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1.
Arzneimittelforschung ; 27(9): 1691-4, 1977.
Artículo en Alemán | MEDLINE | ID: mdl-579140

RESUMEN

The effect of silybin dihemisuccinate on the hepatic biosynthesis of cholesterol was studied by measuring the incorporation of [1-14C]-acetate and [2-14C]-mevalonate in the postmitochondrial supernatant of liver homogenates. 2. Under absolute in vitro conditions, silybin dihemisuccinate inhibits the biosynthesis of cholesterol in dependence on its concentration. With [1-14C]-acetate or [2-14C]-mevalonate the concentrations of silybin for 50% inhibition are 0.37 mM or 0.40 mM, resp. 3. 30 min after i.v. injection of 150.6 mg silybin dihemisuccinate/kg with both precursors the biosynthesis of cholesterol studied in vitro is diminished in comparison to controls. 60 min or 24 h after i.v. injection of silybin no effects on in vitro biosynthesis of cholesterol can be observed.


Asunto(s)
Colesterol/biosíntesis , Flavonoides/farmacología , Hígado/efectos de los fármacos , Silimarina/farmacología , Animales , Radioisótopos de Carbono , Técnicas In Vitro , Hígado/metabolismo , Ratas , Silimarina/administración & dosificación
2.
Arzneimittelforschung ; 26(2): 235-8, 1976 Feb.
Artículo en Alemán | MEDLINE | ID: mdl-947204

RESUMEN

60 min after i.v. application of 140.5 mg silymarin-N-methylglucamine salt/kg body weight dissolved in 4% polyvinylpyrrolidone solution, and 30 min after i.p. administration [1-14C]-acetate, compared to rats treated with solvent only, a statistically significant increase of specific radioactivities in total lipids, triglycerides, total phospholipids as well as in the phosphatidylcholine fraction and a decrease of specific activities in the free cholesterol fraction of the liver can be determined. 70 min after i.p. application of 140.5 mg silybin-dihemisuccinate/kg body weight dissolved in phosphate buffer, and 10 min after i.v. administration of [1-14C]-acetate in comparison with rats treated with solvent only, a statistically significant enhancement of specific activities of total liver lipids, free hepatic cholesterol, liver triglycerides, total liver phospholipids, and the hepatic fraction of phosphatidyl ethanolamine can be measured. Silybin also produces an increased specific radioactivity of the serum triglyceride fraction.


Asunto(s)
Acetatos/metabolismo , Flavonoides/farmacología , Lípidos/biosíntesis , Hígado/metabolismo , Silimarina/farmacología , Animales , Colesterol/metabolismo , Inyecciones Intraperitoneales , Inyecciones Intravenosas , Lípidos/análisis , Hígado/efectos de los fármacos , Fosfatidilcolinas/metabolismo , Fosfatidiletanolaminas/metabolismo , Fosfolípidos/metabolismo , Ratas , Silimarina/administración & dosificación , Silimarina/análogos & derivados , Triglicéridos/metabolismo
5.
Arzneimittelforschung ; 26(3): 399-402, 1976.
Artículo en Alemán | MEDLINE | ID: mdl-989335

RESUMEN

After acute intoxication with praseodymium nitrate (10 mg/kg body weight i.v.), time functions of enzyme activities of GOT, GPT, ChE, AP and of free fatty acids concentration in rat serum were analysed and the results subjected to significance and correlation analysis. Time functions of free fatty acids concentration corresponded with those of enzyme activities of GOT and GPT. In the early state of intoxication serum concentrations of palmitoleinic and oleic acid were more increased than those of stearinic acid. There seems to be an alteration in the correlations of analysed measures with regard to their temporal changes parallel to the progress of intoxication.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Praseodimio/envenenamiento , Alanina Transaminasa/sangre , Fosfatasa Alcalina/sangre , Animales , Aspartato Aminotransferasas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Colinesterasas/sangre , Ácidos Grasos no Esterificados/sangre , Masculino , Ácidos Palmíticos/sangre , Ratas , Ácidos Esteáricos/sangre
6.
Res Exp Med (Berl) ; 166(1): 43-52, 1975 Nov 26.
Artículo en Alemán | MEDLINE | ID: mdl-1202588

RESUMEN

After intraperitoneal application of desoxycholate in cells of exocrine pancreas, ultrastructural alterations are observed. Initial changes are seen in mitochondria and focal parts of the endoplasmic reticulum. In later experimental stages there is sizable increase in the extent of the initially focal degradations, in such a way that great areas of the cytoplasm are involved. It is remarkable to note, that there are no indications about any disturbance in the synthesis and excretion of zymogen granules. The described morphological alterations will be discussed as conceivably being caused primarily by an irritation in the lipoid metabolism of the membrane.


