A Common Mechanism for Blockade of Heme Polymerization by Antimalarial Quinolines
نویسندگان
چکیده
منابع مشابه
Inhibition of Heme Polymerization, the Mechanism of Antimalarial Activity in Phlomis caucasica Rech.f. (Lamiaceae)
Background: Malaria is one of the most important parasitic diseases in the world caused by Plasmodium species. The malaria parasite digests hemoglobin in vacuole to amino acids and heme. Plasmodium has got several detoxification mechanisms to protect itself from toxic heme. The most important mechanism is heme polymerization. Identifying compounds that inhibit heme polymerization is an approach...
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Background and objectives: Viola odorata L. is a grassy plant that grows in the humid regions and has been used to treat liver diseases and complicated and tropical fevers in Iranian traditional medicine (ITM). V. odorata has cold and humid temperament while the temperament of fever which is the most important symptom of malaria is the opposite. Antimalarial a...
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Background and objectives: There are several methods to assess the in vitro capability of heme inhibitory activity of antimalarial compounds; most of them require some specific equipment or toxic substances and sometimes the needed materials are not accessible. Regarding the necessity and importance of optimizing and standardizing experimental conditions, the present s...
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We have investigated the contribution of drug accumulation and inhibition of heme polymerization to the in vitro activities of a series of antimalarial drugs. Only those compounds exhibiting structural relatedness to the quinolines inhibited heme polymerization. We could find no direct correlation between in vitro activity against chloroquine-susceptible or chloroquine-resistant isolates and ei...
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Chloroquine is thought to exert its antimalarial effect by preventing the polymerization of toxic heme released during proteolysis of hemoglobin in the Plasmodium digestive vacuole. The mechanism of this blockade has not been established. We incubated cultured parasites with subinhibitory doses of [3H]chloroquine and [3H] quinidine. These [3H]quinoline compounds became associated with hemozoin ...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1998
ISSN: 0021-9258
DOI: 10.1074/jbc.273.47.31103