ABSTRACT
We studied the effects of some aniline and dioxaborininopyridine derivatives on the rate of oxidative deamination of putrescine and polyamines in a tissue with high mitotic index. These effects were evaluated quantitatively by measuring diamine oxidase and polyamine oxidase activities in a model cell-free test system of regenerating rat liver tissue. Aniline derivatives exhibited mainly antiproliferative effects and promoted oxidative degradation of putrescine, spermidine, and spermine. Dioxaborininopyridine derivatives inhibited this process, thus exhibiting carcinogenic properties.
Subject(s)
Amine Oxidase (Copper-Containing)/chemistry , Aniline Compounds/pharmacology , Antineoplastic Agents/pharmacology , Boron Compounds/pharmacology , Carcinogens/pharmacology , Oxidoreductases Acting on CH-NH Group Donors/chemistry , Pyridines/pharmacology , Aniline Compounds/chemical synthesis , Animals , Antineoplastic Agents/chemical synthesis , Boron Compounds/chemical synthesis , Carcinogens/chemical synthesis , Cell-Free System/chemistry , Cell-Free System/drug effects , Cell-Free System/metabolism , Enzyme Assays , Kinetics , Liver/chemistry , Liver/metabolism , Liver Regeneration , Male , Oxidation-Reduction , Putrescine/chemistry , Pyridines/chemical synthesis , Rats , Spermidine/chemistry , Spermine/chemistry , Structure-Activity Relationship , Polyamine OxidaseABSTRACT
For the development of methods of additional differential diagnostics of gliomas of various grades of malignancy and gliomas and local inflammatory processes in the CNS we studied the intensity of aggregation of peripheral blood cells under the influence of channel blockers ketamine and verapamil. In in vitro experiments, verapamil and ketamine in various dilutions (from 10 to 100,000 times) were added to blood samples and the effects of these dilutions on the intensity of blood aggregation in patients with gliomas of different degree of malignancy, traumatic brain injuries, and other types of neurosurgical pathologies were studied. A correlation was revealed between the decrease in surface charge of blood cells and the type of neurosurgical pathology. The use of functional properties of potential-dependent inotropic NMDA receptors and calcium channels allowed indirect estimation of their activity via parameters of blood cell aggregation induced by channel blockers ketamine and verapamil.
