Peehl D M, Wong S T, Stamey T A
Division of Urology, Stanford Medical Center, California.
J Urol. 1991 Mar;145(3):624-30. doi: 10.1016/s0022-5347(17)38408-2.
Suramin is currently undergoing clinical trials as a chemotherapeutic agent for prostate cancer. The effects of suramin on cultured human epithelial cells derived from normal, benign hyperplastic, and malignant prostate tissues were examined. In serum-free medium, suramin inhibited the clonal growth of prostate cells at a half-maximal dose of approximately 10 micrograms/ml. Growth inhibition by suramin was completely reversible even after 24 hours of exposure. In conjunction, suramin did not alter cellular phenotype with regard to expression of keratins and prostate-specific antigens. Although suramin is reportedly an antagonist of growth factor-mediated mitogenesis, ten-fold excesses of growth factors did not appreciably suppress the cytostatic activity of suramin. In comparison to the activities of other possible chemotherapeutic agents, suramin would appear suboptimal because its inhibitory effects are reversible and it does not induce a terminally differentiated cellular phenotype.
苏拉明目前正在作为一种前列腺癌化疗药物进行临床试验。研究了苏拉明对源自正常、良性增生和恶性前列腺组织的培养人上皮细胞的影响。在无血清培养基中,苏拉明以约10微克/毫升的半数最大剂量抑制前列腺细胞的克隆生长。即使暴露24小时后,苏拉明对生长的抑制也是完全可逆的。同时,苏拉明在角蛋白和前列腺特异性抗原的表达方面并未改变细胞表型。尽管据报道苏拉明是生长因子介导的有丝分裂的拮抗剂,但十倍过量的生长因子并不能明显抑制苏拉明的细胞生长抑制活性。与其他可能的化疗药物的活性相比,苏拉明似乎并不理想,因为其抑制作用是可逆的,并且不会诱导终末分化的细胞表型。