新型强效促黄体生成素释放激素激动剂ICI 118630的抗肿瘤活性
Anti-tumour activity of ICI 118630, a new potent luteinizing hormone-releasing hormone agonist.
作者信息
Nicholson R I, Maynard P V
出版信息
Br J Cancer. 1979 Mar;39(3):268-73. doi: 10.1038/bjc.1979.50.
Abstract
Experiments were undertaken with DMBA-induced mammary tumours of the rat to determine the anti-tumour properties of a new and potent luteinizing hormone releasing hormone (LH-RH) agonist, [D-Ser(But) 6Azgly10]-LH-RH (ICI 118630). Tumours were classified according to their oestrogen-receptor (ER) content. Twice daily i.m. injections of either 5 micrograms or 0.5 micrograms ICI 118630 in saline were as effective as ovariectomy or tamoxifen therapy in causing the regression of ER+ DMBA-induced mammary tumours. ER- mammary tumours showed a more equivocal overall response to ICI 118630, some tumours progressing, others regressing. About one-third of the ER+ tumours disappeared in the 20-day treatment period. Those tumours which did regrow after the cessation of treatment proved to be hormone-dependent. In addition to the inhibitory effects of the LH-RH agonist on pre-existing tumours, ICI 118630 also reduced the total number of new tumours formed during and after treatment.
摘要
利用二甲基苯蒽（DMBA）诱导的大鼠乳腺肿瘤进行实验，以确定一种新型强效促黄体生成素释放激素（LH-RH）激动剂[D-丝氨酸（叔丁基）6、氮杂甘氨酸10]-LH-RH（ICI 118630）的抗肿瘤特性。根据肿瘤的雌激素受体（ER）含量对肿瘤进行分类。每天两次在盐水中腹腔注射5微克或0.5微克ICI 118630，在促使ER阳性的DMBA诱导的乳腺肿瘤消退方面，其效果与卵巢切除术或他莫昔芬治疗相同。ER阴性的乳腺肿瘤对ICI 118630的总体反应更为模糊，一些肿瘤进展，另一些则消退。约三分之一的ER阳性肿瘤在20天的治疗期内消失。那些在治疗停止后确实重新生长的肿瘤被证明是激素依赖性的。除了LH-RH激动剂对已存在肿瘤的抑制作用外，ICI 118630还减少了治疗期间及治疗后形成的新肿瘤总数。
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