Haematin (haem) polymerization and its inhibition by quinoline antimalarials

Ann Trop Med Parasitol. 1997 Jul;91(5):559-66. doi: 10.1080/00034989760932.

Abstract

Haematin (ferriprotoporphyrin IX) is released from haemoglobin during its degradation in the malarial parasites' food vacuole and is detoxified by its polymerization into a form of beta-haematin called haemozoin, or malarial pigment. This process is protein independent in vitro. Quinoline antimalarial blood schizonticides accumulate in the food vacuole and may inhibit haematin polymerization by binding to haematin and preventing its incorporation into the growing haemozoin chain. Drug resistance to quinolines is thought to be due to reduced accumulation of the drug in the food vacuole. As some quinolines overcome this resistance, quinolines, as a class, remain a potential source of future antimalarial drugs.

Publication types

  • Review

MeSH terms

  • Animals
  • Antimalarials / metabolism
  • Antimalarials / pharmacology*
  • Hemeproteins
  • Hemin / antagonists & inhibitors*
  • Hemin / chemistry
  • Hemin / metabolism
  • Pigments, Biological / metabolism
  • Plasmodium / drug effects
  • Polymers
  • Quinolines / metabolism
  • Quinolines / pharmacology*
  • Vacuoles / metabolism

Substances

  • Antimalarials
  • Hemeproteins
  • Pigments, Biological
  • Polymers
  • Quinolines
  • hemozoin
  • Hemin