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

FEBS Letters

Adams, Paul A.²  Egan, Timothy J.¹  Ross, David C.¹ 

[1] Department of Chemical Pathology, Institute of Child Health, Red Cross War Memorial Children's Hospital, Private Bag, Rondebosch 7700, South Africa;Department of Chemical Pathology, University of Cape Town Medical School, Observatory, South Africa

关键词: Quinoline anti-malarial drug;    Haem;    β-Haematin;    Haemozoin;   

DOI  :  10.1016/0014-5793(94)00921-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown