title: Modulating effect of new potential antimelanomic agents, spin-labeled triazenes and nitrosoureas on the DOPA-oxidase activity of tyrosinase.
abstract: The modulating effect of newly synthesized alkylating spin labeled triazene and spin labeled nitrosourea derivatives on the DOPA-oxidase activity of mushroom tyrosinase has been investigated by Bumett's spectrophotometric method (Burnett et al., 1967). All spin labeled triazenes have exhibited activating effect on DOPA-oxidase activity of tyrosinase, whereas clinically used triazene (DTIC), which does not contain nitroxide moiety, have showed inhibiting effect. At the same experimental conditions the spin labeled aminoacid nitrosoureas have showed dual effect - activating, in the beginning of the enzyme reaction and inhibiting later on. It is deduced that the activating effect of the spin labeled compounds is due to the nitroxide moiety and the inhibiting effect of all compounds depends on their half-life time. This study might contribute to make more clear the mechanism of action of the new compounds and on the other hand would come in quite useful as a preliminary prognosis for their antimelanomic activity.
authors.affiliation: Department of Chemistry and Biochemistry, Medical Faculty, Stara Zagora, Bulgaria.
authors.forename: V
authors.initials: V
authors.lastname: Gadjeva
authors.forename: A
authors.initials: A
authors.lastname: Zheleva
authors.forename: E
authors.initials: E
authors.lastname: Raikova
mesh_terms: D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000494:pharmacology*; D002384:Catalysis; D003497:Cyclic N-Oxides / Q000737:chemistry / Q000494:pharmacology; D003606:Dacarbazine / Q000737:chemistry / Q000494:pharmacology; D004295:Dihydroxyphenylalanine / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D008130:Lomustine / Q000737:chemistry / Q000494:pharmacology; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000201:enzymology*; D051379:Mice; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors; D009607:Nitrosourea Compounds / Q000494:pharmacology*; D010084:Oxidation-Reduction; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D010940:Plant Proteins / Q000037:antagonists & inhibitors; D013053:Spectrophotometry; D013113:Spin Labels; D013329:Structure-Activity Relationship; D014226:Triazenes / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000201:enzymology
chemical_list: D018906:Antineoplastic Agents, Alkylating; D003497:Cyclic N-Oxides; D004791:Enzyme Inhibitors; D009363:Neoplasm Proteins; D009607:Nitrosourea Compounds; D010880:Piperidines; D010940:Plant Proteins; D013113:Spin Labels; D014226:Triazenes; D004295:Dihydroxyphenylalanine; D008130:Lomustine; D003606:Dacarbazine; D014442:Monophenol Monooxygenase