Zupi G, Greco C, Laudonio N, Benassi M, Silvestrini B, Caputo A
Anticancer Res. 1986 Sep-Oct;6(5):1245-9.
Lonidamine (LND), a powerful antispermatogenic compound, has been shown to impair differentially the energy metabolism of normal and neoplastic cells and to increase significantly the survival of animal bearing experimental tumors. Clinical trials are presently ongoing and preliminary favourable results have been obtained with LND as a single agent or associated with other antineoplastic drugs. In this work the effect of the combination LND plus ADM was investigated on in vitro and in vivo tumors. The in vitro effect was analysed by the colony forming technique and the in vivo antitumor activity was assessed by means of local control parameters, increase in host lifespan and weight reduction of metastasing target organs (liver, kidney, ovary). The results obtained indicate that LND is poorly effective when used alone, while a very high cytotoxicity is observed when it is combined with ADM. Exposure of cells to different time-sequences and schedules of both drugs elicits a different response. In particular a synergistic effect is obtained when ADM precedes LND. These results have been preliminarily confirmed by in vivo studies.
氯尼达明（LND）是一种强效抗生精化合物，已被证明对正常细胞和肿瘤细胞的能量代谢有不同程度的损害，并能显著提高荷实验性肿瘤动物的存活率。目前正在进行临床试验，并且已获得了将LND作为单一药物或与其他抗肿瘤药物联合使用的初步良好结果。在这项研究中，研究了LND加阿霉素（ADM）联合用药对体外和体内肿瘤的影响。通过集落形成技术分析体外效应，并通过局部控制参数、宿主寿命延长以及转移靶器官（肝脏、肾脏、卵巢）重量减轻来评估体内抗肿瘤活性。所得结果表明，单独使用LND时效果不佳，而与ADM联合使用时则观察到非常高的细胞毒性。细胞暴露于两种药物的不同时间顺序和给药方案会引发不同的反应。特别是当ADM先于LND给药时可获得协同效应。这些结果已得到体内研究的初步证实。
