RESUMEN
Methods of fluorescent probing, spectrophotometry and microcalorimetry were applied to investigate the alterations in biophysical parameters of erythrocytes membranes, and specifically microviscosity, surface charge, molecular organization of lipid bilayer and lipid-protein interactions under conditions of acute pain syndrome produced by experimental chemical lesion. The distinctive features of non-opiod analgesics interactions and binding to the erythrocytes membranes of rats subjected to acute nociceptive pain accompanied with oxidative stress development were investigated. The abilities of analgesics under research, and namely paracetamol, aspirin, phenazone, ketorolac, pyrodazole, ketoprofenum, natrium mefenaminate, indometacin, nimesulide to make up physico-chemical complexes with lipoperoxidation modified erythrocytes surface and protein-lipid bilayer showed marked changes. The significance of oxidative damage of biophase under conditions of acute pain syndrome for analgesics effective pharmacodynamics and pharmacokinetics realization is under consideration.
Asunto(s)
Dolor Agudo/prevención & control , Analgésicos no Narcóticos/metabolismo , Membrana Eritrocítica/metabolismo , Membrana Dobles de Lípidos/metabolismo , Acetaminofén/metabolismo , Acetaminofén/farmacología , Analgésicos no Narcóticos/farmacología , Animales , Antipirina/metabolismo , Antipirina/farmacología , Aspirina/metabolismo , Aspirina/farmacología , Calorimetría , Fraccionamiento Celular , Membrana Eritrocítica/química , Colorantes Fluorescentes , Indometacina/metabolismo , Indometacina/farmacología , Cetoprofeno/metabolismo , Cetoprofeno/farmacología , Ketorolaco/metabolismo , Ketorolaco/farmacología , Membrana Dobles de Lípidos/química , Peroxidación de Lípido/efectos de los fármacos , Masculino , Orfenadrina/metabolismo , Orfenadrina/farmacología , Dimensión del Dolor , Ratas , Espectrometría de Fluorescencia , Sulfonamidas/metabolismo , Sulfonamidas/farmacologíaRESUMEN
Under modelling of brain ischemia in rats the antioxidant and cerebroprotective action of new N-,S-chinazolone derivative--compound NC-224 has been established. The compensation of pathobiochemical abnormalities in the system "LPO-antioxidant protection" is observed, indicators of carbohydrate metabolism and energy-supply, and morpho-functional status of brain cells are improved under administration of the compound NC-224. Administration of the compound NC-224 to rats promoted a decrease of the lethality index and signs of neurological deficiency.
Asunto(s)
Antioxidantes/farmacología , Isquemia Encefálica/tratamiento farmacológico , Encéfalo/efectos de los fármacos , Neuroglía/efectos de los fármacos , Neuronas/efectos de los fármacos , Fármacos Neuroprotectores/farmacología , Quinazolinas/farmacología , Animales , Antioxidantes/uso terapéutico , Encéfalo/metabolismo , Encéfalo/patología , Isquemia Encefálica/metabolismo , Isquemia Encefálica/mortalidad , Isquemia Encefálica/patología , Catalasa/metabolismo , Modelos Animales de Enfermedad , Metabolismo Energético/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Masculino , Neuroglía/metabolismo , Neuroglía/patología , Neuronas/metabolismo , Neuronas/patología , Fármacos Neuroprotectores/uso terapéutico , Óxido Nítrico Sintasa/metabolismo , Estrés Oxidativo/efectos de los fármacos , Piracetam/farmacología , Piracetam/uso terapéutico , Quinazolinas/uso terapéutico , Ratas , Ratas Wistar , ATPasa Intercambiadora de Sodio-Potasio/metabolismo , Superóxido Dismutasa/metabolismo , Tasa de SupervivenciaRESUMEN
Energy and structural parameters of monochromanes and trimethylphenols derivatives have been chracterized through the employment of semiempirical methods of quantum chemistry. The correlation has been proved between antiradical, hepatoprotective properties of these compounds and energy and structural of their molecules that confirms the presence of relation between structure activity and electron-donor properties of the investigated monochromanes and trimethylphenols.
