FEBS Lett. 1994 Sep 19;352(1):54-7.

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

Source

Department of Chemical Pathology, Red Cross War Memorial Children's Hospital, Rondebosch, South Africa.

Abstract

Polymerisation of haematin to beta-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 degrees 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 beta-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 beta-haematin formation and leaving toxic haematin in the parasite food vacuoles.

PMID:: 7925942; [PubMed - indexed for MEDLINE]

Publication Types, MeSH Terms, Substances

Publication Types

Research Support, Non-U.S. Gov't

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

COS Scholar Universe

Libraries

LinkOut Holdings

Supplemental Content

Save items

Related citations in PubMed

Review Haematin (haem) polymerization and its inhibition by quinoline antimalarials. [Ann Trop Med Parasitol. 1997]
Review Haematin (haem) polymerization and its inhibition by quinoline antimalarials.
Ridley RG, Dorn A, Vippagunta SR, Vennerstrom JL. Ann Trop Med Parasitol. 1997 Jul; 91(5):559-66.
Formation of haemozoin/beta-haematin under physiological conditions is not spontaneous. [FEBS Lett. 1996]
Formation of haemozoin/beta-haematin under physiological conditions is not spontaneous.
Pandey AV, Tekwani BL. FEBS Lett. 1996 Sep 16; 393(2-3):189-93.
Non-iron porphyrins inhibit beta-haematin (malaria pigment) polymerisation. [FEBS Lett. 1997]
Non-iron porphyrins inhibit beta-haematin (malaria pigment) polymerisation.
Basilico N, Monti D, Olliaro P, Taramelli D. FEBS Lett. 1997 Jun 9; 409(2):297-9.
A comparison and analysis of several ways to promote haematin (haem) polymerisation and an assessment of its initiation in vitro. [Biochem Pharmacol. 1998]
A comparison and analysis of several ways to promote haematin (haem) polymerisation and an assessment of its initiation in vitro.
Dorn A, Vippagunta SR, Matile H, Bubendorf A, Vennerstrom JL, Ridley RG. Biochem Pharmacol. 1998 Mar 15; 55(6):737-47.
Review Theories on malarial pigment formation and quinoline action. [Int J Parasitol. 2002]
Review Theories on malarial pigment formation and quinoline action.
Sullivan DJ. Int J Parasitol. 2002 Dec 4; 32(13):1645-53.

See reviews... See all...

Cited by 21 PubMed Central articles

The mechanism of antimalarial action of [Au(CQ)(PPh(3))]PF(6): structural effects and increased drug lipophilicity enhance heme aggregation inhibition at lipid/water interfaces. [J Inorg Biochem. 2011]
The mechanism of antimalarial action of [Au(CQ)(PPh(3))]PF(6): structural effects and increased drug lipophilicity enhance heme aggregation inhibition at lipid/water interfaces.
Navarro M, Castro W, Martínez A, Sánchez Delgado RA. J Inorg Biochem. 2011 Feb; 105(2):276-82. Epub 2010 Nov 13.
The hydroxyl functionality and a rigid proximal N are required for forming a novel non-covalent quinine-heme complex. [J Inorg Biochem. 2011]
The hydroxyl functionality and a rigid proximal N are required for forming a novel non-covalent quinine-heme complex.
Alumasa JN, Gorka AP, Casabianca LB, Comstock E, de Dios AC, Roepe PD. J Inorg Biochem. 2011 Mar; 105(3):467-75. Epub 2010 Sep 22.
Lipophilic mediated assays for beta-hematin inhibitors. [Comb Chem High Throughput Scre...]
Lipophilic mediated assays for beta-hematin inhibitors.
Carter MD, Phelan VV, Sandlin RD, Bachmann BO, Wright DW. Comb Chem High Throughput Screen. 2010 Mar; 13(3):285-92.

See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Quinoline anti-malarial drugs inhibit spontaneous formation of beta-haematin (ma...
Quinoline anti-malarial drugs inhibit spontaneous formation of beta-haematin (malaria pigment).
FEBS Lett. 1994 Sep 19 ;352(1):54-7.

PubMed
Studies on the infectivity of tropical African strains of Plasmodium falciparum ...
Studies on the infectivity of tropical African strains of Plasmodium falciparum to some southern European vectors of malaria.
Parassitologia. 1975 Jan-Dec ;17(1-3):39-48.

PubMed
A longitudinal study of naturally acquired cellular and humoral immune responses...
A longitudinal study of naturally acquired cellular and humoral immune responses to a merozoite surface protein (MSP1) of Plasmodium falciparum in an area of seasonal malaria transmission.
Parasite Immunol. 1993 Sep ;15(9):513-24.

PubMed
Malaria - the mime. Recent lessons from a group of civilian travellers.
Malaria - the mime. Recent lessons from a group of civilian travellers.
Am J Med. 1976 Aug ;61(2):159-64.

PubMed
Serum antibodies from malaria-exposed people recognize conserved epitopes formed...
Serum antibodies from malaria-exposed people recognize conserved epitopes formed by the two epidermal growth factor motifs of MSP1(19), the carboxy-terminal fragment of the major merozoite surface protein of Plasmodium falciparum.
Infect Immun. 1995 Feb ;63(2):456-66.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to: