Effects of khellin and timefurone on secretion and catabolism of lipoproteins by cultured rabbit and human hepatocytes
| Autor: | Vadim S. Repin, Alexander V. Victorov, Sergey A. Volgushev, Vladimir N. Smirnov, Eugeniy A. Podres, V. A. Kosykh, Dmitriy K. Novikov |
|---|---|
| Rok vydání: | 1989 |
| Předmět: |
medicine.medical_specialty
Very low-density lipoprotein Khellin Apolipoprotein B Catabolism Cholesterol Pharmaceutical Science Biology chemistry.chemical_compound Endocrinology medicine.anatomical_structure chemistry Internal medicine Hepatocyte medicine biology.protein lipids (amino acids peptides and proteins) Secretion Lipoprotein |
| Zdroj: | International Journal of Pharmaceutics. 57:223-227 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/0378-5173(89)90211-1 |
| Popis: | The effects of timefurone and khellin on lipoprotein metabolism in cultured rabbit and human hepatocytes were characterized by the following parameters: (1) the uptake and degradation of 125 I-LDL; (2) secretion of total apolipoprotein B (apo-B) as measured by enzyme-linked immunosorbent assay (ELISA); (3) VLDL [ 35 S]methionine labeled apo-B and apo-E secretion; and (4) cholesterol (CH) synthesis and CH secretion in VLDL. Timefurone and khellin at therapeutic (10 μg/ml) concentration did not alter 125 I-LDL uptake and degradation, whereas both agents reduced the VLDL secretion and total release of apo-B; secretion of apo-E in VLDL remaining unchanged. A marked inhibition (by 30–50%) of CH synthesis was observed for both drugs. These results suggest that khellin and timefurone can exert their hypolipidemic action by a simultaneous decrease of hepatic CH synthesis and secretion of apo-B containing VLDL particles. |
| Databáze: | OpenAIRE |
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