Cytotoxicities of the l and d isomers of phenylalanine mustard in L1210 cells |
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Authors: | David T Vistica Anne Rabon Marco Rabinovitz |
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Institution: | Laboratory of Medicinal Chemistry and Biology, Developmental Therapeutics Program, National Cancer Institute, Bethesda, MD 20205, U.S.A. |
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Abstract: | The cytotoxicity of d-phenylalanine mustard (medphalan) to murine L1210 leukemia cells in culture was reduced by both the d and l isomers of leucine. l-Leucine only partially protected L1210 cells from medphalan cytotoxicity at drug concentration's above 10 μM, suggesting that medphalan uptake occured via both an amino acid carrier and an as yet undetermined agency, possibly passive diffusion. At equitoxic concentrations of l-phenylalanine mustard (melphalan) and medphalan, l-leucine reduced medphalan cytotoxicity by only one-sixth that obtained with melphalan. Analysis of melphalan and medphalan inhibition of the initial rate of l-leucine transport indicated a melphalan Ki of 0.085 mM, a value one-seventh that of melphalan (Ki, 0.635 mM). |
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Keywords: | PBS phosphate-buffered saline (pH 7 4) BSA bovine serum albumin PAG phosphate-buffered saline containing 0 1 mM BSA and 0 25% glucose (pH 7 4) |
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