RESUMEN
New amino acid derivatives of glycyrrhizic acid and its methyl ester were selectively synthesized using active N-succinimide esters. The compounds with residues of glycine ethyl ester and alanine methyl and butyl esters increased the level of agglutinins and hemolysins in blood serum of mice two- to threefold in comparison with the control upon parenteral administration at a dose of 2 mg/kg for 14 days. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 2; see also http://www.maik.ru.
Asunto(s)
Adyuvantes Inmunológicos/síntesis química , Adyuvantes Inmunológicos/farmacología , Glicopéptidos/química , Ácido Glicirrínico/síntesis química , Ácido Glicirrínico/farmacología , Adyuvantes Inmunológicos/química , Animales , Éteres/química , Ácido Glicirrínico/química , RatonesRESUMEN
New cysteine-containing derivatives of glycyrrhizic acid were synthesized by its coupling with Cys(Bzl) esters or the Cys(Bzl)-Val-OBu(t) dipeptide by the active ester method (DCC/HOSu) or by Woodward's reagent K. The derivatives with Cys(Bzl) and Cys(Bzl)-Val residues attached to the carbohydrate part of the molecule stimulated the primary immune response and the reaction of delayed-type hypersensitivity in mice at a dose of 2 mg/kg. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 1; see also http://www.maik.ru.
Asunto(s)
Adyuvantes Inmunológicos/síntesis química , Cisteína/química , Glicopéptidos/síntesis química , Ácido Glicirrínico/química , Adyuvantes Inmunológicos/química , Adyuvantes Inmunológicos/farmacología , Glicopéptidos/química , Glicopéptidos/farmacología , Resonancia Magnética Nuclear BiomolecularRESUMEN
A phytopreparation from lucerne (Medicago sativa) was studied with respect to the acute and chronic toxicity and the action upon the cellular genetic mechanism. It was found that the preparation belongs to the group of practically nontoxic properties.
Asunto(s)
Medicago sativa/toxicidad , Animales , Células Cultivadas , Perros , Relación Dosis-Respuesta a Droga , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Ratones , Pruebas de Mutagenicidad/estadística & datos numéricos , Pomadas , Extractos Vegetales/toxicidad , Conejos , Ratas , Pruebas Cutáneas/estadística & datos numéricos , Soluciones , Comprimidos , Teratógenos/toxicidad , Factores de TiempoRESUMEN
The specific activity of new drug forms (tablets, suppositories, ointments) of dubinal was studies on models of ischemic damage to the heart, toxic hepatitis, aseptic inflammation, damage to the skin and mucosa of the large intestine. It was found that the drug forms under study possessed a cardioprotective, hepatoprotective, anti-inflammatory, and wound-healing effect. This may serve as a prerequisite to their further clinical study.
Asunto(s)
Antioxidantes/administración & dosificación , Hidroxitolueno Butilado/administración & dosificación , Animales , Asepsia , Intoxicación por Tetracloruro de Carbono/complicaciones , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Enfermedades Intestinales/tratamiento farmacológico , Ratones , Infarto del Miocardio/tratamiento farmacológico , Infarto del Miocardio/etiología , Miocarditis/inducido químicamente , Miocarditis/tratamiento farmacológico , Pomadas , Ratas , Supositorios , Comprimidos , Factores de Tiempo , Úlcera/tratamiento farmacológicoRESUMEN
The effect of eracond on some parameters of immunity and allergic reactions was studied in experiments on mice and guinea pigs. The drug was found to possess an immunomodulating effect.
Asunto(s)
Adyuvantes Inmunológicos/farmacología , Medicago sativa/química , Animales , Formación de Anticuerpos/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Cobayas , Inmunidad Celular/efectos de los fármacos , Inmunización , Masculino , Ratones , Ratones Endogámicos CBA , Anafilaxis Cutánea Pasiva/efectos de los fármacos , Extractos Vegetales/farmacologíaRESUMEN
Triterpene 2,6-dideoxy-alpha-L-arabino-hexopyranosides were synthesized by the glycosylation of oleanane triterpene alcohols with L-rhamnal acetate in the presence of cationite KU-2-8 and lithium bromide. 2,6-Dideoxy-alpha-L-arabino-hexopyranosides of allobetulin and methyl glycyrrhetinate showed pronounced antiulcerous activity; the latter also stimulated reparative skin regeneration in rats and was effective as a hepatoprotectant.
