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2126109 
Journal Article 
INHIBITION BY 6-MERCAPTOPURINE OF THE BINDING OF A BENZO(A)PYRENE DIOL-EPOXIDE TO DNA IN CHINESE HAMSTER OVARY CELLS 
Macleod, MC; Humphrey, RM; Bickerstaff, T; Daylong, A 
1990 
Yes 
Cancer Research
ISSN: 0008-5472
EISSN: 1538-7445 
BIOSIS/90/25124 
50 
14 
4355-4359 
English 
2114214 
WOS:A1990DM71800031 
BIOSIS COPYRIGHT: BIOL ABS. The finding that 7r,8t-dihydroxy-9,10t-oxy-7,8,9,10-tetrahydrobenzo(a)pyrene (BPDE-I) is stabilized against hydrolysis by binding to cellular membranes suggested that nucleophilic compounds which would colocalize with BPDE-I in membranes might inhibit the deleterious biological effects of BPDE-I. We have explored the possibility that hydrophobic, sulhyhdryl-containing compounds might provide such inhibition using the binding of PBDE-I to DNA in Chinese hamster ovary cells as a biological end point. Of several such compounds tested, 6-mercaptopurine (6-MP) was the most potent, exhibiting 50% inhibition of BPDE-I:DNA binding at about 30 muM and about 95% inhibition at 500 muM. 6-MP, at concentrations of 30 muM or greater, was also effective in preventing the induction of mutations by BPDE-I at the aprt locus. By varying the time of addition of the two compounds, it was shown that the action of 6-MP is intracellular. In vitro 6-MP readily forms an adduct with BPDE-I, and t