Abstract
BHAC is a newly synthesized lipophilic derivertive of Ara-C.To clarify its pharmacological mode of action, P388 murine leukemic.cells were incubated with two different types of 14C-labeled BHAC,(cytosine-2-14C) BHAC and (acyl-1-14C)BHAC, and DNA was extracted with phenol. And then the phenol extracted DNA was hydrolyzed by nuclease P1 and analyzed with high-performance liquid chromatography(HPLC). The radioactivity of DNA, from the cells incubated with (cytosine-2-14C)BHAC, was detected as Ara-CMP. But the radioactivity of DNA, from the cells incubated with (acyl-1-14C)BHAC, was almost not detected. On the other hand, the main radioactivity of acid soluble fraction was determined as Ara-CTP. On the basis of our results, BHAC is not phosphorylated directly to produce N4-behenoly-ara-CTP, but mainly once converted to Ara-C and it subsequently produces Ara-CTP, the active metabolite of the drug, and then incorporated into DNA.
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Higashigawa, M., Ohkubo, T., Kawasaki, H. et al. 56 INCORPORATION OF N4-BEHENOLY-1-β-D-ARABINOFURANOSYLCYTOSINE (BHAC) INTO DNA AS l-β-D-ARABINOFURANOSYLCYTOSINE (ARA-C). Pediatr Res 24, 120 (1988). https://doi.org/10.1203/00006450-198807000-00080
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DOI: https://doi.org/10.1203/00006450-198807000-00080