Nitroxide-mediated protection against X-ray- and neocarzinostatin-induced DNA damage

Free Radic Biol Med. 1992 Nov;13(5):479-87. doi: 10.1016/0891-5849(92)90142-4.

Abstract

The stable free radical Tempol (4-hydroxy-2,2,6,6-tetramethyl-piperidinyloxy) has been shown to protect against X-ray-induced cytotoxicity and hydrogen peroxide- or xanthine oxidase-induced cytotoxicity and mutagenicity. The ability of Tempol to protect against X-ray- or neocarzinostatin (NCS)-induced mutagenicity or DNA double-strand breaks (dsb) was studied in Chinese hamster cells. Tempol (50 mM) provided a protection factor of 2.7 against X-ray-induced mutagenicity in Chinese hamster ovary (CHO) AS52 cells, with a protection factor against cytotoxicity of 3.5. Using the field inversion gel electrophoresis technique of measuring DNA dsb, 50 mM Tempol provides a threefold reduction in DNA damage at an X-ray dose of 40 Gy. For NCS-induced damage, Tempol increased survival from 9% to 80% at 60 ng/mL NCS and reduced mutation induction by a factor of approximately 3. DNA dsb were reduced by a factor of approximately 7 at 500 ng/mL NCS. Tempol is representative of a class of stable nitroxide free radical compounds that have superoxide dismutase-mimetic activity, can oxidize metal ions such as ferrous iron that are complexed to DNA, and may also detoxify radiation-induced organoperoxide radicals by competitive scvenging. The NCS chromophore is reduced by sulfhydryls to an active form. Electron spin resonance (ESR) spectroscopy shows that 2-mercaptoethanol-activated NCS reacts with Tempol 3.5 times faster than does unactivated NCS. Thus, Tempol appears to inactivate the NCS chromophore before a substantial amount of DNA damage occurs.

MeSH terms

  • Animals
  • CHO Cells
  • Cell Line
  • Cell Survival / drug effects
  • Cell Survival / radiation effects*
  • Cricetinae
  • Cyclic N-Oxides / pharmacology*
  • DNA / drug effects*
  • DNA / radiation effects*
  • DNA Damage*
  • Dose-Response Relationship, Drug
  • Dose-Response Relationship, Radiation
  • Kinetics
  • Mutagenesis
  • Radiation-Protective Agents / pharmacology*
  • Spin Labels
  • X-Rays
  • Zinostatin / pharmacology*

Substances

  • Cyclic N-Oxides
  • Radiation-Protective Agents
  • Spin Labels
  • DNA
  • Zinostatin
  • tempol