Asunto(s)
Antioxidantes/farmacología , Cromanos/farmacología , Hígado/efectos de los fármacos , Modelos Químicos , Fenoles/farmacología , Teoría Cuántica , Animales , Antioxidantes/química , Fenómenos Químicos , Cromanos/química , Transporte de Electrón , Retículo Endoplásmico/efectos de los fármacos , Retículo Endoplásmico/metabolismo , Membranas Intracelulares/efectos de los fármacos , Membranas Intracelulares/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Hígado/metabolismo , Fenoles/química , Ratas , Relación Estructura-ActividadRESUMEN
Using some biochemical and physico-chemical methods of investigation, antioxidant activity and membrane protective effect of derivatives of monochromanes and trimethylphenols has been studied most active inhibitors of lipoperoxidation and the compounds capacity to structural modification of properties of the surface and hydrophobic zones of phospholipids bilayer in membranes of endoplasmic reticulum of the liver cells of rats have been determined.
Asunto(s)
Antioxidantes/farmacología , Cromanos/farmacología , Retículo Endoplásmico/efectos de los fármacos , Membranas Intracelulares/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Fenoles/farmacología , Animales , Antioxidantes/química , Cromanos/química , Retículo Endoplásmico/metabolismo , Técnicas In Vitro , Membranas Intracelulares/metabolismo , Hígado/citología , Hígado/efectos de los fármacos , Masculino , Estructura Molecular , Fenoles/química , Fosfolípidos/metabolismo , Ratas , Relación Estructura-ActividadRESUMEN
Antioxidant activity of nine [1,2,4]-triazinone derivatives was studied in the work. Our data show that [1,2,4]-triazinone derivatives with benzyl alcohol, propyl alcohol, me-thyl alcohol and tolyl residues in their structure have antioxidant activity in condition of in vitro NO formation. KO-17 compound proved to have the greatest antioxidant activity which exceeded N-acetyl cysteine's one.
Asunto(s)
Antioxidantes/farmacología , Encéfalo/efectos de los fármacos , Óxido Nítrico/química , Estrés Oxidativo/efectos de los fármacos , Triazinas/farmacología , Animales , Antioxidantes/química , Encéfalo/enzimología , Encéfalo/metabolismo , Técnicas In Vitro , Masculino , Modelos Químicos , Estructura Molecular , Donantes de Óxido Nítrico/química , Ratas , Ratas Wistar , Relación Estructura-Actividad , Superóxido Dismutasa/metabolismo , Triazinas/químicaRESUMEN
It was established that acute poisoning of rats by 1,2-dichloroethane induced considerable changes in lipid peroxidation indices, glutathione content and activity of antioxidant enzymes--superoxidase, catalase, glutathione peroxidase in the brain tissue, erythrocytes and blood plasma. It was shown that nicotinamide in the dose of 200 mg/kg prevented considerable degree of the intoxication caused by 1,2-dichloroethane as well as activation of lipid peroxidation and inhibition of antioxidant defens enzyme activities in tissue of experimental animals.
Asunto(s)
Encéfalo/efectos de los fármacos , Eritrocitos/efectos de los fármacos , Dicloruros de Etileno/envenenamiento , Niacinamida/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Complejo Vitamínico B/uso terapéutico , Animales , Proteínas Sanguíneas/metabolismo , Encéfalo/metabolismo , Eritrocitos/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Masculino , Niacinamida/farmacología , Intoxicación/sangre , Intoxicación/metabolismo , Intoxicación/prevención & control , Ratas , Ratas Wistar , Complejo Vitamínico B/farmacologíaRESUMEN
The effect of cadmium chloride on the fatty acid composition of lipids of the erythrocytes and blood plasma has been studied. It has been established that in the process of cadmium intoxication the decrease of the level of unsaturated fatty acids takes place and the most considerable changes in the content of oleic and arachidonic acids. It makes possible to assume the disturbance of both the erythrocytes membrane structure and metabolism in the erythrocyte. Unitiol injection promotes the normalisation of the indices under investigation.
