Inhibitory effect of a new androstenedione derivative, 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT) on aromatase activity of human uterine tumors

Yamamoto T, T. Yamamoto, Takara Yamamoto, Masaaki Fukuoka, Fukuoka M, M Fukuoka, Fujimoto Y, Yasuko Fujimoto, Y Fujimoto, Kitawaki Jo, Kitawaki J, J. Kitawaki, Masamichi Nakakoshi, Nakakoshi M, M Nakakoshi, M Yoshihama, Yoshihama M, Makoto Yoshihama, Okada H, H Okada, Hiroji Okada
Journal of steroid biochemistry · 1990 · vol. 36(6) , pp. 517–521 · doi:10.1016/0022-4731(90)90167-q · PMID:2214767 · W2051905313
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Abstract

The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14 alpha-hydroxy-4-androstene-3,6,17-trione (14 alpha-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). 14 alpha-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1-10 microM). Moreover, 14 alpha-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. Thus, 14 alpha-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.

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MeSH descriptors

Androstenols Aromatase Inhibitors Uterine Neoplasms Adult Androstenols Animals Aromatase Aromatase Dose-Response Relationship, Drug Female Humans Middle Aged Placenta Placenta Rabbits Uterine Neoplasms

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