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Toxicity of structurally related anthraquinones and anthrones to mammalian cells in vitro

G S Bondy1, C L Armstrong, B A Dawson

  • 1Toxicology Research Division, Bureau of Chemical Safety, Food Directorate, Health Protection Branch, Health and Welfare Canada, Ottawa, Ontario, Canada K1A 0L2.

Toxicology in Vitro : an International Journal Published in Association with BIBRA
|August 10, 2010
PubMed

Insights

Anthraquinones exhibit cytotoxicity in mammalian cells, with toxicity varying based on chemical structure and assay type. Anthrones are generally more toxic than anthraquinones in cloning efficiency assays.

Area of Science:

  • Toxicology
  • Pharmacology
  • Biochemistry

Background:

  • Anthraquinones and related compounds are known for diverse biological activities.
  • Understanding their structure-activity relationships is crucial for assessing toxicological profiles.
  • Mammalian cell line assays provide a model for evaluating chemical toxicity.

Purpose of the Study:

  • To investigate the in vitro cytotoxicity of anthraquinones and related compounds.
  • To compare the sensitivity of different mammalian cell lines to these compounds.
  • To explore the influence of structural features on anthraquinone toxicity.

Main Methods:

  • Cytotoxicity was assessed using two in vitro assays: cloning efficiency and MTT reduction.
  • V79 cells were used to determine the concentration of chemicals causing 50% inhibition (IC50).
  • Four mammalian cell lines, including K562 and H4IIE, were tested using the MTT assay.

Main Results:

  • Cytotoxicity varied significantly between anthrones and anthraquinones, and between the two assay methods.
  • Anthrones (anthralin, chrysarobin) were more toxic in cloning efficiency assays, while anthraquinones (danthron, emodin) were more toxic in MTT assays.
  • The human leukemia cell line K562 was most sensitive, while rat hepatoma H4IIE cells showed reduced sensitivity to anthraquinones.

Conclusions:

  • In vitro cytotoxicity assays are valuable tools for studying the structure-activity relationships of anthraquinones.
  • Chemical structure, particularly the position of carbonyl and hydroxy groups, significantly influences toxicity.
  • Cell line-specific responses highlight the importance of selecting appropriate models for toxicological assessments.

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