There is a variety of antineoplastic drugs that are based on natural compounds from ecological niches with high evolutionary pressure. We used two cell lines (Jurkat J16 and Ramos) in a screening to assess 300 different naturally occurring compounds with regard to their antineoplastic activity. The results of the compounds 4,6-dibromo-2-(2',4'-dibromophenoxy)phenol (P01F03), 4,5,6-tribromo-2-(2',4'-dibromophenoxy)phenol (P01F08), and 5-epi-nakijinone Q (P03F03) prompted us to perform further research. Using viability and apoptosis assays on the cell lines of primary human leukemic and normal hematopoietic cells, we found that P01F08 induced apoptosis in the cell lines at IC50 values between 1.61 and 2.95 μM after 72 h. IC50 values of peripheral blood mononuclear cells (PBMNCs) from healthy donors were higher, demonstrating that the cytotoxicity in the cell lines reached 50%, while normal PBMNCs were hardly affected. The colony-forming unit assay showed that the hematopoietic progenitor cells were not significantly affected in their growth by P01F08 at a concentration of 3 μM. P01F08 showed a 3.2-fold lower IC50 value in primary leukemic cells [acute myeloid leukemia (AML)] compared to the PBMNC of healthy donors. We could confirm the antineoplastic effect of 5-epi-nakijinone Q (P03F03) on the cell lines via the induction of apoptosis but noted a similarly strong cytotoxic effect on normal PBMNCs.

中文翻译：

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筛选300种天然存在的化合物的初步结果：4,6-二溴-2-（2'，4'-二溴苯氧基）苯酚，4,5,6-三溴-2-（2'，4'-二溴苯氧基）苯酚，5-表-nakijinone Q作为具有抗癌潜力的物质。

有多种抗肿瘤药是基于具有高进化压力的生态位的天然化合物。我们在筛选中使用了两种细胞系（Jurkat J16和Ramos）来评估300种不同天然化合物的抗肿瘤活性。化合物4,6-二溴-2-（2'，4'-二溴苯氧基）苯酚（P01F03），4,5,6-三溴-2-（2'，4'-二溴苯氧基）苯酚（P01F08）的结果，以及5-epi-nakijinone Q（P03F03）促使我们进行进一步的研究。通过在原代人白血病和正常造血细胞的细胞系上进行活力和凋亡分析，我们发现P01F08在72 h后以1.61和2.95μM之间的IC50值诱导了细胞系的凋亡。健康捐献者外周血单个核细胞（PBMNC）的IC50值较高，表明细胞系的细胞毒性达到了50％，而正常PBMNC几乎没有受到影响。集落形成单位测定法显示，浓度为3μM的P01F08对造血祖细胞的生长没有显着影响。与健康捐献者的PBMNC相比，P01F08在原代白血病细胞[急性髓细胞性白血病（AML）]中显示出较低的IC50值3.2倍。我们可以通过诱导细胞凋亡来确认5-表-nakijinone Q（P03F03）对细胞系的抗肿瘤作用，但注意到对正常PBMNCs具有相似的强细胞毒性作用。与健康捐献者的PBMNC相比，P01F08在原代白血病细胞[急性髓细胞性白血病（AML）]中显示出较低的IC50值3.2倍。我们可以通过诱导细胞凋亡来确认5-表-nakijinone Q（P03F03）对细胞系的抗肿瘤作用，但注意到对正常PBMNCs具有相似的强细胞毒性作用。与健康捐献者的PBMNC相比，P01F08在原代白血病细胞[急性髓细胞性白血病（AML）]中显示出较低的IC50值3.2倍。我们可以通过诱导细胞凋亡来确认5-表-nakijinone Q（P03F03）对细胞系的抗肿瘤作用，但注意到对正常PBMNCs具有相似的强细胞毒性作用。