Effect of acyl derivatives of 4,4,4-trifluoro-1-phenyl-1,3-butanedione on 2-acetylaminofluorene-induced glutathione S-transferase positive foci in the rat liver.
Acyl derivatives of 4,4,4-trifluoro-1-phenyl-1,3-butanedione (TFPB), 1-benzoyl-2-trifluoromethyl-2-acetoxyethene (BTAE), and 1-benzoyl-2-trifluoromethyl-2-(4-methylthio)benzoyloxyethene (BTME), were synthesized and investigated for inhibition of tRNA binding by N-acetoxy-2-acetylaminofluorene (N-AcO-AAF), and induction of glutathione S-transferase placental form (GST-P) positive foci in the rat liver by 2-acetylaminofluorene (2-AAF). Male F344 rats were given BTAE or BTME intraperitoneally and 2-AAF by intragastric intubation. Two weeks following the treatment, the rats were maintained on the diet containing 0.05% phenobarbital for an additional 6 weeks and then killed. Development of GST-P positive foci was not affected by concomitant treatment with BTAE or BTME. These two compounds inhibited the in vitro binding of N-AcO-AAF to tRNA. Thus, although these diacylmethane derivatives had the in vitro inhibitory activity, they did not inhibit tumor-initiating activity of 2-AAF in the rat liver.
First Department of Pathology, Nagoya City University Medical School, Japan.
R
R
Hasegawa
C Y
CY
Wang
D J
DJ
Kim
M S
MS
Lee
Y
Y
Yoshida
N
N
Ito
D015073:2-Acetylaminofluorene; D000818:Animals; D016588:Anticarcinogenic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001565:Benzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001681:Biological Assay; D004790:Enzyme Induction; D005982:Glutathione Transferase / Q000032:analysis* / Q000096:biosynthesis; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D008113:Liver Neoplasms / Q000201:enzymology / Q000517:prevention & control; D008297:Male; D012343:RNA, Transfer / Q000187:drug effects*; D051381:Rats; D011916:Rats, Inbred F344
D016588:Anticarcinogenic Agents; D001565:Benzoates; C081835:1-benzoyl-2-trifluoromethyl-2-acetoxyethene; C081836:1-benzoyl-2-(4-methylthio)benzoyloxyethene; D012343:RNA, Transfer; D015073:2-Acetylaminofluorene; D005982:Glutathione Transferase