期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 43, 期 8, 页码 1785-1790出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2007.11.004
关键词
acetylsalicylic acid; oligo(3-hydroxybutanoate); polymer-drug conjugate; antiproliferutive effect
资金
- Development of Polish Pharmacology and Medicine Foundation [20/2002]
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 2 g of the conjugate (equivalent to 0.6 g of pure aspirin) per kg of body weight did not exhibit toxic effects. (C) 2007 Elsevier Masson SAS. All fights reserved.
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