ABSTRACT
Neurotropic, neuroprotective and antioxidant actions of the enantiomers and the racemate of 2-(3,7-dioxo-2,4,6,8-tetraazabicyclo[3.3.0]oct-2-yl)-4-methylthiobutanoic acid were investigated. Only (+)-(S)-2-(3,7-dioxo-2,4,6,8-tetraazabicyclo[3.3.0]oct-2-yl)-4-methylthiobutanoic acid was found to have neuroprotective properties. A distereoselective synthesis of enantiomers and racemate was performed by condensations of (S), (R) and (R,S)-N-carbamoylmethionines with 4,5-dihydroxyimidazolidin-2-one (DHI), respectively. By the X-ray method, the major racemate was proved to crystallize from water as a conglomerate. No antioxidant activity was revealed.
Subject(s)
Butyrates/chemistry , Butyrates/chemical synthesis , Neuroprotective Agents/chemistry , Neuroprotective Agents/chemical synthesis , Animals , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Butyrates/pharmacology , Male , Mice , Molecular Structure , Neuroprotective Agents/pharmacologyABSTRACT
Water-soluble sulfate polysalts of carboxymethyl cellulose and tertiary aminomethyl derivatives of 2-isobornyl-4-methylphenol was obtained. For the synthesized conjugates investigated in vivo anti-inflammatory activity in the test of acute formalin inflammation and analgesic activity in tests the "hot plate" and "vinegar cramps".
Subject(s)
Carboxymethylcellulose Sodium , Inflammation , Pain Measurement/drug effects , Pain , Animals , Carboxymethylcellulose Sodium/analogs & derivatives , Carboxymethylcellulose Sodium/chemical synthesis , Carboxymethylcellulose Sodium/chemistry , Carboxymethylcellulose Sodium/pharmacology , Formaldehyde/toxicity , Inflammation/chemically induced , Inflammation/drug therapy , Mice , Pain/drug therapy , Pain/pathology , Solubility , Sulfates/chemical synthesis , Sulfates/chemistry , Sulfates/pharmacology , Water/chemistryABSTRACT
The immunotropic effect of the 2,3-seco derivatives of allobetulon, betulonic acid, and the methyl ester of betulonic acid were studied. It was found that the highest activity is shown by compounds with an oleanane fragment. The presence of a free C28-carboxyl group enhances the activity of lupeolic 2,3-seco derivatives. A significant contribution to the development of the immune response is introduced by a functional group at the C3 atom in the A ring - the C3-carboxy derivatives intensify the processes of antibody production and alter the number and ratio of leukocyte forms. It is shown that 2,3-seco-1-cyano-19beta,28-epoxy-18alpha-olean-3-oic acid stimulates humoral immunity with a positive influence on hematopoiesis.
Subject(s)
Immunologic Factors/pharmacology , Triterpenes/pharmacology , Animals , Antibody Formation/drug effects , Female , Immunity, Humoral/drug effects , Immunologic Factors/chemical synthesis , Immunologic Factors/chemistry , Mice , Oleanolic Acid/chemical synthesis , Oleanolic Acid/chemistry , Oleanolic Acid/pharmacology , Structure-Activity Relationship , Triterpenes/chemical synthesis , Triterpenes/chemistryABSTRACT
New lupane beta-enaminoketones were synthesized by interaction of methyl 2-hydroxymethylene-3-oxolup-20(29)-en-28-oate with aliphatic amines. Immunotropic activity was found for some of these compounds.
Subject(s)
Immunosuppressive Agents/chemical synthesis , Triterpenes/chemical synthesis , Animals , Antibody Formation , Esters , Immunity, Cellular , Immunosuppressive Agents/chemistry , Immunosuppressive Agents/immunology , Ketones/chemical synthesis , Ketones/immunology , Magnetic Resonance Spectroscopy , Male , Mice , Spectrophotometry, Infrared , Structure-Activity Relationship , Triterpenes/chemistry , Triterpenes/immunologyABSTRACT
2-Alkylaminomethylene-19beta,28-epoxyolean-3-ones were obtained by interaction of 2-hydroxymethylene-19beta,28-epoxyolean-3-one with aliphatic amines. Some of the resulting substances exhibit immunotropic activity.
