Cellular uptake and covalent binding of nitroso-chloramphenicol
A comparative study of the cellular transport of CAP and its nitroso derivative (NO-CAP) was carried out in Raji cells, a transformed human lymphoblastoid cell line. Both agents were concentrated by the cells by a factor of 3 (cellular/extracellular concentration ratio). The cellular uptake of NO-CAP, like that of CAP, was found to be rapid and temperature-independent. Thus the greater cytotoxicity of NO-CAP is apparently not due to an enhanced uptake of the nitroso derivative relative to CAP. In contrast to the similarity of uptake, NO-CAP becomes covalently bound to both Raji cells and freshly isolated human bone marrow cells to a much higher extent (15-fold). Also, cells previously loaded with CAP or NO-CAP retain three times as much of the nitroso compound during a 24 hr dialysis against a drug-free isotonic solution. The increased binding of NO-CAP to human hematopoietic cells attests to the greater reactivity of the p-substituted aromatic nitroso group and is consistent with the postulate that reduction products of the nitro group of CAP may be responsible for CAP-induced aplastic anemia.
- OSTI ID:
- 5102121
- Journal Information:
- J. Lab. Clin. Med.; (United States), Vol. 98:3
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
CHLORAMPHENICOL
METABOLISM
NITROSO COMPOUNDS
BIOLOGICAL PATHWAYS
BONE MARROW CELLS
LYMPHOCYTES
UPTAKE
ANIMAL CELLS
ANTI-INFECTIVE AGENTS
ANTIBIOTICS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BODY FLUIDS
CONNECTIVE TISSUE CELLS
DRUGS
LEUKOCYTES
MATERIALS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
SOMATIC CELLS
560301* - Chemicals Metabolism & Toxicology- Cells- (-1987)