Abstract
The comparative efficacy of the pure diastereoisomers of leucovorin, the natural (6S) and the unnatural (6R) forms was compared to the racemic form (6RS). A protective effect in methotrexate-treated CCRF-CEM cells was obtained with 6S at concentrations 100-fold higher than those of methotrexate and with 6RS at concentrations 2-fold greater than those of 6S; however, at low concentrations of methotrexate, 6S was more effective than 6RS in preventing the cytotoxicity of methotrexate; on the opposite, 6R exhibited a protective effect at concentrations 10(4) higher than those of methotrexate. On the same cell line, 6S was shown to enhance the cytotoxic effect of 5 Fluorouracil exactly as 6RS while 6R did not exhibit any enhancing effect on cells exposed to 5 Fluorouracil.
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Zittoun, J., Marquet, J., Pilorget, J. et al. Comparative effect of 6S, 6R and 6RS Leucovorin on methotrexate rescue and on modulation of 5-fluorouracil. Br J Cancer 63, 885–888 (1991). https://doi.org/10.1038/bjc.1991.194
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DOI: https://doi.org/10.1038/bjc.1991.194
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