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  2. The antiviral, antitumoural xanthate D609 is a competitive inhibitor of phosphatidylcholine-specific phospholipase C

The antiviral, antitumoural xanthate D609 is a competitive inhibitor of phosphatidylcholine-specific phospholipase C

  • Drugs Exp Clin Res. 1996;22(6):287-94.
E Amtmann 1
Affiliations

Affiliation

  • 1 German Cancer Research Centre, Heidelberg, Germany.
PMID: 9034754
Abstract

The effect of the Antiviral, antitumoural xanthate D609 on the activity of Phospholipase A2, C (PC- and Pi-specific) and D was investigated. D609 is the first model substance of a new concept of Antiviral therapy that interferes with cellular regulation mechanisms, rather than with virus coded enzymes. Exclusively phosphatidylcholine (PC) specific Phospholipase C (PC-PLC) was found to be inhibited in a dose-dependent manner. Enzyme activity was determined either as the rate of acid release from PC or as the rate of phosphorylcholine production form 3H labelled PC. Lineweaver-Burk plots revealed D609 as a competitive inhibitor of PC-PLC with a Ki of 6.4 microM. In addition, D609 competitively inhibited PC-PLC mediated cleavage of P-nitrophenylphosphorylcholine (p-NPP), a pseudo-substrate of PC-PLC with a Ki of 8.8 microM. These data suggest that D609 competes with the phosphorylcholine residue of PC for binding to PC-PLC.

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