Some properties of the polyamine deprivation-inducible uptake system for methylglyoxal bis(guanylhydrazone) in tumor cells. 1981

P Seppänen

Intracellular polyamine deprivation, produced by DL-alpha-difluoromethylornithine (DFMO), resulted in a striking enhancement of cellular transport of the natural polyamines and methylglyoxal bis(guanylhydrazone) (MGBG). In addition to the natural polyamines and MGBG, the uptake of other diamines and triamines was likewise enhanced in response to DFMO, although longer than three-carbon backbone was required for about 10-fold stimulation to occur. Intracellular deprivation of polyamines did not increase the affinity of the transport system for MGBG but greatly enhanced the maximum velocity of the drug transport. The uptake process of MGBG was temperature dependent and the activation energy (Ea = 67.5 kJ) for the uptake system was the same for both the polyamine-depleted tumour cells and for the untreated cells. The uptake of the drug appeared to be more dependent on the Na+-linked uptake, as indicated by the inhibitory effect of ouabain, than on energy production. Deprivation of putrescine and spermidine changed the intracellular distribution of MGBG since a major portion of the drug was concentrated in the microsomal fraction in polyamine-depleted cells.

UI MeSH Term Description Entries
D007461 Iodoacetates Iodinated derivatives of acetic acid. Iodoacetates are commonly used as alkylating sulfhydryl reagents and enzyme inhibitors in biochemical research. Iodoacetic Acids,Acids, Iodoacetic
D008935 Mitoguazone Antineoplastic agent effective against myelogenous leukemia in experimental animals. Also acts as an inhibitor of animal S-adenosylmethionine decarboxylase. Methylglyoxal Bis(guanylhydrazone),MGBG,Methyl-gag,NSC-32946,Methyl gag,Methylgag,NSC 32946,NSC32946
D009374 Neoplasms, Experimental Experimentally induced new abnormal growth of TISSUES in animals to provide models for studying human neoplasms. Experimental Neoplasms,Experimental Neoplasm,Neoplasm, Experimental
D009952 Ornithine An amino acid produced in the urea cycle by the splitting off of urea from arginine. 2,5-Diaminopentanoic Acid,Ornithine Dihydrochloride, (L)-Isomer,Ornithine Hydrochloride, (D)-Isomer,Ornithine Hydrochloride, (DL)-Isomer,Ornithine Hydrochloride, (L)-Isomer,Ornithine Monoacetate, (L)-Isomer,Ornithine Monohydrobromide, (L)-Isomer,Ornithine Monohydrochloride, (D)-Isomer,Ornithine Monohydrochloride, (DL)-Isomer,Ornithine Phosphate (1:1), (L)-Isomer,Ornithine Sulfate (1:1), (L)-Isomer,Ornithine, (D)-Isomer,Ornithine, (DL)-Isomer,Ornithine, (L)-Isomer,2,5 Diaminopentanoic Acid
D010042 Ouabain A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE. Acocantherin,G-Strophanthin,Acolongifloroside K,G Strophanthin
D011073 Polyamines Amine compounds that consist of carbon chains or rings containing two or more primary amino groups. Polyamine
D011700 Putrescine A toxic diamine formed by putrefaction from the decarboxylation of arginine and ornithine. 1,4-Butanediamine,1,4-Diaminobutane,Tetramethylenediamine,1,4 Butanediamine,1,4 Diaminobutane
D002286 Carcinoma, Ehrlich Tumor A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms. Ehrlich Ascites Tumor,Ascites Tumor, Ehrlich,Ehrlich Tumor Carcinoma,Tumor, Ehrlich Ascites
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D006146 Guanidines A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.

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P Seppänen
October 1985, Archives of biochemistry and biophysics,
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