In vitro screening of carcinogenesis inhibitors acting by inhibition of microsomal polycyclic aromatic hydrocarbon activation.
A procedure for in vitro prescreening of carcinogenesis inhibitors acting by the inhibition of the microsomal activation systems is described. It consists of measuring the protection conferred by the investigated chemicals against DNA binding of ultimate carcinogens resulted during G(3H)B[a]P activation. This rapid and reproducible procedure is able to select only carcinogenesis inhibitors which interact with the cytochrome P-450 dependent microsomal enzymes being specific in this respect. The effectiveness of 23 compounds (mainly antioxidants) was tested and the results compared with literary data concerning their activity. The concordance was satisfactory.
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D001564:Benzo(a)pyrene / Q000037:antagonists & inhibitors*; D002083:Butylated Hydroxyanisole / Q000494:pharmacology; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004247:DNA / Q000378:metabolism; D066298:In Vitro Techniques; D007527:Isoenzymes / Q000378:metabolism; D008722:Methods; D051379:Mice; D008861:Microsomes / Q000201:enzymology*; D011083:Polycyclic Compounds / Q000378:metabolism*
D000975:Antioxidants; D007527:Isoenzymes; D011083:Polycyclic Compounds; D002083:Butylated Hydroxyanisole; D001564:Benzo(a)pyrene; D004247:DNA; D003577:Cytochrome P-450 Enzyme System; C051361:2-tert-butyl-4-hydroxyanisole