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Inhibition of alkaline phosphatase by substituted xanthines

1979; Elsevier BV; Volume: 28; Issue: 7 Linguagem: Inglês

10.1016/0006-2952(79)90334-4

1873-2968

Martin A. Croce, George L. Kramer, David L. Garbers,

Folate and B Vitamins Research

Various xanthine derivatives were synthesized and tested as inhibitors of calf intestinal and beef hepatic alkaline phosphatases. Three derivaties, 1-carboxymethyl-3-isobutylxanthine, theophylline and 1-carboxymethyl-3-methylxanthine, were potent uncompetitive inhibitors of calf intestinal alkaline phosphatase. 1-Carboxymethyl-3-methylxanthine, theophylline and 1-carboxymethyl-3-isobutylxanthine, at 80 μM concentrations, inhibited intestinal alkaline phosphatase by 50.0, 21.3 and 38.7 per cent respectively. Theophylline was also a potent inhibitor of beef hepatic alkaline phosphatase (53.2 per cent inhibition at 80μM). The most potent inhibitors of the beef liver enzyme were 1-isoamyl-3-methy +lxanthine, 1-n-propyl-3-methylxanthine and 1-phenethyl-3-methylxanthine, which inhibited the beef liver enzyme by 56.6, 46.4 and 45.5 per cent respectively, at 80 μM. These inhibitors of the beef liver enzyme, however, except for theophylline. were ineffective inhibitors of the calf intestine enzyme.