Reed M J, Beranek P A, Bonney R C, Ghilchik M W, James V H
Department of Chemical Pathology, St. Mary's Hospital Medical School, London, U.K.
Anticancer Res. 1987 Nov-Dec;7(6):1265-9.
The uptake and metabolism of 3H-oestradiol by breast tumour tissue was studied in three postmenopausal women before, after 1 week of treatment with ethynyl-oestradiol (EE, 10 micrograms/day) and again two weeks later after treatment with medroxyprogesterone acetate (MPA, 500mg/day, i.m.). Treatment with EE reduced the tissue: plasma gradients for both 3H-oestradiol and 3H-oestrone and little further change in these ratios occurred after MPA treatment. The proportion of oestrogen present as 3H-oestrone increased in tumours from 2/3 women after treatment with MPA but not EE, although no increase in the activity of oestradiol 17 beta-hydroxysteroid dehydrogenase (E2DH) was detected. Plasma and tissue concentrations of 5-androstenediol, dehydroepiandrosterone and dehydroepiandrosterone sulphate were all reduced after MPA treatment. The results from this study show that treatment with EE and MPA can reduce the uptake of oestradiol by breast tumours. No increase in E2DH activity was detected but it is possible that MPA influences other enzymes involved in oestradiol metabolism.
在三名绝经后女性中,研究了乳腺肿瘤组织对³H-雌二醇的摄取和代谢情况。在服用乙炔雌二醇(EE,10微克/天)治疗1周前、治疗1周后以及随后用醋酸甲羟孕酮(MPA,500毫克/天,肌肉注射)治疗两周后再次进行研究。EE治疗降低了³H-雌二醇和³H-雌酮的组织:血浆梯度,MPA治疗后这些比率几乎没有进一步变化。MPA治疗后,2/3女性肿瘤中以³H-雌酮形式存在的雌激素比例增加,但EE治疗后未增加,尽管未检测到雌二醇17β-羟基类固醇脱氢酶(E2DH)活性增加。MPA治疗后,血浆和组织中5-雄烯二醇、脱氢表雄酮和硫酸脱氢表雄酮的浓度均降低。本研究结果表明,EE和MPA治疗可降低乳腺肿瘤对雌二醇的摄取。未检测到E2DH活性增加,但MPA可能影响参与雌二醇代谢的其他酶。