Treatment of leukemia L1210 and P388 by arabinosylcytosine‐polysaccharide conjugates

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Abstract
Conjugates of 1‐β‐D‐arabinofuranosylcytosine (araC) with two polysaccharides such as polygalacturonic acid (PGA) and carboxymethylated yeast β‐D‐glucan (CMG) were tested for their antileukemic activity in vitro on a L1210 cell line in suspension culture, in soft agar assay and in vivo on L1210, L1210/araC‐ and P388‐leukemia‐bearing mice. Both conjugates showed high activity in vitro in soft agar assay, compared with araC. Single administration of PGA‐araC or CMG‐araC increased the survival time 1.5 × or 1.7 ×, respectively, compared with araC in vivo in L1210‐leukemia‐bearing mice. The conjugates were not active against araC‐resistant leukemia line L1210/araC. The marked effect of both PGA‐araC and CMG‐araC against leukemia L1210 and P388 is probably due to the prolonged release of free araC from conjugates caused by hydrolysis.

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