liver (IPL) method. Six metabolites of CXN from the perfusate were separated by HPLC, and identified with MS, 1HNMR or compared with the authentic compounds. Metabolite I is unchanged CXN, the other are oxidized metabolites. Most of the metabolites lost their activities of ChE inhibition strikingly except metabolite III which retained the 2-position unchanged. The toxicities of some metabolites (II,V) decreased obviously.