Concentrations Of Quinacrine Research Articles

Studies on the measurement of tissue levels of administered quinacrine and lodoquinacrine

AbstractThe uptake of administered quinacrine was studied in normal tissues and in Walker. 256 carcinosarcoma tumors implanted in livers and stomachs of rats. Tissue concentrations were measured by a fluorometric technique. The concentration of quinacrine in tumors as compared to that in the liver (T/L ratios) or in the stomach (T/S ratios) was directly related to the size of the tumor. These ratios averaged > 3 in animals with the smallest tumors and < 1 in animals with large tumors. Additional studies comparing uptake of quinacrine and iodoquinacrine suggested that peak T/L ratios occurred at 1 to 3 days with the former compound, with an earlier peak occurring at 1 day with the latter chemical. It is speculated that cancer diagnostic techniques could be developed using tissue measurements, histochemistry, or radioactive scanning of these compounds.

Erratum: Fluorescent Labeling of Chromosomal DNA: Superiority of Quinacrine Mustard to Quinacrine

In "Fluorescent labeling of chromosomal DNA: Superiority of quinacrine mustard to quinacrine" by T. Caspersson, L. Zech, and E. J. Modest [170, 762 (1970)] lines 10 through 14 of paragraph 2, column 3, page 762 should read "the optimum concentrations of quinacrine (5 to 10 mg/ml) compared with quinacrine mustard (50 μg/ml) are in the ratio of 100 to 200. . . ."

Nicotinamide adenine dinucleotide photoreduction with Chromatium and Rhodospirillum rubrum chromatophores

The photoreduction of nicotinamide adenine dinucleotide (NAD) catalyzed by Rhodospirillum rubrum and Chromatium chromatophores was compared. Both preparations catalyze a light-induced electron transfer from either succinate or reduced 2,6-dichlorophenolindophenol (DPIPH 2) to NAD. Varying concentrations of quinacrine, oligomycin, and gramicidin inhibited the photoreductions in a similar manner, regardless of which electron donor or chromatophore preparation was employed. The light-induced transfer of electrons from DPIPH 2 (reduced by excess ascorbate) to NAD was inhibited by 2- n-heptyl-4-hydroxyquinoline-N-oxide (HOQNO) in the case of Chromatium chromatophores, but not with R. rubrum chromatophores. Rhodospirillum rubrum particles were equally sensitive to carbonylcyanide m-chlorophenyl-hydrazone ( m-Cl-CCP) inhibition, regardless of which electron donor was employed. In contrast, electron transfer from DPIPH 2 to NAD in Chromatium preparations was more sensitive to m-Cl-CCP than the transfer from succinate to NAD. Inhibition of photophosphorylation with Chromatium preparations by m-Cl-CCP, HOQNO and o-phenanthroline paralleled the inhibition of the photo-induced reduction of NAD by succinate. At a given concentration of inhibitor photophosphorylation was more sensitive to oligomycin and less sensitive to gramicidin than NAD photoreduction. Reduced ubiquinone-2 also serves as an electron donor for the Chromatium system.

Carbohydrate metabolism of schistosoma mansoni.

1. Schistosoma mansoni utilizes in 1 hour an amount of glucose equivalent to one-sixth to one-fifth of its dry weight. Over 80 per cent of the metabolized glucose is converted to lactic acid by this organism. 2. The rates of glucose utilization and of lactic acid production by S. mansoni are the same under aerobic and under anaerobic conditions. 3. A high rate of lactic acid production and the absence of a postanaerobic increase in the oxygen uptake differentiate S. mansoni from most other parasitic helminths whose metabolism has been studied. 4. Arsenite and p-chloromercuric benzoate inhibit in low concentrations the oxygen uptake and the rate of glycolysis of S. mansoni. This inhibition is not prevented or reversed by an excess of glutathione or of thioglycollate. 5. Fluoride inhibits the removal of glucose and the production of lactic acid by S. mansoni to the same degree. 6. Low concentrations of quinacrine (atabrine) do not affect the respiration or the carbohydrate metabolism of the schistosomes. 7. The inhibitory effect of aldehydes on the metabolism of S. mansoni has been measured. Among this group of compounds dl-glyceraldehyde and o-nitrobenzaldehyde are the most effective inhibitors of glycolysis. 8. In a concentration of 2.6 x 10(-6)M (1:1,000,000) a cyanine dye inhibits almost completely the respiration of the schistosomes, but has no effect on their rate of glycolysis. The oxygen uptake of the worms is inhibited by fuadin to a greater degree than their rate of glycolysis. 2-methyl-1,4-napthoquinone is a much more effective inhibitor of glycolysis than of the respiration of S. mansoni. The latter compound interacts with plasma albumin and, therefore, its inhibitory action on the metabolism of the schistosomes is greatly reduced in human serum or plasma. 9. Evidence is discussed which indicates that, in contrast to glycolysis, respiratory metabolism is not essential for the survival of S. mansoni.

PLASMA QUINACRINE CONCENTRATION IN TREATMENT OF PLASMODIUM VIVAX MALARIA ACQUIRED IN THE SOUTH PACIFIC

The development of an adequate technic for determining plasma quinacrine concentrations¹has facilitated the investigation of several important phases of therapy for soldiers evacuated from the South Pacific with chronic relapsing Plasmodium vivax malaria. The concentrations of quinacrine in plasma attained at selected intervals as the result of oral administration of known amounts of the drug have been determined for specific dosages. Determinations were made on 6,733 specimens from 291 patients during and after treatment for four hundred and twelve attacks of malaria at Harmon General Hospital. <h3>METHODS</h3> The method of Brodie and Udenfriend¹was employed in the determination of the concentration of quinacrine in plasma. Plasma was used instead of whole blood because these investigators stated that variations in values in whole blood quinacrine concentrations are often reflections of changes in the number of leukocytes, since they contain a concentration several hundred times that of plasma. Shortly