苯乙酮衍生物通过蛋白酶体抑制前列腺癌细胞的抗肿瘤活性。

Yun-Hee Lee, Jaesuk Yun, Jae-chul Jung, Seikwan Oh, Young-Suk Jung
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引用次数: 5

摘要

一些查尔酮衍生物具有抗炎、抗氧化和抗肿瘤活性等生物学特性。查尔酮衍生物可诱导不同类型的癌细胞凋亡,但其作用机制尚不明确。本研究以前列腺癌细胞为工作模型,研究查尔酮家族的合成化合物苯甲醚苯乙酮衍生物(JC3)在人类癌症中的主要作用靶点。在这里,我们表明JC3抑制蛋白酶体活性,这是体外和基于细胞的测定所表明的。特别是在蛋白酶体抑制方面,jc3 -二聚体比单体更有效,显著诱导前列腺癌细胞凋亡。由于蛋白酶体在人类肿瘤进展、侵袭和转移生物学中的重要作用,这些发现为开发新的抗肿瘤药物提供了重要线索。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Anti-tumor activity of benzylideneacetophenone derivatives via proteasomal inhibition in prostate cancer cells.
A number of some chalcone derivatives possess promising biological properties including anti-inflammation, anti-oxidant, and anti-tumor activity. Although it has been shown that some derivatives of chalcone induce apoptosis in different kinds of cancer cells, the involved mechanism of action is not well defined. The purpose of this study is to investigate the primary target of a benzylideneacetophenone derivative (JC3), which is a synthetic compound derived from the chalcone family, in human cancer, using prostate cancer cells as a working model. Herein, we show that JC3 inhibits proteasomal activity as indicated by both in vitro and in cell-based assays. Especially, the JC3-dimer was more potent than monomer in the aspect of proteasome inhibition, which induced apoptosis significantly in the prostate cancer cells. Owing to the critical roles of the proteasome in the biology of human tumor progression, invasion, and metastasis, these findings give an important clue for the development of novel anti-tumor agents.
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