Oligo(3-hydroxybutanoate) conjugates with acetylsalicylic acid and their antitumour activity.

摘要

In this paper we discuss the anticancer activity of acetylsalicylic acid with oligo(3-hydroxybutanoate) conjugates, their characteristics and in vitro biological evaluation. Acetylsalicylic acid (aspirin) attached via hydrolysable ester bonds to non-toxic well-defined 3-hydroxybutanoic acid oligomers shows novel method of drug modification. The resulting conjugates were more effective than aspirin in growth inhibition of human colon adenocarcinoma cells HT-29 and human colon carcinoma cells HCT 116 in vitro. Treatment of rats with doses as high as 2g of the conjugate (equivalent to 0.6g of pure aspirin) per kg of body weight did not exhibit toxic effects.