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

Journal of steroid biochemistry Pub Date : 1990-08-28 DOI:10.1016/0022-4731(90)90167-Q

Takara Yamamoto , Masaaki Fukuoka , Yasuko Fujimoto , Jo Kitawaki , Masamichi Nakakoshi , Makoto Yoshihama , Hiroji Okada

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引用次数: 20

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.

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新型雄烯二酮衍生物14α-羟基-4-雄烯-3,6,17-三酮(14α-OHAT)对人子宫肿瘤芳香酶活性的抑制作用

人子宫雌激素依赖性肿瘤的发生被认为与雌激素的生物合成密切相关。本研究考察微生物合成的新型4-雄烯-3,6,17-二酮衍生物14α-羟基-4-雄烯-3,6,17-三酮(14α-OHAT)是否抑制人子宫肿瘤(即子宫内膜癌、子宫平滑肌瘤和子宫腺肌病组织)雌激素生物合成酶(芳香酶)活性。14α-OHAT对所有子宫肿瘤的芳香酶活性均呈剂量依赖性(0.1 ~ 10 μM)。此外，14α-OHAT与兔子宫细胞溶胶性类固醇没有结合亲和力，在人胎盘制剂中也不会转化为雌激素。因此，14α-OHAT，一种芳香化酶抑制剂，可能在临床上用于绝经期或绝经后子宫雌激素依赖性肿瘤的内分泌化疗。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Journal of steroid biochemistry

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