Add time:08/08/2019         Source:sciencedirect.com

The synthetic nucleoside tiazofurin(2-β-ribofuranosylthiazole-4-carboxamide) and its selenium analog selenazofurin inhibited the growth of L1210 leukemia cell culture in a dose dependent manner with IC50 value of 2.0 and 0.2 Um respectively. The GTPATP ratio was diminished 4–6 fold as measured by HPLC, while IMPATP increased 6–8 fold. The decreased guanylate pools may explain the 30% reduction in cyclic GMP levels and GTPase activity measured after the treatment with the nucleosides. Inhibition of phospholipase C activity is suggested since diacylglycerol content, protein kinase C activity and phorbol ester binding of the membrane fraction were also reduced 20–40%. These results reveal a novel aspect in the action of these compounds which may play a role in their therapeutic action and selectivity.

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