Abstract
The metabolism of 1-β-D-arabinofuranosylcytosine (ara-C) and N4-behenoyl-1β-D-arabinofuranosylcytosine (BH-AC) was studied in HeLa cells. After the cells were exposed to ara-C at a concentration of 20 μg/ml or BH-AC at 46.5 μg/ml for 1, 3, 6, 12 or 24 hr, the level of ara-C was determined using the radioimmunoassay method, and the level of BH-AC and 1-β-D-arabinofuranosyluracil (ara-U), using high-performance liquid chromatography. In the ara-C-treated cells, the intracellular ara-C increased to 1.26 μg/g cells after exposure for 6 hr, and ara-C was rapidly changed to ara-U in the cells and in the medium. In the BH-AC-treated cells, the intracellular BH-AC increased after exposure for 24 hr and BH-AC was gradually converted to ara-C in the cells: the intracellular level of ara-C was only 15% of that of BH-AC after exposure for 24 hr. BH-AC level in the medium persisted for 24 hr, at the initial concentration. Our findings show that BH-AC is stable compared to ara-C and gradually converts to ara-C. This conversion is presumably a critical step in the antineoplastic effect of BH-AC.
| Original language | English |
|---|---|
| Pages (from-to) | 41-44 |
| Number of pages | 4 |
| Journal | Anticancer research |
| Volume | 9 |
| Issue number | 1 |
| Publication status | Published - Jan 1 1989 |
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All Science Journal Classification (ASJC) codes
- Oncology
- Cancer Research
Cite this
Cytotoxicity of N4-behenoyl-1-β-D-arabinofuranosylcytosine through gradual conversion to 1-β-D-arabinofuranosylcytosine in HeLa cells. / Maehara, Y.; Kusumoto, T.; Sakaguchi, Y.; Kusumoto, H.; Anai, H.; Sugimachi, K.
In: Anticancer research, Vol. 9, No. 1, 01.01.1989, p. 41-44.Research output: Contribution to journal › Article
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TY - JOUR
T1 - Cytotoxicity of N4-behenoyl-1-β-D-arabinofuranosylcytosine through gradual conversion to 1-β-D-arabinofuranosylcytosine in HeLa cells
AU - Maehara, Y.
AU - Kusumoto, T.
AU - Sakaguchi, Y.
AU - Kusumoto, H.
AU - Anai, H.
AU - Sugimachi, K.
PY - 1989/1/1
Y1 - 1989/1/1
N2 - The metabolism of 1-β-D-arabinofuranosylcytosine (ara-C) and N4-behenoyl-1β-D-arabinofuranosylcytosine (BH-AC) was studied in HeLa cells. After the cells were exposed to ara-C at a concentration of 20 μg/ml or BH-AC at 46.5 μg/ml for 1, 3, 6, 12 or 24 hr, the level of ara-C was determined using the radioimmunoassay method, and the level of BH-AC and 1-β-D-arabinofuranosyluracil (ara-U), using high-performance liquid chromatography. In the ara-C-treated cells, the intracellular ara-C increased to 1.26 μg/g cells after exposure for 6 hr, and ara-C was rapidly changed to ara-U in the cells and in the medium. In the BH-AC-treated cells, the intracellular BH-AC increased after exposure for 24 hr and BH-AC was gradually converted to ara-C in the cells: the intracellular level of ara-C was only 15% of that of BH-AC after exposure for 24 hr. BH-AC level in the medium persisted for 24 hr, at the initial concentration. Our findings show that BH-AC is stable compared to ara-C and gradually converts to ara-C. This conversion is presumably a critical step in the antineoplastic effect of BH-AC.
AB - The metabolism of 1-β-D-arabinofuranosylcytosine (ara-C) and N4-behenoyl-1β-D-arabinofuranosylcytosine (BH-AC) was studied in HeLa cells. After the cells were exposed to ara-C at a concentration of 20 μg/ml or BH-AC at 46.5 μg/ml for 1, 3, 6, 12 or 24 hr, the level of ara-C was determined using the radioimmunoassay method, and the level of BH-AC and 1-β-D-arabinofuranosyluracil (ara-U), using high-performance liquid chromatography. In the ara-C-treated cells, the intracellular ara-C increased to 1.26 μg/g cells after exposure for 6 hr, and ara-C was rapidly changed to ara-U in the cells and in the medium. In the BH-AC-treated cells, the intracellular BH-AC increased after exposure for 24 hr and BH-AC was gradually converted to ara-C in the cells: the intracellular level of ara-C was only 15% of that of BH-AC after exposure for 24 hr. BH-AC level in the medium persisted for 24 hr, at the initial concentration. Our findings show that BH-AC is stable compared to ara-C and gradually converts to ara-C. This conversion is presumably a critical step in the antineoplastic effect of BH-AC.
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M3 - Article
C2 - 2705754
AN - SCOPUS:0024477410
VL - 9
SP - 41
EP - 44
JO - Anticancer Research
JF - Anticancer Research
SN - 0250-7005
IS - 1
ER -