Chloroquine inhibit the novel heme polymerase enzyme

Discussion in 'Chloroquine 250' started by sumbur, 28-Feb-2020.

  1. matchless777 Moderator

    Chloroquine inhibit the novel heme polymerase enzyme


    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.

    Chloroquine and release of cargo Plaquenil sideceffects

    In this review the recent discovery that chloroquine and related quinolines inhibit the novel heme polymerase enzyme that is also present in the trophozoite food vacuole is introduced. The proposal that this inhibition of heme polymerase can explain the specific toxicity of these drugs for the intraerythrocytic malaria parasite is then. Although the mechanism of action is not fully 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. Chloroquine may also interfere with the biosynthesis of nucleic acids. Eckman JR, Modler S, Eaton JW, Berger E, Engel RR. Host heme catabolism in drug-sensitive and drug-resistant malaria. J Lab Clin Med. 1977 Oct; 90 4767–770. Slater AF, Cerami A. Inhibition by chloroquine of a novel haem polymerase enzyme activity in malaria trophozoites. Nature. 1992 Jan 9; 355 6356167–169.

    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 inhibit the novel heme polymerase enzyme

    On the molecular mechanism of chloroquine's antimalarial action PNAS, Chloroquine sulfate C18H28ClN3O4S - PubChem

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    All heme polymerase activity is destroyed by heating at 100 degrees C for 3 minutes. Chloroquine treatment of malarious mice reduces by 80 percent the activity of this enzyme, without inhibiting release of FP from hemoglobin, and thereby causes excess nonpolymerized, nonhemozoin FP to accumulate. Jul 18, 2017 This is the least-effective mechanism of heme crystal growth inhibition. In a second mechanism, known as “step-pinning,” the quinolines, such as chloroquine and quinine, bind anywhere on a flat surface face in addition to kink sites. By this process, heme crystal formation is inhibited over broad areas of the crystal surface. C. inhibit heme polymerase, an enzyme that converts toxic heme into nontoxic hemazoin. D. raise the internal pH, clump the plasmodial pigment, and intercalate into plasmodial DNA. B. form reactive oxygen intermediates inside Plasmodium-infected red blood cells.

     
  6. UralM New Member

    Chloroquine has long been used in the treatment or prevention of malaria from Plasmodium vivax, P. malariae, excluding the malaria parasite Plasmodium falciparum, for it started to develop widespread resistance to it. Dissecting pharmacological effects of chloroquine in cancer. Chloroquine and hydroxychloroquine for cancer therapy Synergistic anti-tumour effects of tetrandrine and chloroquine.
     
  7. mainpartner New Member

    May 19, 2004 -- Cutting pills in half is a widely accepted strategy for lowering the cost of prescription medications, and there has even been talk by some insurers of mandating the practice for certain drugs. Lupus Medicines Hydroxychloroquine - Brigham and Women's Hospital Rx Side Effects New Plaquenil Guidelines and More. Plaquenil side effects - kidney problems? - Symptoms - Life With Lupus
     
  8. london Well-Known Member

    Hydroxychloroquine Oral Uses, Side Effects, Interactions. Hydroxychloroquine is used to prevent or treat malaria infections caused by mosquito bites. It does not work against certain types of malaria chloroquine-resistant. The United States Center for.

    Hydroxychloroquine Sulfate Sandoz Inc FDA Package Insert
     
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