[Comparative studies on the radiosensitizing action of 4-nitroimidazole and metronidazole (author's transl)].
After the 2-nitroimidazole derivatives, misonidazole, and the 5-nitroimidazole derivative, metronidazole, had been tried in clinical radiotherapy, it seemed necessary to test substances from the group of 4-nitroderivatives of the imidazole on their effectiveness as hypoxic radiosensitizers. Therefore, the influence of 1-(2'-hydroxyethyl)-2-methyl-4-nitroimidazole vs. metronidazole on the semiconservative DNA synthesis prior to the following irradiation on leukemia cells L5178Y, on the reproductive capacity in V-70 cells on the Chinese hamster and on radiation-induced inhibition of tumour growth has been investigated in comparative experiments. The results showed a considerably lower inhibitory effect on DNA synthesis by 4-nitroimidazole compared with metronidazole. Neither substance has any influence on radiation-induced DNA synthesis under oxic conditions. Under hypoxia the 4-nitroimidazole derivative shows a little stronger radiosensitizing action than metronidazole. The radiation-induced decrease of the survival rate of V-79 cells is not influenced by either substance in well oxygenized cells, while being increased to approximately the same degree in hypoxic cultures. The radiation-induced inhibition of breast cancer growth in the 1st transplantation passage of C3H inbred mice is potentiated by 4-nitroimidazole in a similar way as by metronidazole.
D000230:Adenocarcinoma / Q000532:radiotherapy; D000818:Animals; D002470:Cell Survival / Q000528:radiation effects; D004273:DNA, Neoplasm / Q000096:biosynthesis; D005260:Female; D007940:Leukemia L5178 / Q000532:radiotherapy; D008325:Mammary Neoplasms, Experimental / Q000532:radiotherapy; D008795:Metronidazole / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D051379:Mice; D008809:Mice, Inbred C3H; D011838:Radiation-Sensitizing Agents; D011878:Radiotherapy / Q000379:methods*
D004273:DNA, Neoplasm; D011838:Radiation-Sensitizing Agents; D008795:Metronidazole; C031624:isometronidazole
Vergleichende Untersuchungen zur strahlensensibilisierenden Wirkung von 4-Nitroimidazol und Metronidazol.