Modulation of the growth of Plasmodium falciparum in vitro by protein serine/threonine phosphatase inhibitors

Biochem Biophys Res Commun. 1998 Jun 9;247(1):18-23. doi: 10.1006/bbrc.1998.8730.

Abstract

To elucidate the physiological roles of the protein serine/threonine phosphatases of P. falciparum, first we identified and characterized phosphatase activities of Plasmodium falciparum enzymologically and pharmacologically. We have demonstrated that P. falciparum possesses phosphatase-1-like activities predominantly over phosphatase-2A-like activities, while erythrocytes possess mainly phosphatase-2A-like activities. Then, we examined the effects of okadaic acid and calyculin A, potent inhibitors of protein phosphatase 1 and 2A, on the growth of P. falciparum in vitro. Both of the drugs inhibited parasite growth dose dependently. The manner of growth inhibition by calyculin A and okadaic acid suggested that these drugs inhibit parasite growth mainly by inhibiting parasite phosphatase-1-like activities. Both drugs were shown to inhibit the growth of three different developmental stages of parasites--ring forms, trophozoites, and schizonts--and inhibit trophozoites the most. This is the first report on P. falciparum protein serine/threonine phosphatase activities, which are essential to regulate the erythrocytic stage of parasite growth.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Division / drug effects
  • Culture Media
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology*
  • Erythrocytes / parasitology
  • Marine Toxins
  • Okadaic Acid / pharmacology
  • Oxazoles / pharmacology
  • Phosphoprotein Phosphatases / antagonists & inhibitors*
  • Phosphoprotein Phosphatases / physiology
  • Plasmodium falciparum / drug effects
  • Plasmodium falciparum / enzymology*
  • Plasmodium falciparum / growth & development*
  • Protein Phosphatase 1
  • Protein Phosphatase 2
  • Time Factors

Substances

  • Culture Media
  • Enzyme Inhibitors
  • Marine Toxins
  • Oxazoles
  • Okadaic Acid
  • calyculin A
  • Phosphoprotein Phosphatases
  • Protein Phosphatase 1
  • Protein Phosphatase 2