INVITRO CYTOTOXIC AND BIOCHEMICAL EFFECTS OF 5-AZA-2'-DEOXYCYTIDINE

  • 1 January 1977
    • journal article
    • research article
    • Vol. 37  (6) , 1636-1639
Abstract
The in vitro effect of 5-aza-2''-deoxycytidine (5-aza-CdR) on cytotoxicity and macromolecular synthesis in A(T1)C1-3 hamster fibrosarcoma cells was investigated. The in vitro concentrations that produce 50% cell kill for 5-aza-CdR were .apprx. 1.0 and 0.01 .mu.g/ml for a 2- and 24 h exposure, respectively. 5-aza-CdR inhibited growth of the fibrosarcoma cells by 40% at a concentration of 0.05 .mu.g/ml. Deoxycytidine, but not cytidine, was a potent antagonist of the cytotoxicity produced by 5-aza-CdR. At cytotoxic concentrations 5-aza-CdR did not appear to inhibit DNA, RNA or protein synthesis during a 1 h incubation as measured by the incorporation of radioactive thymidine, uridine or leucine into acid insoluble material. At a concentration of 10 .mu.g/ml, 5-aza-CdR stimulated the incorporation of radioactive thymidine into DNA by > 50%. These results indicate that 5-aza-CdR is a very potent cytotoxic agent to tumor cells in vitro at concentrations that do not inhibit macromolecular synthesis.

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