Abstract
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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 396-401 |
| Number of pages | 6 |
| Journal | The Journal of laboratory and clinical medicine |
| Volume | 98 |
| Issue number | 3 |
| State | Published - 1981 |
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ASJC Scopus subject areas
- Medicine(all)
- Pathology and Forensic Medicine
Cite this
The cellular uptake and covalent binding of nitroso-chloramphenicol. / Murray, Thomas; Yunis, Adel A.
In: The Journal of laboratory and clinical medicine, Vol. 98, No. 3, 1981, p. 396-401.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - The cellular uptake and covalent binding of nitroso-chloramphenicol
AU - Murray, Thomas
AU - Yunis, Adel A
PY - 1981
Y1 - 1981
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0019517794&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0019517794&partnerID=8YFLogxK
M3 - Article
C2 - 7264436
AN - SCOPUS:0019517794
VL - 98
SP - 396
EP - 401
JO - Translational Research
JF - Translational Research
SN - 1931-5244
IS - 3
ER -