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Binding of N-acetylbenzidine and N,N'-diacetylbenzidine to hepatic DNA of rat and hamster in vivo and in vitro

Journal Article · · Carcinogenesis (N.Y.); (United States)
OSTI ID:7003193

Benzidine, a potent hepatocarcinogen in rodents, is readily metabolised to acetylated derivatives. In this study, the covalent binding of (/sup 3/H-acetyl)N-acetylbenzidine and (/sup 3/H-acetyl)N,N'-diacetylbenzidine to liver DNA in rats and hamsters was investigated. Binding to liver DNA of rats at 1 or 7 days after i.p. injection of N-acetylbenzidine was 2-fold higher than that observed in the liver DNA of hamsters which had been similarly treated. Analysis of enzymically hydrolysed DNA from both species indicated the presence of a single adduct which co-eluted with N-(deoxyguanosin-8-yl)-N'-acetylbenzidine. In vitro treatment of rat or hamster liver slices with N-acetylbenzidine also resulted in covalent binding to hepatic DNA and the identical DNA adduct was detected at levels comparable to that observed in vivo. When N,N'-diacetylbenzidine was injected i.p. into rats, a comparatively low level of binding to liver DNA was observed. Following enzymic hydrolysis, the major DNA adduct detected by h.p.l.c. analysis was again N-(deoxyguanosin-8-yl)-N'-acetylbenzidine accompanied by a small amount of N-(deoxyguanosin-8-yl)-N,N'-diacetylbenzidine. In vitro incubation of N,N'-diacetylbenzidine with rat liver slices resulted in DNA binding levels similar to that observed with N-acetylbenzidine. In contrast to what was found in vivo, N-(deoxyguanosin-8-yl)-N,N'-diacetylbenzidine was the major adduct detected in DNA from rat liver slices. These data suggest that both N-hydroxy-N'-acetylbenzidine and N-hydroxy-N,N'-diacetylbenzidine are proximate carcinogenic species of benzidine, with N-hydroxy-N'-acetylbenzidine the more important. The low level of N-(deoxyguanosin-8-yl)N,N'-diacetylbenzidine observed in vivo may be due to its rapid repair. Alternatively, N-sulphonyloxy-N,N'-diacetylbenzidine, which would produce this adduct on reaction with DNA, may be efficiently detoxified in vivo.

Research Organization:
Cancer Research Unit, University of York, UK
OSTI ID:
7003193
Journal Information:
Carcinogenesis (N.Y.); (United States), Journal Name: Carcinogenesis (N.Y.); (United States) Vol. 5:3; ISSN CRNGD
Country of Publication:
United States
Language:
English