Oligo(3-hydroxybutanoate) conjugates with acetylsalicylic acid and their antitumour activity.
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.
Juzwa
Maria
M
Centre of Polymer and Carbon Materials, Polish Academy of Sciences, M. Skłodowskiej-Curie 34, Zabrze 41-819, Poland.
Rusin
Aleksandra
A
Zawidlak-Wegrzyńska
Barbara
B
Krawczyk
Zdzisław
Z
Obara
Ilona
I
Jedliński
Zbigniew
Z
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001241:Aspirin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D006885:Hydroxybutyrates / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011091:Polyesters / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship; D000094122:Polyhydroxybutyrates
D000970:Antineoplastic Agents; D001241:Aspirin; D006885:Hydroxybutyrates; D011091:Polyesters; C003182:poly-beta-hydroxybutyrate; D000094122:Polyhydroxybutyrates