Asunto(s)
Antiulcerosos/síntesis química , Glicósidos/síntesis química , Ramnosa/análogos & derivados , Triterpenos/síntesis química , Animales , Antiulcerosos/farmacología , Bromuros , Tetracloruro de Carbono , Resinas de Intercambio Iónico , Compuestos de Litio , Hígado/efectos de los fármacos , Ratas , Piel/efectos de los fármacos , Triterpenos/farmacologíaRESUMEN
The experiments on rats with toxic hepatic damage induced by tetrachloromethane have shown that the derivatives of glycyrrhizinic acid (5NGA) promote a decrease in the rate of lipid peroxide oxygenation in the hepatic tissue homogenate and the blood serum, in the inhibition of organospecific enzyme activity (BHMT, ALT, AST) and increase in choleresis. The data obtained testify to the hepatoprotective activity of the derivatives of glycyrrhizinic acid.
Asunto(s)
Colagogos y Coleréticos/uso terapéutico , Ácido Glicirretínico/análogos & derivados , Hígado/efectos de los fármacos , Animales , Intoxicación por Tetracloruro de Carbono/complicaciones , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Evaluación Preclínica de Medicamentos , Flavonoides/uso terapéutico , Ácido Glicirretínico/uso terapéutico , Ácido Glicirrínico , Ratones , Extractos Vegetales/uso terapéutico , Prednisolona/uso terapéutico , Ratas , Ratas Wistar , Silimarina/uso terapéutico , Factores de TiempoRESUMEN
The authors studied the effect of inflammation mediators--serotonin, histamine, bradykinin, as well as that of trypsin on lipid peroxidation (LPO). It was demonstrated by chemiluminescence of native hepatic mitochondria in vitro and blood serum in vivo and tests for diene conjugates and malonic dialdehyde that inflammation mediators (histamine, serotonin, bradykinin) and the proteolytic enzyme trypsin activate LPO processes, which correlates with the antiinflammatory effect of these biologically active substances.
Asunto(s)
Bradiquinina/farmacología , Histamina/farmacología , Inflamación/tratamiento farmacológico , Peroxidación de Lípido/efectos de los fármacos , Serotonina/farmacología , Tripsina/farmacología , Animales , Femenino , Técnicas In Vitro , Masculino , Ratas , Ratas WistarRESUMEN
By using the NMR spectroscopy it was shown that hydrogen bond is formed during the interaction between pyrazole molecule and iecithin. The hydrogen bond formation is probably one of the manifestations of the biological activity of pyrazole.
Asunto(s)
Lípidos de la Membrana/química , Fosfolípidos/química , Pirazoles/química , Cromatografía en Capa Delgada , Cristalización , Interacciones Farmacológicas , Técnicas In Vitro , Espectroscopía de Resonancia Magnética , Lípidos de la Membrana/aislamiento & purificación , Fosfolípidos/aislamiento & purificación , Pirazoles/aislamiento & purificación , Relación Estructura-Actividad , TemperaturaRESUMEN
Three triterpene glycopeptides, glycyrrhizic acid monomethly ester derivatives containing peptide fragment of N-acetylmuramoyldipeptide and its analogues, are synthesized. They possess high prednizolone-like antiinflammatory activity and display pronounced stimulative effect on humoral factors of immunity.