Subject(s)
Oleanolic Acid/chemical synthesis , Oleanolic Acid/immunology , Terpenes/chemical synthesis , Terpenes/immunology , Amines/chemistry , Amines/immunology , Animals , Male , Mice , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/chemistry , Oleanolic Acid/pharmacology , Terpenes/chemistry , Terpenes/pharmacologyABSTRACT
The effects of the serotonin reuptake inhibitor fluoxetine (FL) and its complexes with glycyrrhizic acid (GA) in molar ratios of 1:1 (FLG-1) and 4:1 (FLG-4) on the behavior of adult rats were studied in an elevated cross maze, with measurement of brain monoamine and monamine metabolite levels. Agents were given via the intragastric route using a cannula at a dose of 25 mg/kg 1 h before testing. FL increased anxiety in the rats and decreased their movement activity; FLG-1 and FLG-4 had no effect on behavior. None of the agents affected brain serotonin content, though all decreased the levels of its metabolite 5-hydroxyindoleacetic acid in the hypothalamus, FLG-4 also decreasing this in the cortex. Noradrenaline levels in the hypothalamus were increased after FLG-1 and FLG-4. In the striatum, FL increased the levels of dopamine and its metabolite dihydroxyphenylacetic acid but had no effect on the level of transmitter catabolism. Unlike FL, FLG-1 activated dopamine metabolism in the striatum. Overall, use of FL complexed with GA significantly modified its behavioral effects, which appears to be associated with the effects of FL and its complexes on the function of the monoaminergic systems involved in controlling behavior.
Subject(s)
Anti-Infective Agents/pharmacology , Behavior, Animal/drug effects , Biogenic Monoamines/metabolism , Brain/drug effects , Fluoxetine/pharmacology , Glycyrrhizic Acid/pharmacology , Selective Serotonin Reuptake Inhibitors/pharmacology , Animals , Brain/anatomy & histology , Chromatography, High Pressure Liquid/methods , Drug Combinations , Male , Maze Learning/drug effects , Rats , Rats, WistarABSTRACT
Effects of serotonin uptake inhibitor fluoxetine (F) and it's complexes with glycyrrizhinic acid (GA) in molar proportions 1GA : 1F (FGA-1) and 4GA : 1F (FGA-4) on rat behavior in elevated plus-maze and brain monoamine concentrations were studied. Drugs (25 mg/kg) were administered per os 1 h before investigations. F-treated rats showed increased anxiety and reduced locomotor activity, whereas FGA-1 and FGA-4 had no effects on the behaviors. None of the compounds modified brain tissue serotonin content, but all of them decreased the level of its metabolite 5-hydroxyindole-3-acetic acid level in the hypothalamus, and FGA-4 also decreased it in the cortex. Noradrenaline levels were increased in the hypothalamus of rats treated with F in both combinations with GA. In the striatum, F increased dopamine and its metabolite DOPAC levels, but their ratio (an indicator of the neurotransmitter turnover) was not altered by this drug. Unlike F, FGA-1 significantly activated dopamine turnover in the striatum. The data obtained suggested that application of F in complexes with GA significantly modified the drug behavioral effects and these alterations may be related to specific effects of the pure compound and its complexes on the functions of the brain monoaminergic systems that regulate investigated behavior.
Subject(s)
Anti-Infective Agents/pharmacology , Behavior, Animal/drug effects , Biogenic Monoamines/metabolism , Brain/drug effects , Fluoxetine/pharmacology , Glycyrrhizic Acid/pharmacology , Selective Serotonin Reuptake Inhibitors/pharmacology , Animals , Anti-Infective Agents/administration & dosage , Dopamine/metabolism , Fluoxetine/administration & dosage , Glycyrrhizic Acid/administration & dosage , Hydroxyindoleacetic Acid/metabolism , Locomotion/drug effects , Male , Maze Learning/drug effects , Norepinephrine/metabolism , Rats , Rats, Wistar , Serotonin/metabolism , Selective Serotonin Reuptake Inhibitors/administration & dosageABSTRACT
As shown by investigations of alkaline phosphatase, plasma levels of calcium, non-organic phosphorus, coefficient Ca/P in 58 patients with osteoarthrosis deformans before and after radon baths, mud applications or their combination, the highest biochemical effect was achieved in a group of patients on mud therapy.
