Schirner M, Schneider M R
Research Laboratories of Schering AG, Berlin, Federal Republic of Germany.
J Cancer Res Clin Oncol. 1992;118(7):497-501. doi: 10.1007/BF01225263.
Investigations on mechanisms of metastatic tumour spread revealed a role for compounds that inhibit tumour dissemination at the time of hematogenous dissemination. The platelet aggregation inhibitor prostacyclin and its stable analogues were shown to inhibit tumour-cell-induced platelet interaction as well as tumour cell adhesive mechanisms. This study concentrates on the effect of the stable prostacyclin analogue cicaprost: 5-[(E)-(1S,5S,6S,7R)-7-hydroxy-6-[(3S,4S)-3-hydroxy-4-methylnona-1 ,6- diinyl]-bicyclo[3,3,0]octan-3-ylidene]-3-oxapentanoic acid (Schering AG), as cyclodextrin clathrate, on spontaneous tumour metastases of two different carcinomas of the rat. In Cop rats bearing spontaneously metastasizing R 3327 MAT Lu prostate carcinomas, cicaprost (1.0 mg/kg p.o. daily) inhibited the number of lung metastases by about 80%, whereas the lower doses (0.1 and 0.5 mg/kg) exhibited borderline efficacy. In female Wistar-Furth rats bearing s.c. implanted SMT 2A mammary carcinomas, spontaneously metastasizing into regional lymph nodes and lungs, cicaprost (0.1, 0.5 and 1 mg/kg) p.o. daily exhibited a dose-dependent inhibition of the number of lung metastases. Five out of ten animals treated by 1 mg/kg were free of visible lung metastases. The weight of the axillary lymph node was significantly reduced by the 1 mg/kg dose of cicaprost, whereas lower doses had no effect on the weight of the lymph nodes. The growth of the primary tumour was not influenced by cicaprost in the R 3327 MAT Lu prostate carcinoma nor in the SMT 2A mammary carcinoma in the dose range tested. In conclusion, the stable prostacyclin analogue cicaprost exhibits a strong antimetastatic action in two metastasizing tumours of the rat and interferes with the steps not only of haematogenous, but also of lymphogenous metastasis.
对转移性肿瘤扩散机制的研究揭示了某些化合物在血行播散时对抑制肿瘤扩散的作用。血小板聚集抑制剂前列环素及其稳定类似物已被证明可抑制肿瘤细胞诱导的血小板相互作用以及肿瘤细胞黏附机制。本研究聚焦于稳定的前列环素类似物西卡前列素:5-[(E)-(1S,5S,6S,7R)-7-羟基-6-[(3S,4S)-3-羟基-4-甲基壬-1,6-二烯基]-双环[3,3,0]辛-3-亚基]-3-氧代戊酸(先灵公司),作为环糊精包合物,对大鼠两种不同癌自发肿瘤转移的影响。在携带自发转移的R 3327 MAT Lu前列腺癌的Cop大鼠中,西卡前列素(每日口服1.0毫克/千克)可使肺转移瘤数量减少约80%,而较低剂量(0.1和0.5毫克/千克)的疗效不明显。在皮下植入SMT 2A乳腺癌且自发转移至局部淋巴结和肺部的雌性Wistar-Furth大鼠中,每日口服西卡前列素(0.1、0.5和1毫克/千克)对肺转移瘤数量呈现剂量依赖性抑制作用。接受1毫克/千克治疗的十只动物中有五只没有可见的肺转移瘤。1毫克/千克剂量的西卡前列素可使腋窝淋巴结重量显著减轻,而较低剂量对淋巴结重量没有影响。在所测试的剂量范围内,西卡前列素对R 3327 MAT Lu前列腺癌和SMT 2A乳腺癌的原发肿瘤生长均无影响。总之,稳定的前列环素类似物西卡前列素在大鼠的两种转移性肿瘤中表现出强大的抗转移作用,不仅干扰血行转移步骤,还干扰淋巴转移步骤。