Low level toxicity and antitumor activity of butyric mono- and polyester monosaccharide derivates in mice.
This study compares the antitumor activity of five mono- and polyesters of n-butyric acid derived from monosaccharides in the murine model of Crocker 180 TG Sarcoma. Tumor incidence at ten days, mean survival time and final survival rate were significantly affected in all cases. Combined treatment by butyric esters, alpha/beta interferon (IFN) and/or Corynebacterium parvum used as immunestimulator improved the antitumor protection. Studies of acute toxicity in mice, performed by i.p. and oral routes, showed the low toxicity of butyric esters, which were devoid of detectable side effects with no incidence on ponderal growth when administered per os in rats daily for one month. Finally, a comparative study of antitumor activity, toxicity and water-solubility of various butyric esters enabled us to select among these new molecules two isomers (carbon-3 and carbon-6 of the glucose ring substituted with n-butyric acid) derived from monoacetone glucose for further investigations of their biological mechanism in vivo and in vitro.
Pouillart
P
P
Laboratoire de Chimie Organique et Cinétique, UFR des Sciences, Université de Picardie, Amiens, France.
Ronco
G
G
Cerutti
I
I
Chany
C
C
Villa
P
P
D000818:Animals; D000970:Antineoplastic Agents; D002087:Butyrates / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009005:Monosaccharides / Q000494:pharmacology* / Q000633:toxicity; D011091:Polyesters / Q000494:pharmacology* / Q000633:toxicity; D012510:Sarcoma 180 / Q000188:drug therapy; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water
D000970:Antineoplastic Agents; D002087:Butyrates; D009005:Monosaccharides; D011091:Polyesters; D014867:Water