卤代黄烷酮类化合物作为潜在的诱导细胞凋亡试剂：合成与生物活性评价。
Halogenated flavanones as potential apoptosis-inducing agents: synthesis and biological activity evaluation.
机构信息
Institute of Biochemistry and Biophysics, University of Tehran, PO Box 13145-1384, Tehran, Iran.
出版信息
Eur J Med Chem. 2012 Dec;58:573-80. doi: 10.1016/j.ejmech.2012.10.043. Epub 2012 Nov 2.
A series of halogenated flavanones were synthesized from 2-hydroxychalcones and tested for their cytotoxicity against a panel of human cancer cell lines. Among the synthesized compounds, 3',7-dichloroflavanone (2d) showed the highest activity against MCF-7, LNCaP, PC3, Hep-G2, KB and SK-N-MC cells. However, 3',6-dichloroflavanone (2g) with IC(50) value of 2.9 ± 0.9 μM was the most potent compound against MDA-MB-231 cells, being approximately 12 times more active than etoposide as reference drug. According to the flow-cytometric analysis, compound 2g can induce apoptosis by 66.19 and 21.37% in PC3 and MDA-MB-231 cells, respectively. The results of acridine orange/ethidium bromide staining and TUNEL assay suggested that the cytotoxic activity of this compound in PC3 and MDA-MB-231 cells occurs via apoptosis.
从 2-羟基查耳酮合成了一系列卤代黄烷酮，并测试了它们对一系列人类癌细胞系的细胞毒性。在所合成的化合物中，3'，7-二氯黄烷酮（2d）对 MCF-7、LNCaP、PC3、Hep-G2、KB 和 SK-N-MC 细胞的活性最高。然而，具有 IC50值为 2.9 ± 0.9 μM 的 3'，6-二氯黄烷酮（2g）是对 MDA-MB-231 细胞最有效的化合物，作为参考药物，其活性约为依托泊苷的 12 倍。根据流式细胞术分析，化合物 2g 可分别诱导 PC3 和 MDA-MB-231 细胞中的 66.19%和 21.37%的细胞凋亡。吖啶橙/溴化乙锭染色和 TUNEL 检测结果表明，该化合物在 PC3 和 MDA-MB-231 细胞中的细胞毒性通过细胞凋亡发生。
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