AUTHOR: Wood AW, Huang MT, Chang RL, Newmark HL, Lehr RE, Yagi H, Sayer JM, Jerina DM, Conney AH
TITLE: INHIBITION OF THE MUTAGENICITY OF BAY-REGION DIOL EPOXIDES OF POLYCYCLIC AROMATIC HYDROCARBONS BY NATURALLY OCCURRING PLANT PHENOLS: EXCEPTIONAL ACTIVITY OF ELLAGIC ACID
SOURCE: Proc Natl Acad Sci U S A; 79(18):5513-5517 1982   UI: 82631054
ABSTRACT: Ferulic, caffeic, chlorogenic, and ellagic acids, four naturally occurring plant phenols, inhibit the mutagenicity and cytotoxicity of (+-) 7beta,8alpha-dihydroxy-9alpha,10alpha-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene (B[a]P 7,8-diol-9,10-epoxide-2), the only known ultimate carcinogenic metabolite of benzo[a]pyrene. One nmol of ellagic acid in the 0.5-ml incubation mixture inhibits the mutagenicity of 0.05 nmol of B[a]P 7,8-diol,9,10-epoxide-2 in strain TA100 of Salmonella typhimurium. A 3-nmol dose of ellagic acid inhibits mutation induction by 90%. Ellagic acid is also a potent antagonist of B[a]P 7,8-diol-9,10-epoxide-2 in Chinese hamster V79 cells. Similar to results obtained with the bacteria, ferulic, caffeic, and chlorogenic acids are approx two orders of magnitude less active than ellagic acid in the mammalian cell assay. In parallel with the mutagenicity studies, ellagic acid is 80-300x more effective than the other phenols in accelerating the disappearance of B[a]P 7,8-diol-9,10-epoxide-2. Ellagic acid is a highly potent inhibitor of the mutagenic activity of bay-region diol epoxides of benzo[a]pyrene, dibenzo[a,h]pyrene, and dibenzo[a,i]pyrene, but higher concentrations of ellagic acid are needed to inhibit the mutagenic activity of the chemically less reactive bay-region diol epoxides of benz[a]anthracene, chrysene, and benzo[c]phenanthrene. These studies demonstrate that ellagic acid is a potent antagonist of the adverse biological effects of the ulimate carcinogenic metabolites of several polycyclic aromatic hydrocarbons and suggest that this naturally occurring plant phenol, normally ingested by humans, may inhibit the carcinogenicity of polycyclic aromatic hydrocarbons. (42 Refs)