Dunzendorfer U, Releyea N, Whitmore W F, Fogh J, Balis M E
Arzneimittelforschung. 1984;34(1):36-9.
Difluoromethylornithine (DFMO) and methylglyoxal-bis(guanyl-hydrazone) (MGBG), inhibitors of ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase (AMDC), respectively, were tested in two experimental prostatic cancer models. DFMO resulted in a reduction in tumor size in both the rapidly growing R-3327 rat prostatic adenocarcinoma (30.5 +/- 15 versus 61 +/- 9.5 in control animals) and the human DU-145 adenocarcinomas (1.7 ml versus 3.3 ml in control animals) in nude mice. MGBG was tested only in the rat tumor, where it induced a reduction of 22.9 +/- 9.5 ml versus 61 +/- 9.5 in control animals in tumor size but was highly toxic. Flutamide or 9-B-D-arabinofuranosyladenine (Ara-A) proved ineffective per se in reducing tumor growth of the human DU-145 or of the R-3327-G strain, respectively, but increased the efficacy of DFMO against the DU-145 tumor had a high level of ODC which was reduced by DFMO of by Ara-A; the R-3327 tumor had a low level of ODC which was too low to be decreased by DFMO.
二氟甲基鸟氨酸(DFMO)和甲基乙二醛双(胍腙)(MGBG)分别是鸟氨酸脱羧酶(ODC)和S-腺苷甲硫氨酸脱羧酶(AMDC)的抑制剂,在两种实验性前列腺癌模型中进行了测试。DFMO使快速生长的R-3327大鼠前列腺腺癌(对照动物为61±9.5,处理后为30.5±15)以及裸鼠中的人DU-145腺癌(对照动物为3.3 ml,处理后为1.7 ml)的肿瘤大小均减小。MGBG仅在大鼠肿瘤中进行了测试,它使肿瘤大小减小,对照动物为61±9.5,处理后为22.9±9.5,但毒性很高。氟他胺或9-β-D-阿拉伯呋喃糖基腺嘌呤(Ara-A)本身分别对减少人DU-145或R-3327-G株的肿瘤生长无效,但可提高DFMO对DU-145肿瘤的疗效,该肿瘤具有高水平的ODC,可被DFMO或Ara-A降低;R-3327肿瘤的ODC水平较低,低到无法被DFMO降低。