Effect of 5-chloro-7-iodo-8-hydroxy-quinoline (clioquinol) on the uptake and distribution of nickel, zinc and mercury in mice. 1984

H Tjälve, and K Ståhl

5-Chloro-7-iodo-8-hydroxy-quinoline (clioquinol) was found to induce a very marked increase in the concentration of 63Ni2+ in various tissues of mice when given orally together with the metal, compared with oral administrations of 63Ni2+ only. Markedly increased tissue concentrations, although less expressed than for the 63Ni2+, were also observed for 65Zn2+. Clioquinol increased the tissue levels of 203Hg2+ to a lesser extent. When clioquinol was given intraperitoneally and 63Ni2+ was given intravenously there were also very markedly increased tissue levels of the metal, compared with intravenous injections of 63Ni2+ only. It was also shown that the urinary excretion of 63Ni2+ was greatly increased in mice given the metal orally together with clioquinol, compared with mice given the 63Ni2+ only. Clioquinol and other 8-hydroxy-quinolines form lipophilic chelates with metallic cations and the observed effects on the tissue-disposition of the metals are probably due to a facilitated penetration through the cellular membranes. Determinations of the chloroform:water partition coefficients showed the highest lipophilicity for the nickel-clioquinol-complex followed in decreasing order by the complexes with zinc and mercury. These data suggest that the ability of the clioquinol to affect the uptake of the metals in the cells may be related to the relative lipophilicity of the metal-clioquinol-complexes. Clioquinol and other halogenated 8-hydroxy-quinolines are linked with the SMON-syndrom, which has been observed preferentially in Japan. It is suggested that the pathogenesis of SMON may involve an accumulation of toxic concentrations of metals in the tissues due to facilitated uptake by complex-formation with halogenated 8-hydroxy-quinolines.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007464 Clioquinol A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide. Chloroiodoquine,Iodochlorhydroxyquin,Iodochloroxyquinoline,5-Chloro-7-iodo-8-quinolinol,Chinoform,Entero-Septol,Entero-Vioform,Enteroquinol,Vioform,5 Chloro 7 iodo 8 quinolinol,Entero Septol,Entero Vioform,EnteroSeptol,EnteroVioform
D008628 Mercury A silver metallic element that exists as a liquid at room temperature. It has the atomic symbol Hg (from hydrargyrum, liquid silver), atomic number 80, and atomic weight 200.59. Mercury is used in many industrial applications and its salts have been employed therapeutically as purgatives, antisyphilitics, disinfectants, and astringents. It can be absorbed through the skin and mucous membranes which leads to MERCURY POISONING. Because of its toxicity, the clinical use of mercury and mercurials is diminishing.
D008810 Mice, Inbred C57BL One of the first INBRED MOUSE STRAINS to be sequenced. This strain is commonly used as genetic background for transgenic mouse models. Refractory to many tumors, this strain is also preferred model for studying role of genetic variations in development of diseases. Mice, C57BL,Mouse, C57BL,Mouse, Inbred C57BL,C57BL Mice,C57BL Mice, Inbred,C57BL Mouse,C57BL Mouse, Inbred,Inbred C57BL Mice,Inbred C57BL Mouse
D009422 Nervous System Diseases Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle. Neurologic Disorders,Nervous System Disorders,Neurological Disorders,Disease, Nervous System,Diseases, Nervous System,Disorder, Nervous System,Disorder, Neurologic,Disorder, Neurological,Disorders, Nervous System,Disorders, Neurologic,Disorders, Neurological,Nervous System Disease,Nervous System Disorder,Neurologic Disorder,Neurological Disorder
D009532 Nickel A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.
D005260 Female Females
D006912 Hydroxyquinolines The 8-hydroxy derivatives inhibit various enzymes and their halogenated derivatives, though neurotoxic, are used as topical anti-infective agents, among other uses. Quinolinols,Chiniofon
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D014018 Tissue Distribution Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios. Distribution, Tissue,Distributions, Tissue,Tissue Distributions

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