Asunto(s)
Ácido Desoxicólico/farmacología , Páncreas/ultraestructura , Pancreatitis/inducido químicamente , Animales , Gránulos Citoplasmáticos/ultraestructura , Retículo Endoplásmico/ultraestructura , Masculino , Membranas/ultraestructura , Mitocondrias/ultraestructura , Pancreatitis/patología , Ratas
8.
Arzneimittelforschung ; 25(10): 1582-5, 1975 Oct.
Artículo en Alemán | MEDLINE | ID: mdl-1243043

RESUMEN

1. 24 h after application of 900 mg D-galactosamine/kg body weight, an increase of total lipids, triglycerides, phosphatidyl-choline and phosphatidic acid concentrations, and also a decrease of total phospholipids and phosphatidylethanolamine can be determined in the whole rat liver. After administration of [1-14C]-palmitate, specific radioactivity of phosphatidyl-choline is diminished without alteration of specific radioactivity of other lipid fractions. Prophylactic application of silybin-dihemisuccinate abolished completely decrease of phosphatidyl-ethanolamine and diminished increase of total lipids and triglyceride concentrations. 2. Specific radioactivity of total lipids in serum of galactosamine-intoxicated rats is enhanced, specific radioactivity of triglycerides and phospholipids is diminished, simultaneously, total lipids concentration is reduced. 3. In the microsomal fraction of galactosamine-injured livers, a decrease of specific radioactivity of total phospholipids and phosphatidyl-choline can be observed. Prophylactic administration of silybin abolishes diminution of specific radioactivity of phosphatidyl-choline partially. 4. Diminution of specific radioactivity of total lipids, total phospholipids and phosphatidyl-ethanolamine, induced by galactosamine intoxication in the mitochondrial fraction, is normalized by application of silybin. 5. Diminished triglyceride infiltration in siybin-treated rats may be based onnormalization of inhibited phosphatidyl-choline turnover.


Asunto(s)
Flavonoides/farmacología , Galactosamina/envenenamiento , Fosfolípidos/metabolismo , Silimarina/farmacología , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas , Hígado/metabolismo , Masculino , Microsomas Hepáticos/metabolismo , Mitocondrias Hepáticas/metabolismo , Ácidos Palmíticos/farmacología , Ácidos Fosfatidicos/metabolismo , Fosfatidilcolinas/metabolismo , Fosfatidiletanolaminas/metabolismo , Ratas , Silimarina/análogos & derivados , Triglicéridos/metabolismo
9.
Arzneimittelforschung ; 25(2): 188-94, 1975 Feb.
Artículo en Alemán | MEDLINE | ID: mdl-1173031

RESUMEN

Single application of 600-750 mug phalloidine/kg body weight produces within 4-6 h a decrease of serum cholesterol esters and a rising concentration of free fatty acids and lysophosphatidyl choline in liver homogenate. Analysis of fatty acids compounds in liver lipid fractions indicates an increase of shorter-chain fatty acids and a percentage diminution of highly unsaturated longer-chain fatty acids. In the prophylactic test, and also when giving silymarine-N-methylglucamine-salt simultaneously with the toxic agent, most analysed parameters show a variance according to those of the nonintoxicated control group. Correlation analysis of paramenters points out typical variations between normal, control and experimental animals.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Flavonoides/farmacología , Hígado/metabolismo , Micotoxinas , Péptidos Cíclicos , Fosfolípidos/metabolismo , Alanina Transaminasa/sangre , Alcoholes/farmacología , Alcoholes/uso terapéutico , Animales , Anticolesterolemiantes/farmacología , Aspartato Aminotransferasas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Colesterol/sangre , Ácidos Grasos no Esterificados/sangre , Flavonoides/uso terapéutico , Glutamato Deshidrogenasa/sangre , Masculino , Fosfolípidos/sangre , Ratas , Triglicéridos/sangre
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