| Autor: |
N, Van-Bac, C, Moisand, A, Gouyette, G, Muzard, N, Dat-Xuong, J B, Le Pecq, C, Paoletti |
| Rok vydání: |
1980 |
| Předmět: |
|
| Zdroj: |
Cancer treatment reports. 64(8-9) |
| ISSN: |
0361-5960 |
| Popis: |
Radiolabeled 9-hydroxyellipticine (iv and ip routes) and the corresponding radioactive quaternary salt, 2-methyl-9-hydroxyellipticinium acetate (iv route), were administered to mice. Tissue distribution was then followed up to 64 hours by means of autoradiography. Both drugs accumulated in the kidneys, lungs, and liver; 9-hydroxyellipticine also accumulated in the spleen and bone marrow. The quaternary salt was concentrated in the gastrointestinal walls and the salivary and thyroid glands; none was found in the brain. Metabolic studies after administration of these antitumor drugs to rats and mice showed that 9-hydroxyellipticine is extensively metabolized, mainly to its glucuronide. Under our experimental conditions, the ellipticinium derivative was excreted unchanged in the bile (70%) and in the urine (30%). Pharmacokinetic studies in mice using either radioactivity measurements or selective extraction followed by spectrofluorometric quantitation have shown that blood levels drop very rapidly during the distribution phase followed by a much slower disposition phase, with a half-life of about 30 hours for the quaternary salt. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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