Houjou T, Wada T, Yasutomi M
First Department of Surgery, Kinki University School of Medicine, Osaka, Japan.
Clin Ther. 1993 Jan-Feb;15(1):137-47.
The antitumor and endocrine effects of a new nonsteroidal aromatase inhibitor were studied using DMBA-induced rat mammary carcinomas. CGS 16949A (CGS) was administered orally once daily for 3 weeks. A marked antitumor effect was noted at doses of more than 1 mg/kg, and weight gain was dose dependent. Histologic examination showed atrophic changes of the tumors and decreased expression of estrogen receptor levels. To investigate the mechanism of the antitumor effect of CGS, we studied the changes in endocrine function in rats given this agent. In the groups receiving more than 1 mg/kg of CGS, the serum estradiol and prolactin levels were lower and the serum luteinizing hormone level was higher than in the control group. In rats treated with CGS, ovary weight was increased, while uterus and pituitary weights were decreased. These changes were dose dependent. In contrast, the serum corticosterone level and adrenal weight remained unchanged. We conclude that CGS inhibits the growth of hormone-dependent tumors by changing the hormonal environment.
使用二甲基苯并蒽（DMBA）诱导的大鼠乳腺癌研究了一种新型非甾体芳香化酶抑制剂的抗肿瘤和内分泌作用。CGS 16949A（CGS）每日口服一次，持续3周。在剂量超过1mg/kg时观察到明显的抗肿瘤作用，且体重增加呈剂量依赖性。组织学检查显示肿瘤出现萎缩性变化，雌激素受体水平表达降低。为了研究CGS抗肿瘤作用的机制，我们研究了给予该药物的大鼠内分泌功能的变化。在接受超过1mg/kg CGS的组中，血清雌二醇和催乳素水平低于对照组，而血清促黄体生成素水平高于对照组。在用CGS治疗的大鼠中，卵巢重量增加，而子宫和垂体重量减少。这些变化呈剂量依赖性。相比之下，血清皮质酮水平和肾上腺重量保持不变。我们得出结论，CGS通过改变激素环境来抑制激素依赖性肿瘤的生长。