Asunto(s)
Adyuvantes Inmunológicos/síntesis química , Antiinflamatorios no Esteroideos/síntesis química , Glicopéptidos/síntesis química , Ácido Glicirretínico/análogos & derivados , Aglutininas/análisis , Animales , Formación de Anticuerpos , Fenómenos Químicos , Química , Glicopéptidos/farmacología , Ácido Glicirrínico , Ratones , Tamaño de los Órganos/efectos de los fármacos , RatasRESUMEN
In experiments on rats with alloxan diabetes efficacy of amidopyrine, acetylsalicylic acid, methyluracil, butadione and brufen in experimental inflammation was shown. The antiinflammatory drugs under study were found to have various effects on insulin and glucose blood levels in intact rats and those with diabetes. The increase in glucose content under the influence of methyluracil is presumably connected with the elevation of somatotrophic hormone blood level. Acetylsalicylic acid and butadione reduce the content of somatotrophic hormone. Methyluracil potentiates antiexudative effects of acetylsalicylic acid and amidopyrine.
Asunto(s)
Antiinflamatorios/uso terapéutico , Diabetes Mellitus Experimental/tratamiento farmacológico , Animales , Glucemia/análisis , Diabetes Mellitus Experimental/sangre , Evaluación Preclínica de Medicamentos , Femenino , Granuloma/sangre , Granuloma/tratamiento farmacológico , Hormona del Crecimiento/sangre , Insulina/sangre , Masculino , Ratas , Factores de TiempoRESUMEN
Antioxidative activity of analginum, amidopyrine, butadion, acetylsalicilic acid, ascorbic and mephenamine acids, indometacin, bruphene, voltarene, delagil, prednisolone and hydrocortisone was studied. The antioxidative activity was estimated by means of inhibition of chemoluminescence in liver mitochondria and blood serum as well as by evaluation of malonic dialdehyde and diene conjugates content. Lipid peroxidation was shown to accelerate in inflammation as shown by accumulation of malonic dialdehyde and diene conjugates. The drugs studied inhibited lipid peroxidation in intact animals and in animals with experimental inflammation.
Asunto(s)
Antiinflamatorios/farmacología , Antioxidantes , Peróxidos Lipídicos/metabolismo , Animales , Inflamación/sangre , Peróxidos Lipídicos/sangre , Hígado/metabolismo , Mediciones Luminiscentes , Malondialdehído/metabolismo , RatasRESUMEN
The action on the reparative stage of inflammation of acetylsalicylic, ascorbic and mephenamic acids, amidopyrine, analgin, butadion, ibuprophen, indomethacin, voltaren, glycyrrhizic acid and its penta-O-nicotinate, delagil, methyluracil, and prednisolone was evaluated from the rate of the healing of skin wounds in mice and rats, formation of the granulation tissue on the integmentary glass implanted into the subcutaneous fat from the effect on the functional status of fibroblast chromatin and changes in phagocytosis. Prednisolone, indomethacin voltaren, delagil, appeared to inhibit whereas amidopyrine, acetylsalicylic acid, butadion, ibuprophen and methyluracil to stimulate the reparative stage of inflammation. The anti-inflammatory agents that stimulated reparative regeneration raised the functional activity of chromatin.
Asunto(s)
Antiinflamatorios/uso terapéutico , Tejido de Granulación/efectos de los fármacos , Inflamación/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacos , Animales , Cromatina/efectos de los fármacos , Ratones , Microscopía Fluorescente , Fagocitosis/efectos de los fármacos , Ratas , Piel/lesiones , Factores de TiempoRESUMEN
The derivatives of glycyrrhizin acid--dihydrazidohydrazose of glycyrrhizin acid (DHGA), DHGA plus benzaldehyde, DHGA plus 5-nitrofurfurol, DHGA plus furfurol, glycyrrhizin acid, methylmethioninsulfonium-glycyrrhizinate, sodium salt of 18-glycyrrhetic acid, and potassium salt of glycyrrhizin acid--show a pronounced anti-inflammatory action, inhibit the development of histamine-, serotonin-, bradykinin-, and formalin-induced edemas, barrier function of an inflammatory focus, lower vascular permeability, the granulemic sac weight and exudate amount. The anti-inflammatory action of the compounds remains unchanged under adrenalectomy. By antiphlogistic activity, the derivatives in question compare very favourably to butadion and hydrocortisone, and are similar to prednisolone.