Article: Aromatase inhibition by R 83 842, the dextro isomer of R 76 713, in JEG-3 choriocarcinoma grown in ovariectomized nude mice.
The Journal of steroid biochemistry and molecular biology
1992 Volume 41, Issue 3-8, Page(s) 761–764
Abstract: The effects of repeated (5 days) dosing with the non-steroidal aromatase inhibitor R 83 842 ... the dextro isomer of R 76 713) on tumor aromatase and uterus weight in ovariectomized nude mice bearing JEG-3 ... Oral administration of R 76 713 (10 mg/kg) for 5 days reduced the increase in uterus weight by 84% in tumor bearing ...
Abstract | The effects of repeated (5 days) dosing with the non-steroidal aromatase inhibitor R 83 842 (the dextro isomer of R 76 713) on tumor aromatase and uterus weight in ovariectomized nude mice bearing JEG-3 tumors were examined. In animals bearing an androstenedione implant the presence of a JEG-3 tumor significantly increased uterus weight, proving that tumor aromatase indeed converted androgens to estrogens. Oral administration of R 76 713 (10 mg/kg) for 5 days reduced the increase in uterus weight by 84% in tumor bearing mice revealing true in vivo aromatase inhibition by R 76 713. Experiments performed in the absence of exogenously added androgens gave similar results. Uterus weights in tumor bearing mice were significantly higher than in control mice. Oral administration of R 83 842 (5 mg/kg) for 5 days reduced uterus weight in the tumor bearing animals. Ex vivo aromatase measurements performed in JEG-3 tumors from these animals showed an aromatase inhibition of 93.9% in treated mice as compared to untreated mice. Five days oral treatment with R 83 842 dose-dependently lowered both aromatase activity and uterus weight. Doses of 5 and 0.5 mg/kg inhibited tumor aromatase by 94.1 and 74.7%, respectively, and reduced uterus weight. After a dose of 0.05 mg/kg aromatase activity and uterus weight were similar to those in the control group. |
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MeSH term(s) | Animals ; Aromatase Inhibitors ; Cell Line ; Choriocarcinoma/enzymology ; Female ; Humans ; Isomerism ; Mice ; Mice, Nude ; Neoplasm Transplantation ; Pregnancy ; Transplantation, Heterologous ; Triazoles/pharmacology ; Tumor Cells, Cultured ; Uterine Neoplasms/enzymology |
Chemical Substances | Aromatase Inhibitors ; Triazoles ; vorozole (1E2S9YXV2A) |
Language | English |
Publishing date | 1992-03 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 1049188-0 |
ISSN | 1879-1220 ; 0960-0760 |
ISSN (online) | 1879-1220 |
ISSN | 0960-0760 |
DOI | 10.1016/0960-0760(92)90419-j |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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