J. Jaffe
Sep 1, 1961
Citations
0
Influential Citations
20
Citations
Quality indicators
Journal
Biochemical pharmacology
Abstract
Abstract 6-Azauracil, an analog of uracil which is an inhibitor of the growth of a number of experimental murine neoplasms and of several species of bacteria, prevents the reproduction of T. equiperdum in mice. This action results in growth suppression without trypanocidal sequelae. When treatment is stopped, the drug is rapidly cleared from the body, and the rate of reproduction of the trypanosomes rapidly returns to normal. The potency of a given dose of 6-azauracil is significantly enhanced when infected mice are fed a diet totally lacking in purines and pyrimidines. Conversely, the inhibitory activity of the analog is partially reversed when infected mice are fed a diet supplemented with uracil. The ribonucleoside of 6-azauracil, i.e. 6-azauridine, a much more potent inhibitor of the growth of certain transplanted neoplasms in mice than is 6-azauracil, does not inhibit the growth of T. equiperdum in the same species. Also, experiments with T. equiperdum in vitro have shown that 6-azauracil is at least 100 times more potent than 6-azauridine as an inhibitor of orotidylic acid decarboxylase, an enzyme selectively inhibited by the ribonucleotide of 6-azauracil (i.e. 6azauridine 5'phosphate).