给予促黄体生成素释放激素拮抗剂后，大鼠前列腺癌肿瘤大小减小。
Prostate carcinoma tumor size in rats decreases after administration of antagonists of luteinizing hormone-releasing hormone.
作者信息
Redding T W, Coy D H, Schally A V
出版信息
Proc Natl Acad Sci U S A. 1982 Feb;79(4):1273-6. doi: 10.1073/pnas.79.4.1273.
The effects of two potent antagonistic analogues of luteinizing hormone-releasing hormone (LH-RH) on the growth of two different models of rat prostate tumors have been investigated. Chronic administration of [NAc-p-F-DPhe1,p-Cl-DPhe2,DTrp3.6,D-Ala10]LH-RH (antagonist I) at 50 micrograms/day for 21 days significantly inhibited the growth of the chemically induced squamous cell carcinoma 11095 in Fisher 344 male rats. The weights of the pituitary, ventral prostate, and testes were not significantly altered. After 21 days of treatment with this analogue serum luteinizing hormone (lutropin), follicle-stimulating hormone, and testosterone levels were markedly decreased. When male Copenhagen F-1 rats bearing the Dunning 3327H prostate adenocarcinoma were injected with antagonist I at 50 micrograms/day for 6 weeks or with [NAc-p-Cl-DPhe1,2,DTrp3,DPhe6,DAla10]LH-RH (antagonist II) at 50 micrograms/day for 17 days, the percentage increase in tumor volume was decreased to half or less and the actual tumor volume was diminished 34-96% compared to controls. Tumor weight was decreased 30% and 89% after antagonist I and, respectively, compared to untreated controls. The tumor doubling time was 3- to 4-fold longer in rats receiving the inhibitory analogues than in the controls. Treatment with antagonist II decreased the weight of the whole prostate, but neither antagonist changed the weight of testes, anterior pituitary gland, or adrenals. Serum luteinizing hormone, follicle-stimulating hormone, and testosterone levels in Copenhagen F-1 rats bearing Dunning tumors were significantly decreased after treatment with the inhibitory analogues, but progesterone levels were increased. The inhibitory effects of these antagonistic analogues on rat prostate tumors suggest that these compound might be considered in the development of new types of therapy for prostate carcinoma and other endocrine-dependent neoplasias.
研究了两种促黄体生成激素释放激素（LH-RH）强效拮抗类似物对两种不同大鼠前列腺肿瘤模型生长的影响。以50微克/天的剂量连续21天给予[NAc-p-F-DPhe1,p-Cl-DPhe2,DTrp3.6,D-Ala10]LH-RH（拮抗剂I），可显著抑制费希尔344雄性大鼠化学诱导的鳞状细胞癌11095的生长。垂体、腹侧前列腺和睾丸的重量未发生显著改变。用该类似物治疗21天后，血清促黄体生成素（促性腺激素）、促卵泡激素和睾酮水平显著降低。当给患有邓宁3327H前列腺腺癌的雄性哥本哈根F-1大鼠每天注射50微克拮抗剂I，持续6周，或每天注射50微克[NAc-p-Cl-DPhe1,2,DTrp3,DPhe6,DAla10]LH-RH（拮抗剂II），持续17天时，肿瘤体积的百分比增加降至一半或更低，与对照组相比，实际肿瘤体积减小了34%-96%。与未治疗的对照组相比，拮抗剂I治疗后肿瘤重量分别降低了30%和89%。接受抑制性类似物治疗的大鼠的肿瘤倍增时间比对照组延长了3至4倍。用拮抗剂II治疗可降低整个前列腺的重量，但两种拮抗剂均未改变睾丸、垂体前叶或肾上腺的重量。用抑制性类似物治疗后，患有邓宁肿瘤的哥本哈根F-1大鼠的血清促黄体生成素、促卵泡激素和睾酮水平显著降低，但孕酮水平升高。这些拮抗类似物对大鼠前列腺肿瘤的抑制作用表明，在开发新型前列腺癌和其他内分泌依赖性肿瘤的治疗方法时，可能会考虑这些化合物。
Zotero 插件