Asunto(s)
Intoxicación por Cadmio/sangre , Quelantes/uso terapéutico , Membrana Eritrocítica/efectos de los fármacos , Ácidos Grasos/sangre , Unitiol/uso terapéutico , Animales , Cloruro de Cadmio/toxicidad , Intoxicación por Cadmio/tratamiento farmacológico , Modelos Animales de Enfermedad , Membrana Eritrocítica/metabolismo , Ácidos Grasos/química , Ácidos Grasos/metabolismo , Masculino , RatasRESUMEN
In this work the most important stages of the scientific-pedagogic school of biologic and medical chemistry formation in Bogomolets National Medical University starting from the period of foundation as early as in 1863 till nowadays the Chair of Medical Chemistry and Physics as a part of Medical Faculty of Saint Volodymyr Emperor University in the city of Kyiv have been estimated and generalized. The especial attention is attracted to the fact, that it was Kyiv University where firstly the Chair of Biochemistry was created in order of stuyding the regularities of biochemical processes running in the human organism and metabolism disturbances inducing the pathologic processes at some diseases. The scientific and scientific-pedagogical trends of the chair work in different periods of its development are presented, simltneously the leading role of famous Ukrainian scientists--biochemicians in foundation and development of biologic and medical chemistry scientific school in the University are emphasized. Nowadays the Chair is the educational and scientific center supporting and developing the best traditions on training the specialists of different qualification levels: physicians Masters of Science, Philosophy Doctors and Doctors of Science in Medicine and Biology. The Chair is considered to be a basic one among the Ukraine higher medic and pharmaceutic educational institutions having the III-IV accreditation rate on the problems of teaching-organizational, educational-methodical and scientific work. On the Chair base there is functioning the Scientific Problem-Solving Commission of Ministry of health Protections of Academy of Medical Sciences of Ukraine "Biological and medical Chemistry" (the chairman is the Corresponding-Member of Academy of Medical Sciences of Ukraine, Prof. Yu.I. Gubsky. The Chair personnel compiled and issued the contemporary manuals in Ukraine language on Biologic and Bioorganic Chemistry.
Asunto(s)
Bioquímica/historia , Educación Médica Continua/historia , Facultades de Medicina/historia , Historia del Siglo XIX , Historia del Siglo XX , UcraniaRESUMEN
Cadmium intoxication has been defined to make material changes in hemoglobin system by elevation of sulfhemoglobin and methhemoglobin levels on the back-cloth of lowering of general hemoglobin. Alongside with the latter there is observed a violation of antioxydation protection including the activity of erythrocytic catalase, ceruloplasmin, ferrum saturation of transferrine.
Asunto(s)
Antioxidantes/metabolismo , Intoxicación por Cadmio/sangre , Eritrocitos/metabolismo , Hemoglobinas/análisis , Animales , Catalasa/metabolismo , Ceruloplasmina/metabolismo , Eritrocitos/efectos de los fármacos , Eritrocitos/enzimología , Metahemoglobina/metabolismo , Ratas , Sulfahemoglobina/metabolismo , Transferrina/metabolismoRESUMEN
The biochemical mechanisms of genomoprotective action of the new derivatives of pyridinecarbonic acids--PV-3, PV-4 and PV-6 in the conditions of tetrachloromethane chemical cell damage have been studied. This effect is related to their antioxidant influence on LPO processes in transcriptionally active and repressed chromatin fractions of rat liver cells and partial restoration of these fractions structure which has been destroyed during intoxication. PV-4 possesses the most genoprotective activity among the substances studied.
Asunto(s)
Antimutagênicos/farmacología , Tetracloruro de Carbono/farmacología , Ácido Carbónico/farmacología , Genoma , Hígado/efectos de los fármacos , Animales , Ácido Carbónico/química , Masculino , Piridinas/química , Ratas , Ratas WistarRESUMEN
Embikhin causes activation of LPO processes in endoplasmic reticulum and in nuclear chromatine fractions of rat liver cells. The latter is accompanied by the impairment of repressive and active nuclear chromatine fractions structure. Derivate of vitamin E in these conditions renders correcting action on parameters of lipid peroxidation in the investigated subcellular structures, testifying its positive influence on the cell heredity apparatus state. The normalizing action of tocopherol derivative on cytochromes P450 and b5 levels is shown.