Spirohydantoin mustard (SHM), a central nervous system directed nitrogen mustard with anticancer activity, was metabolized in the presence of mouse liver postmitochondrial supernatant (9000g fraction) to a nonpolar alkylating metabolite. The metabolite was isolated by thin-layer chromatography of chloroform or ethyl acetate extracts of incubation mixtures, and its structure was established by mass spectral analysis, synthesis, and cochromatography. The metabolite, spirohydantoin aziridine, was mutagenic for Salmonella typhimurium TA1535 in the Ames assay but inactive as an antitumor agent against P388 leukemia in vivo.
A microbiological assay was developed for bleomycin, an antitumor antibiotic reported to be active in human trials. The assay bacterium was a strain of
Escherichia coli
which is resistant to ethionine. Studies revealed relatively high concentrations of bleomycin in the blood and urine of mice after a single dose, < 0.33
ld
10
, injected intraperitoneally.
A microbiological assay was developed for bleomycin, an antitumor antibiotic reported to be active in human trials. The assay bacterium was a strain of Escherichia coli which is resistant to ethionine. Studies revealed relatively high concentrations of bleomycin in the blood and urine of mice after a single dose, < 0.33 LD10, injected intraperitoneally.
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