Ravera F, Miglietta L, Pirani P, Ferrini S, Favoni R E
Department of Experimental Pharmacology, Istituto Nazionale per la Ricerca sul Cancro, Genova, Italy.
Eur J Cancer. 1993;29A(2):225-30. doi: 10.1016/0959-8049(93)90180-n.
Suramin, a polyanionic drug used in the treatment of trypanosomiasis and onchocerciasis, inhibits growth factor-induced mitogenesis in several human tumours. We have investigated the effect of suramin on human breast cancer cell lines (HBCCL). By cell counts and thymidine incorporation we found that 50 to 400 micrograms/ml suramin inhibits the proliferation of HBCCL in a dose-dependent and reversible fashion (ID50 approximately 200 micrograms/ml for MCF-7 and MDA-MB 231). Radioreceptor and affinity cross-linking assays showed that suramin was also able to reduce the binding of insulin-like growth factor I (IGF-I) to its receptor (40-50% inhibition at 100 micrograms/ml). Our results indicate that the drug does not affect the IGF-I receptor (IGF-I-R), but binds directly to the IGF-I peptide. In conclusion, the strict correlation observed between suramin inhibition of proliferation and IGF-I binding on HBCCL suggests a possible therapeutic role for this molecule as an antineoplastic drug in human breast tumours.
苏拉明是一种用于治疗锥虫病和盘尾丝虫病的多阴离子药物,它能抑制多种人类肿瘤中生长因子诱导的有丝分裂。我们研究了苏拉明对人乳腺癌细胞系(HBCCL)的影响。通过细胞计数和胸腺嘧啶核苷掺入法,我们发现50至400微克/毫升的苏拉明以剂量依赖且可逆的方式抑制HBCCL的增殖(MCF-7和MDA-MB 231的半数抑制剂量约为200微克/毫升)。放射受体和亲和交联分析表明,苏拉明还能够减少胰岛素样生长因子I(IGF-I)与其受体的结合(在100微克/毫升时抑制40 - 50%)。我们的结果表明,该药物不影响IGF-I受体(IGF-I-R),而是直接与IGF-I肽结合。总之,在HBCCL上观察到的苏拉明对增殖的抑制与IGF-I结合之间的严格相关性表明,该分子作为一种抗肿瘤药物在人类乳腺肿瘤中可能具有治疗作用。