Chloroquine intercalating

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  1. z0nata User

    Chloroquine intercalating

    Chloroquine has been extensively used in mass drug administrations, which may have contributed to the emergence and spread of resistance. It is recommended to check if chloroquine is still effective in the region prior to using it.

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    The mode of action of chloroquine is still controversial. Proposed mechanisms of action include 1 DNA intercalation, 2 lysosome accumulation and 3 binding to ferriprotoporphyrin IX. Recent data suggest that intercalation into parasite DNA can occur at physiological concentrations of the drug. The usefulness of hypokalemia as an indicator in the evaluation of chloroquine toxicity was studied in a retrospective series of 191 acute chloroquine poisonings. Results indicated that the risk of severe poisoning and death are proportional to the degree of hypokalemia. Chloroquine, like other intercalators, may work by altering three-dimensional structure. For exam- ple, there is evidence that DNA may form left-handed helices Z-DNAin transcriptionally active regions. We have found that chloroquine prevents the transition of DNA to the Z form in vitro, at concentrations as low as 20 Ref. 17.

    The Centers for Disease Control and Prevention recommend against treatment of malaria with chloroquine alone due to more effective combinations. In areas where resistance is present, other antimalarials, such as mefloquine or atovaquone, may be used instead.

    Chloroquine intercalating

    Medicines for the Prevention of Malaria While Traveling., Chloroquine Side Effects Common, Severe, Long Term.

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  5. Mechanism of action Chloroquine basic concentrates in parasite food vacuole acidic. Prevent heme polymerization into hemozoin causing heme accumulation toxic to parasite. Drug complex with heme disrupt cell membrane function. Other mechanism include intercalating of parasite DNA, DNA synthesis inhibition. 7.

    • Chloroquine - SlideShare.
    • Chloroquine as intercalator a hypothesis revived - ScienceDirect.
    • Curved DNA Design, synthesis, andcircularization.

    Chloroquine enjoys a renaissance as an antineoplastic therapy Therapeutic Perspective Clin. Invest. 2013 38 745 Table 1. Clinical trials investigating the safety/efficacy of chloroquine or hydroxychloroquine monotherapy or combination therapy. Investigative agents Conditions Trial ID number Phase Location Status Ref. Also, a concentration-dependent inhibition of chloroquine was obtained with prodigiosin-treated DNA. Chloroquine is an intercalating agent that unwinds DNA, resulting in a decrease in negative superhelicity and thus in the negative superhelical free energy activity. To understand how chloroquine CQ enhances transgene expression in polycation-based, nonviral gene delivery systems, a number of CQ analogues with variations in the aliphatic amino side chain or in the aromatic ring are synthesized and investigated.

  6. Mr.Artix Guest

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