WR-2721, Its Derivatives and Their Radioprotective Effects on Mammalian Cells in Culture

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Abstract
Although it is well known that WR-2721 is very efficient in protecting mice against lethal irradiation, no radioprotective effect of WR-2721 was found on mouse L cells in culture. But WR-1065 alone (free SH form of WR-2721), and WR-2721 pre-incubated with mouse liver homogenate, showed radioprotective ability. Mouse liver homogenate dephosphorylated WR-2721 to WR-1065. The highest WR-2721 metabolizing activity was found in mouse liver homogenate and Chang liver cell homogenate. Homogenates of human liver and kidney were also shown to possess moderate activity for metabolizing WR-2721. Evidently, WR-2721 must be dephosphorylated before exerting its radioprotective effect and this dephosphorylating activity varies with tissues. Mouse L cell in culture is a novel system to assess the extent of dephosphorylation of WR-2721 in various tissues.