低剂量氨鲁米特对绝经后乳腺癌患者外周芳香化作用的有效抑制
Effective inhibition by low dose aminoglutethimide of peripheral aromatization in postmenopausal breast cancer patients.
作者信息
Dowsett M, Santner S J, Santen R J, Jeffcoate S L, Smith I E
出版信息
Br J Cancer. 1985 Jul;52(1):31-5. doi: 10.1038/bjc.1985.144.
Abstract
Aminoglutethimide without glucocorticoid has been shown to be a clinically effective treatment for postmenopausal breast cancer in low dosage (250 mg day-1). The mechanism of action of this approach is thought to be the inhibition of peripheral aromatase, the enzyme which converts androstenedione to oestrone. The activity of this enzyme was measured in vivo by injection with 3H-androstenedione and 14C-oestrone and found to be 0.20% +/- 0.05 in 5 patients on low dose AG therapy. In comparison with previously published data this demonstrates a 92% inhibition of peripheral aromatase activity confirming aromatase inhibition as a viable aim in the endocrine treatment of breast cancer.
摘要
已证明，无糖皮质激素的氨鲁米特在低剂量（每日250毫克）时是绝经后乳腺癌的一种临床有效治疗方法。这种治疗方法的作用机制被认为是抑制外周芳香化酶，即一种将雄烯二酮转化为雌酮的酶。通过注射3H-雄烯二酮和14C-雌酮在体内测量该酶的活性，发现在接受低剂量氨鲁米特治疗的5名患者中，该酶活性为0.20%±0.05。与先前发表的数据相比，这表明外周芳香化酶活性受到92%的抑制，证实芳香化酶抑制是乳腺癌内分泌治疗的一个可行目标。
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