Chloroquine hemazoin

Discussion in 'Canadian Pharmacies' started by wolflen, 10-Mar-2020.

  1. mаlu Well-Known Member

    Chloroquine hemazoin


    These hematophagous organisms such as Malaria parasites (Plasmodium spp.), Rhodnius and Schistosoma digest haemoglobin and release high quantities of free heme, which is the non-protein component of hemoglobin. Heme is a prosthetic group consisting of an iron atom contained in the center of a heterocyclic porphyrin ring.

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    Chloroquine acts by forming toxic complexes with heme molecules and interfering with their crystallization. 381 This mechanism of action explains why chloroquine is effective against developing intraerythrocytic trophozoites but ineffective against other parasite stages i.e. mature gametocytes, liver schizonts that do not actively consume. Hemozoin is involved in several aspects of the pathology of the disease as well as in important processes such as the immunogenicity elicited. It is known that the once best antimalarial drug, chloroquine, exerted its effect through interference with the process of hemozoin formation. Chloroquine is a 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite.

    In malaria parasites, hemozoin is often called malaria pigment. Free heme is toxic to cells, so the parasites convert it into an insoluble crystalline form called hemozoin.

    Chloroquine hemazoin

    Chloroquine - FDA prescribing information, side effects and uses, Malarial Hemozoin From target to tool

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  6. This chapter analyzes the effect of Chloroquine CQ on hemozoin. The worldwide spread of CQ resistance has led to a significant resurgence of malaria

    • Chapter 7 Chloroquine and Hemozoin - ScienceDirect.
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    Hemozoin collects in the digestive vacuole as insoluble crystals. citation needed Chloroquine enters the red blood cell by simple diffusion, inhibiting the parasite cell and digestive vacuole. Chloroquine then becomes protonated to CQ2+, as the digestive vacuole is known to be acidic pH 4.7; chloroquine then cannot leave by diffusion. Hydroxychloroquine and chloroquine have been recommended by Chinese and South Korean health authorities for the treatment COVID-19. In vitro studies have demonstrated that hydroxychloroquine is more potent than chloroquine against SARS-CoV-2 with a more tolerable safety profile. A 2-μM concentration of chloroquine fully arrests layer generation and step advancement, which is ∼10 4 × less than hematin’s physiological concentration. Our results suggest that adsorption at specific growth sites may be a general mode of hemozoin growth inhibition for the quinoline antimalarials.

     
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  10. Uz___ Moderator

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