Quinoline anti-malarial drugs inhibit spontaneous formation of β-haematin (malaria pigment)

Polymerisation of haematin to β-haematin (haemozoin or malaria pigment) in acidic acetate solutions was studied using infrared spectroscopy. The reaction was found to occur spontaneously between 6 and 65°C, in 0.1–4.5 M acetate and pH 4.2–5.0. The anti-malarial drugs quinine, chloroquine and amodiaq...

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Bibliographic Details
Published in:FEBS letters 1994-09, Vol.352 (1), p.54-57
Main Authors: Egan, Timothy J., Ross, David C., Adams, Paul A.
Format: Article
Language:English
Subjects:
Antimalarials - pharmacology
Haem
Haemozoin
Hemeproteins - metabolism
Hydrogen-Ion Concentration
Pigments, Biological - metabolism
Plasmodium
Polymers
Quinoline anti-malarial drug
Solubility
Temperature
β-Haematin
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Summary:Polymerisation of haematin to β-haematin (haemozoin or malaria pigment) in acidic acetate solutions was studied using infrared spectroscopy. The reaction was found to occur spontaneously between 6 and 65°C, in 0.1–4.5 M acetate and pH 4.2–5.0. The anti-malarial drugs quinine, chloroquine and amodiaquin were found to block spontaneous β-haematin formation, while the anti-malarially inactive 9-epiquinine and 8-hydroxyquinoline had no effect on the reaction, as did primaquine, a drug which is active only against exo-erythrocytic stages of infection. It is argued that the intra-erythrocytically active anti-malarial agents act by binding to haematin, blocking β-haematin formation and leaving toxic haematin in the parasite food vacuoles.
ISSN:0014-5793
1873-3468
DOI:10.1016/0014-5793(94)00921-X