Different efflux rates may determine the cellular accumulation of various bis(guanylhydrazones)

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Abstract
Three bis(guanylhydrazones) (those of methylglyoxal, glyoxal and ethylglyoxal) were compared for their affinity for the putative polyamine carrier and for their cellular retention in L1210 mouse leukemia cells. All the bis(guanylhydrazones) inhibited equally effectively the uptake of spermidine by the tumor cells, indicating that the compounds had roughly equal affinity for the polyamine carrier. The fact that methylglyoxal bis(guanylhydrazone) and glyoxal bis(guanylhydrazone) which were reported to display distinct anti-leukemic activity were much more effectively concentrated in the animal cells than was ethylglyoxal bis(guanylhydrazone) was obviously attributable to the finding that the efflux rate of ethylglyoxal bis(guanylhydrazone) greatly exceeded that of the other bis(guanylhydrazones). The rate of efflux of the drugs was slowed down if the tumor cells were treated with 2-difluoromethylornithine before exposure to the bis(guanylhydrazones). Intracellular binding of the bis(guanylhydrazones) determines their cellular accumulation.

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