己烯雌酚 -3,4-氧化物的肿瘤抑制作用。
The tumor-inhibiting effect of diethylstilbestrol-3,4-oxide.
作者信息
Schneider M R, Kranzfelder G, von Angerer E, Schönenberger H, Metzler M, Michel R T, Fortmeyer H P, Ruckdeschel G
出版信息
J Cancer Res Clin Oncol. 1981;100(3):247-54. doi: 10.1007/BF00410685.
Diethylstilbestrol-3,4-oxide, (DES-3,4-oxide), one of the possible cancerogenic metabolites of the well-known estrogen diethylstilbestrol (DES), is a potential estrophilic cytostatic compound. It shows a very good affinity to the estrogen receptor. The uterotrophic activity determined in the mouse uterine weight bioassay is nearly identical with that of DES. Potential alkylating properties could neither be detected in the p-NBP test not in the prophage induction test. DES-3,4-oxide [0.01-1.0 mg/kg body weight (b. wt.)] markedly inhibited the growth of the DMBA-induced hormone-dependent mammary carcinoma of the SD rat, as well as the growth of a hormone-dependent postmenopausal (but not of a premenopausal) human mammary carcinoma serially transplanted in nude mice. However, DES-3,4-oxide had no significantly better effect on the DMBA-induced mammary carcinoma of the SD rat than DES.
己烯雌酚 - 3,4 - 氧化物（DES - 3,4 - 氧化物）是著名雌激素己烯雌酚（DES）可能的致癌代谢产物之一，是一种潜在的亲雌激素性细胞生长抑制剂。它对雌激素受体表现出非常好的亲和力。在小鼠子宫重量生物测定中确定的子宫营养活性与DES几乎相同。在对硝基苯磷酸酯（p - NBP）试验和噬菌体诱导试验中均未检测到潜在的烷基化特性。DES - 3,4 - 氧化物[0.01 - 1.0毫克/千克体重（b.wt.）]显著抑制了二甲基苯并蒽（DMBA）诱导的SD大鼠激素依赖性乳腺癌的生长，以及在裸鼠中连续移植的激素依赖性绝经后（但不是绝经前）人乳腺癌的生长。然而，DES - 3,4 - 氧化物对SD大鼠DMBA诱导的乳腺癌的影响并不比DES显著更好。
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