BIOSYNTHESIS AND ISOLATION OF AN ETHER GLUCURONIDE OF AZIDOTHYMIDINE FROM RAT BILE BY THIN-LAYER CHROMATOGRAPHY

A rapid, simple, and inexpensive method for the biosynthesis and isola tion of o-3'-deoxy-5'-O-beta-D-glucopyranuronosylthymidine (GAZT), a m ain metabolite of 3'-azido-3'-deoxythymidine (AZT) in humans, is descr ibed. Bile from cannulated rat liver, with recirculating perfusate con taining AZT, was used as a source of GAZT. After liver perfusion GAZT was isolated from bile by preparative TLC. Development with 80 % aceto nitrile gave only one major band, R(f) = 0.48. Subsequent purification of this band by analytical TLC gave this metabolite in relatively hig h purity. Approximately 2 mg pure GAZT can be obtained from one liver perfusion by this procedure within several hours.