Lamoureux François, Picarda Gaëlle, Rousseau Julie, Gourden Clothilde, Battaglia Séverine, Charrier Céline, Pitard Bruno, Heymann Dominique, Rédini Françoise
INSERM, ERI 7, Université de Nantes, Nantes atlantique universités, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives, EA3822, 1 rue Gaston Veil, 44035 Nantes cedex 1, France.
Mol Cancer Ther. 2008 Oct;7(10):3389-98. doi: 10.1158/1535-7163.MCT-08-0497.
Osteosarcoma is the most frequent primary bone tumor that develops mainly during youth, the median age of diagnosis being 18 years. Despite improvement in osteosarcoma treatment, survival rate is only 30% after 5 years for patients with pulmonary metastases at diagnosis. This warrants exploration of new therapeutic options. The anti-bone resorption molecule receptor activator of NF-kappaB (RANK) is very promising, as it may block the vicious cycle between bone resorption and tumor proliferation that takes place during tumor development in bone site. The cDNA encoding murine RANK-Fc (mRANK-Fc) was administered by gene transfer using an amphiphilic polymer in a mouse model of osteolytic osteosarcoma. Clinical and bone microarchitecture variables were assessed by radiography and micro-CT analyses. In vitro experiments were designed to determine the mechanism of action of RANK-Fc on tumor cell proliferation (XTT assays), apoptosis (caspase activation), cell cycle distribution (fluorescence-activated cell sorting analysis), or gene expression (reverse transcription-PCR). RANK-Fc was effective in preventing the formation of osteolytic lesions associated with osteosarcoma development and in reducing the tumor incidence, the local tumor growth, and the lung metastases dissemination leading to a 3.9-fold augmentation of mice survival 28 days after implantation. On the contrary, mRANK-Fc did not prevent the development of nonosseous tumor nodules, suggesting that bone environment is necessary for mRANK-Fc therapeutic efficacy. Furthermore, mRANK-Fc has no direct activity on osteosarcoma cells in vitro. mRANK-Fc exerts an indirect inhibitory effect on osteosarcoma progression through inhibition of bone resorption.
骨肉瘤是最常见的原发性骨肿瘤,主要发生于青少年,诊断的中位年龄为18岁。尽管骨肉瘤治疗有所改善,但诊断时伴有肺转移的患者5年后生存率仅为30%。这就需要探索新的治疗选择。抗骨吸收分子核因子κB受体激活剂(RANK)很有前景,因为它可能阻断骨吸收与肿瘤增殖之间的恶性循环,这种恶性循环在骨部位肿瘤发展过程中发生。在溶骨性骨肉瘤小鼠模型中,使用两亲性聚合物通过基因转移给予编码鼠RANK-Fc(mRANK-Fc)的cDNA。通过X线摄影和显微CT分析评估临床和骨微结构变量。体外实验旨在确定RANK-Fc对肿瘤细胞增殖(XTT分析)、凋亡(半胱天冬酶激活)、细胞周期分布(荧光激活细胞分选分析)或基因表达(逆转录PCR)的作用机制。RANK-Fc有效地预防了与骨肉瘤发展相关的溶骨性病变的形成,并降低了肿瘤发生率、局部肿瘤生长和肺转移扩散,导致植入后28天小鼠生存率提高3.9倍。相反,mRANK-Fc不能预防非骨性肿瘤结节的发展,这表明骨环境是mRANK-Fc治疗效果所必需的。此外,mRANK-Fc在体外对骨肉瘤细胞没有直接活性。mRANK-Fc通过抑制骨吸收对骨肉瘤进展发挥间接抑制作用。