The effect of the aromatase inhibitor, 4-(phenylthio)-4-androstene-3,17-dione, on dimethylbenz(a)anthracene-induced rat mammary tumors

Yusuf J. Abul-Hajj

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

4-(Phenylthio)-4-androstene-3,17-dione (4-PTAD), a known inhibitor of human placental aromatase, was examined as a growth inhibitor of DMBA-induced rat mammary tumors. Subcutaneous administration of 4-PTAD at dose levels of 25 or 50 mg/kg/day caused a significant decrease in hormone-dependent tumor growth. Resumption of tumor growth occurred when either the administration of inhibitor was stopped or when inhibitor was coadministered with estradiol indicating that suppression of tumor growth was due to inhibition of estrogen biosynthesis. Additionally, plasma levels of estradiol were found to be lower in the animals treated with 4-PTAD. The major metabolite of 4-PTAD in vitro was identified as 4-(phenylthio)-4-androstene-17β-ol-3-one and was found to have 60% of the aromatase inhibitory activity of 4-PTAD.

Original languageEnglish (US)
Pages (from-to)439-442
Number of pages4
JournalJournal of Steroid Biochemistry
Volume34
Issue number1-6
DOIs
StatePublished - 1989

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