A neuropeptide, Substance P (SP), has mitogenic action in many types of cancer cells mediated via the neurokinin-1 receptor (NK1R). Small molecular NK1R antagonists have been frequently shown to possess anticancer activity both in vivo and in vitro, but there are only a few papers on such activity regarding peptide antagonists. In order to extend the data on this class of compounds, we have compared the effects of a peptide antagonist, [D-Pro2, D-Trp7,9]-Substance P, and a small molecular antagonist, aprepitant on the proliferation of five cancer and three normal cell lines. The comparison was based on three assays: cell proliferation test, MTT test and assay for colony formation. Consistently with earlier reports, aprepitant potently reduced cell proliferation in cancer cell lines in all assays, but in contrast to previous works, the compound was not selective and it affected normal cell lines to a similar degree. The studied peptide antagonist, [D-Pro2, D-Trp7,9]-Substance P, was able to decrease proliferation only in a few cell lines, and only in the highest concentration (100 µM). In a lower concentration, a slight pro-proliferative effect was observed in a few cell lines. No statistically significant effects on colony formation were found for this compound.

中文翻译：

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[D-Pro2, D-Trp7,9]-物质 P 和阿瑞匹坦对几种癌细胞系的抗增殖作用及其与正常细胞相比的选择性

神经肽物质 P (SP) 在通过神经激肽-1 受体 (NK1R) 介导的多种癌细胞中具有促有丝分裂作用。小分子 NK1R 拮抗剂经常被证明在体内和体外都具有抗癌活性，但关于肽拮抗剂的这种活性的论文很少。为了扩展此类化合物的数据，我们比较了肽拮抗剂 [D-Pro2, D-Trp7,9]-物质 P 和小分子拮抗剂阿瑞匹坦对五种癌症增殖的影响和三个正常细胞系。比较基于三种分析：细胞增殖测试、MTT测试和集落形成分析。与之前的报告一致，阿瑞匹坦在所有检测中都有效地降低了癌细胞系的细胞增殖，但与之前的工作相反，该化合物没有选择性，它对正常细胞系的影响程度相似。所研究的肽拮抗剂 [D-Pro2, D-Trp7,9]-Substance P 只能在少数细胞系中降低增殖，并且只能在最高浓度 (100 µM) 中降低。在较低浓度下，在一些细胞系中观察到轻微的促增殖作用。未发现该化合物对集落形成有统计学意义的影响。