Y. Takara, Fukuoka Masaaki, Fujimoto Yasuko
Aug 28, 1990
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Journal
Journal of Steroid Biochemistry
Abstract
Abstract The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT), a new 4-androstene-3,17-dione derivative synthesized microbiologically, inhibits estrogen biosynthetase (aromatase) activities of human uterine tumors (i.e. uterine endometrial cancer, uterine leiomyoma and uterine adenomyosis tissues). 14α-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1–10 μM). Moreover, 14α-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. p]Thus, 14α-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.