新型组蛋白去乙酰化酶抑制剂SK-7041对人肺癌和乳腺癌细胞的抗肿瘤活性。
Antitumor activity of SK-7041, a novel histone deacetylase inhibitor, in human lung and breast cancer cells.
作者信息
Lee Keun-Wook, Kim Jee Hyun, Park Jung-Hyun, Kim Hwang-Phill, Song Sang-Hyun, Kim Sang Gyun, Kim Tai Young, Jong Hyun-Soon, Jung Kyung Hae, Im Seock-Ah, Kim Tae-You, Kim Noe Kyeong, Bang Yung-Jue
机构信息
Department of Internal Medicine, Seoul National University College of Medicine, Seoul, Korea.
出版信息
Anticancer Res. 2006 Sep-Oct;26(5A):3429-38.
BACKGROUND
A class of synthetic histone deacetylase (HDAC) inhibitors, which are hybrids of trichostatin A and MS-275 were previously developed. In this study, the antitumor effects of SK-7041, one of those novel HDAC inhibitors, was evaluated on lung and breast cancer cell lines.
MATERIALS AND METHODS
Human lung and breast cancer cells, as well as normal human bronchial epithelial (NHBE) cells were treated with SK-7041, and results were compared with those of cells treated with suberoylanilide hydroxamic acid (SAHA).
RESULTS
SK-7041 induced time-dependent histone hyperacetylation and showed more potent cytotoxicity than SAHA in cancer cells. These antiproliferative effects of SK-7041 were due to apoptotic cell death caused by G2/M-phase arrest and to a lesser extent to G1 arrest. Moreover, SK-7041 inhibited cancer cell proliferation more selectively than NHBE cell proliferation.
CONCLUSIONS
These results suggest that SK-7041 may have potential anticancer activity.
背景
先前已开发出一类合成组蛋白去乙酰化酶（HDAC）抑制剂，它们是曲古抑菌素A和MS-275的杂合物。在本研究中，对其中一种新型HDAC抑制剂SK-7041在肺癌和乳腺癌细胞系上的抗肿瘤作用进行了评估。
材料与方法
用SK-7041处理人肺癌和乳腺癌细胞以及正常人支气管上皮（NHBE）细胞，并将结果与用辛二酰苯胺异羟肟酸（SAHA）处理的细胞的结果进行比较。
结果
SK-7041诱导时间依赖性组蛋白高乙酰化，并且在癌细胞中显示出比SAHA更强的细胞毒性。SK-7041的这些抗增殖作用归因于G2/M期阻滞引起的凋亡性细胞死亡，在较小程度上归因于G1期阻滞。此外，SK-7041比NHBE细胞增殖更具选择性地抑制癌细胞增殖。
结论
这些结果表明SK-7041可能具有潜在的抗癌活性。
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