Antibiological Actions of 2-Amino-1,4-naphthoquinone Imine

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Antibiological actions were studied on 2-amino-1,4-naphthoquinone imine-HCl (ANQI), which had been investigated in vitro as a potent inhibitor of DNA synthesis in Ehrlich mouse ascites tumor cells and as an interacting substance to DNA. The results are as follows : 1. Antimicrobial Action : A considerable activity was found against animal and plant microorganisms, especially Xanthomonas oryzae. 2. Acute Mammalian Toxicity : LD_<50> was 5.45 (4.88-6.09) mg/kg in mice (intraperitoneal injection). Only a little and transient effect was observed on behaviors of mice, and on respiration and blood pressure of dogs. 3. Antitumor Activity : ANQI exerted no therapeutic effect on Ehrlich mouse ascites tumor in vivo, but shortened survival days of tumor-bearing mice in its high doses. 4. Chemical Changes in Mouse Ascitic Fluid : ANQI in part was oxidized in ascitic fluid of tumor-bearing mice to 2-amino-1,4-naphthoquinone, which had been found to be not inhibitory to nucleic acid synthesis. The ineffectiveness of ANQI on the tumor in vivo was parlty explained from the susceptibility to biological oxidation.
公益社団法人日本薬学会の論文
1969-07-25