Tumour necrotisation in nude mice xenografts by the reversible protein synthesis inhibitor zilascorb(2H)

The benzaldehyde derivative 4,6-benzylidene-D-glucose (BG) induces an inhibition of protein synthesis at otherwise non-toxic doses in cells grown in vitro. To increase the biological effect of BG, the hydrogen in the formyl group was exchanged with deuterium, resulting in 4,6-benzylidene-d1-D-glucose (P-1013). In this study we compared the bioavailability of BG and P-1013, since both intraperitoneal and, especially, oral administration of the drugs would be a great advantage. We also examined whether or not P-1013 displays dose-dependent pharmacokinetics. Pharmacokinetics were studied by analysing plasma samples using reversed-phase high-performance liquid chromatography (HPLC). P-1013 was given at four different doses i.v. (60, 120, 145 and 230 mg/kg) and p.o. (60, 120, 170 and 230 mg/kg) to female Bom:NMRI-nu mice. The bioavailability was more than 50% for all doses. The results also indicate that P-1013 shows linear pharmacokinetics, with no change being observed in the half-life (t1/2) with increasing dose and only a slightly more than proportional increase in the area under the concentration-time curve (AUC) occurring with increasing dose. A doubling in dose resulted in a 2.2-fold increase in the AUC. P-1013 and BG were also given i.v., p.o. and i.p. to female nu/nu-BALB/cABom mice and male Wistar rats. A high degree of bioavailability was found in both species, with 55-100% of the delivered dose being absorbed. Deuteration of BG does not seem to alter its bioavailability, as we found the same bioavailability for P-1013 as for BG. We conclude that the pharmacokinetics of P-1013 does not prevent its use as a cancer treatment drug given orally.

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The bioavailability and dose dependency of the deuterated anti-tumour agent 4,6-benzylidene-d 1-d-glucose in mice and rats

Dunsæd

Dornish²,

Pettersen

1995

Cancer Chemother. Pharmacol.

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The algebraic relational theory in the analysis of the reversibility of biological processes becoming malignant

Zaretzky

Leguizamón

1996

Mathematical and Computer Modelling

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Trajectories in topological spaces due to lattice responses for low energies relational processes

Leguizamón

Zaretzky

1999

Mathematical and Computer Modelling

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Tumour necrotisation in nude mice xenografts by the reversible protein synthesis inhibitor zilascorb(2H)

Cited by 3 publications

References 15 publications

The bioavailability and dose dependency of the deuterated anti-tumour agent 4,6-benzylidene-d 1-d-glucose in mice and rats

The bioavailability and dose dependency of the deuterated anti-tumour agent 4,6-benzylidene-d 1-d-glucose in mice and rats

The algebraic relational theory in the analysis of the reversibility of biological processes becoming malignant

Trajectories in topological spaces due to lattice responses for low energies relational processes

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