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Quinoline anti‐malarial drugs inhibit spontaneous formation of β‐haematin (malaria pigment)
Open accessAbstract
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.
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Citations
Cited by
The Plasmodium digestive Vacuole: Metabolic Headquarters and Choice Drug Target
Olliaro, P. L., & Goldberg, D. E. (1995) · Parasitology Today · doi:10.1016/0169-4758(95)80042-5 · Cited by 139
The Peculiarities and Paradoxes of Plasmodium Heme Metabolism
Sigala, P. A., & Goldberg, D. E. (2014) · Annual Review of Microbiology · doi:10.1146/annurev-micro-091313-103537 · Cited by 129
Haemozoin: from melatonin pigment to drug target, diagnostic tool, and immune modulator
Hänscheid, T., Egan, T. J., & Grobusch, M. P. (2007) · The Lancet Infectious Diseases · doi:10.1016/s1473-3099(07)70238-4 · Cited by 128
Self-citationInnate inflammatory response to the malarial pigment hemozoin
Shio, M. T., Kassa, F. A., Bellemare, M.-J., & Olivier, M. (2010) · Microbes and Infection · doi:10.1016/j.micinf.2010.07.001 · Cited by 96
Haemozoin: Identification and quantification
Sullivan, A. D., & Meshnick, S. R. (1996) · Parasitology Today · doi:10.1016/0169-4758(96)40001-1 · Cited by 19
Metadata
- Authors
- Egan, T. J., Ross, D. C., & Adams, P. A.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1994-09-19
- Volume
- 352
- Issue
- 1
- Pages
- 54-57
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2092604097
- Cited by
- 372
- References
- 0
- FWCI
- 16.76
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Egan, T. J., Ross, D. C., & Adams, P. A. (1994). Quinoline anti‐malarial drugs inhibit spontaneous formation of β‐haematin (malaria pigment). FEBS Letters. https://doi.org/10.1016/0014-5793(94)00921-x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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