Frezza D, Bianchi V
Teratog Carcinog Mutagen. 1984;4(2):201-10. doi: 10.1002/tcm.1770040205.
Procarbazine ( PCZ ) was tested for its ability to induce mitotic gene conversions at the ade and trp loci of Saccharomyces cerevisiae, strain D4. The influence of the following factors was examined: growth phase of the yeast cells (log vs stationary phase), pH of the treatment solution, and addition of mouse S9 fractions prepared from different organs. The drug was found more toxic and mutagenic at low doses (up to 25 mg/ml) for log phase cells, and scarcely toxic but highly mutagenic, even at high doses, for stationary phase cells. PCZ activity was reduced by acidic pH, and suppressed by S9 mix. Gene conversions were also analyzed in the intrasanguineous host-mediated assay performed in mice orally administered with PCZ . In such conditions PCZ was ineffective in stimulating mitotic gene conversions, probably owing to its inactivation in the acidic environment of the gastroenteric tract.
对丙卡巴肼（PCZ）诱导酿酒酵母D4菌株ade和trp位点有丝分裂基因转换的能力进行了测试。研究了以下因素的影响：酵母细胞的生长阶段（对数期与稳定期）、处理溶液的pH值以及添加从不同器官制备的小鼠S9组分。发现该药物在低剂量（高达25 mg/ml）时对对数期细胞毒性更大且具有致突变性，而对稳定期细胞即使在高剂量时毒性也很小但致突变性很高。酸性pH会降低PCZ活性，S9混合物会抑制其活性。还在给小鼠口服PCZ后进行的体内宿主介导试验中分析了基因转换情况。在这种情况下，PCZ在刺激有丝分裂基因转换方面无效，这可能是由于其在胃肠道酸性环境中失活所致。
