Vitro Metabolic Activation

Magee, P.N. in de Serres, F.J., Fouts, J.R., Bend, J.R. and Philpot, R.M. (eds), In Vitro Metabolic Activation in Mutagenesis Testing , Elsevier/North Holland Biomedical Press, Amsterdam, 1976 pp. 213-216. 

Lin G, Cui Y-Y, Liu X-Q and Wang Z-T (2002b), Species differences in the in vitro metabolic activation of the hepatotoxic pyrrolizidine alkaloids clivorine , Chem Res Toxicol, 15, 1421-1428. 

The In Vitro Metabolic Activation of Nitro Polycyclic Aromatic Hydrocarbons... 

The principal tests can be broadly categorized into microbial and mammalian cell assays. In both cases the tests are carried out in the presence and absence of in vitro metabolic activation enzymes, usually derived from rodent liver. 

In Vitro Metabolic Activation. The target cells for in vitro mutagenicity tests often possess a limited (often overlooked) capacity for endogenous metabolism of xenobiotics. However, to simulate the complexity of metabolic events that occur in the whole animal, there is a critical need to supplement this activity. 

Carver, J.H., Machado, M.L. and MacGregor, J.A. (1985). Petroleum distillates suppress in vitro metabolic activation Higher (S9) required in the Salmonella/microsome mutagenicity assay. Environ. Mutagen. 7 369-380. 

The in-vitro metabolic activation of l,2-dibromo-3-chloropropane, measured as radio-label covalently bound to macromolecules, is three-fold faster in rat testicular cells than in human testicular cells (Bjorge et al., 1996a). 

Natarajan, A.T. Darroudi, F. (1991) Use of human hepatoma cells for in vitro metabolic activation of chemical mutagens/carcinogens. Mutagenesis, 6, 399-40.3... 

JerinaDM et al. (1976) In de SerresFJ et al. (eds) In In vitro metabolic activation in mutagenesis testing, Elsevier/North Holland, Amsterdam, pp 159-177... 

P.P. Fu et al., Effects of nitro substitution on the in vitro metabolic activation of polycyclic aromatic hydrocarbons, in Polycyclic Aromatic Hydrocarbon Carcinogenesis Structure-Activity Relationships, ed. by S.K. Yang, B.D. Silverman (CRC Press, Florida, 1988), pp. 37-65... 

Workshop, In Vitro Metabolic Activation in Mutagenesis Testing Research Triangle Park, N.C. 

D. M. Jerina, R. E. Lehr, H. Yagi, O. Hernandez, P. M. Dansette, P. G. Wislocki, A. W. Wood, R. L. Chang, W. Levin, and A. H. Conney, in Vitro Metabolic Activation In Mutagenesis Testing, Elsevier/North-Holland Biomedical Press, Amsterdam, 1976, pp. 159-177. 

Jerina DM. Lehr RE. Yagi H. et al. 1976. Mutagenicity of B[a]P derivatives and the description of a quantum mechanical model which predicts the ease of carbonium ion formation from diol epoxides. In de Serres FJ. Fouts JR. Bend JR. et al. eds. In vitro metabolic activation in mutagenesis testing. Amsterdam. The Netherlands Elsevier/North Holland. 159-178. 

Lecoq S, Ni She M, Grover PL, et al. 1991b. The in vitro metabolic activation of dibenz[a,h ]anthracene, catalyzed by rat liver microsomes and examined by P- postlabelling. Cancer Lett 57(3) 261-269. 

Jerina 0., Lehr R., Yagi H., Hernandez 0., Dansette P., Wislockl P., Wood A., Chang R., Levin W. and Conney A. 1976 in de Serres F., Fouts J., Bend J. and Philpot R. (eds) In Vitro Metabolic Activation in Mutagenesis Testing, Elsevier, Amsterdam... 

The observation of in vitro metabolic activation of the 3-benzylindole moiety in zafirlukast, an anti-asthma drug, to give the glutathione adduet is an indication that the 3-methyl-indole activation pathway applies to other activated 3-alkyl indoles as well. ... 

C. Specific Applications of in Vitro Metabolic Activation Systems... 

The application of several short-term tests to detect carcinogenic hydrazine derivatives has been of limited success 204a, 260). While a host-mediated assay of 1,2-dimethylhydrazine has been reported to give a positive mutagenic response in S. typhimurium G46 345a), the Ames assay has generally not been sensitive toward this class of compounds. In view of the limited reports on the successful applications of an in vitro metabolic activation system for these compounds, comparisons of such methods are not valid at this time. 

G. M. Williams, A comparison of in vivo and in vitro metabolic activations systems, in Critical Reviews in Toxicology-Strategies for Short-term Testing for Mutagens/Carcinogens (B. Butterworth, ed.), pp. 96-97, C. R. C. Press, West Palm Beach, Fla. (1979). 

E. Vogel, Mutagenicity of carcinogens in Drosophila as function of genotype-controlled metabolism, in In Vitro Metabolic Activation in Mutagenesis Testing (F. J. de Serres, J. R. Fouts, J. R. Bend, and R. M. Philpot, eds ), pp. 63-79, North-Holland, Amsterdam (1976). 

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