Department of Surgery, Institute of Health Biosciences, The University of Tokushima Graduate School, 3-18-15 Kuramoto-cho, Tokushima City 770-8503, Japan.
Int J Clin Oncol. 2011 Dec;16(6):671-8. doi: 10.1007/s10147-011-0246-y. Epub 2011 May 10.
Histone deacetylase (HDAC) is strongly associated with epigenetic regulation and carcinogenesis, and its inhibitor can induce the differentiation or apoptosis of cancer cells.
We investigated the anticancer effects of the HDAC inhibitor valproic acid (VPA) in combination with gemcitabine (GEM), an antimetabolic, and pegylated interferon-α2b (PEG-IFN-α2b) in a human pancreatic cancer cell line using a cell proliferation assay. The gene expressions of HDAC1, MTA1, p21(Waf1), and HIF-1 were evaluated by reverse transcription-PCR.
Valproic acid at 0.5 mM when used alone did not suppress cell proliferation. PEG-IFN-α2b at 10(2 )E/ml weakly suppressed cell proliferation in both the BxPC3 (by 28%) and SUIT-2 (by 17%) human pancreatic cancer cell lines. GEM at 5 nM when used alone suppressed cell proliferation by 36 and 61% in the BxPC3 and SUIT-2 cell lines, respectively. The combination treatment of GEM + PEG-IFN-α2b strongly suppressed cell proliferation in the SUIT-2 (82%) and BxPC3 (51%) cell lines, which was further reinforced by the addition of VPA up to 88 and 67%, respectively. The combination treatment of GEM + PEG-IFN-α2b enhanced the expression of p21(Waf1), which was also reinforced by VPA.
VPA augmented the inhibitory effects of PEG-IFN-α2b alone or in combination with PEG-IFN-α2b and GEM on cell proliferation. Such inhibitory effects may be due to the up-regulation of p21(Waf1) expression.
组蛋白去乙酰化酶(HDAC)与表观遗传调控和癌症发生密切相关,其抑制剂可诱导癌细胞分化或凋亡。
我们通过细胞增殖试验,研究了组蛋白去乙酰化酶抑制剂丙戊酸(VPA)与代谢抑制剂吉西他滨(GEM)和聚乙二醇化干扰素-α2b(PEG-IFN-α2b)联合应用对人胰腺癌细胞系的抗癌作用。采用逆转录-PCR 法检测 HDAC1、MTA1、p21(Waf1)和 HIF-1 的基因表达。
单独使用 0.5mM 的 VPA 不能抑制细胞增殖。PEG-IFN-α2b 在 10(2)E/ml 时微弱抑制 BxPC3(28%)和 SUIT-2(17%)人胰腺癌细胞系的细胞增殖。单独使用 5nM 的 GEM 可使 BxPC3 和 SUIT-2 细胞系的细胞增殖分别抑制 36%和 61%。GEM+PEG-IFN-α2b 联合治疗强烈抑制 SUIT-2(82%)和 BxPC3(51%)细胞系的细胞增殖,而添加 VPA 可分别增强至 88%和 67%。GEM+PEG-IFN-α2b 联合治疗增强了 p21(Waf1)的表达,而 VPA 进一步增强了这种表达。
VPA 增强了 PEG-IFN-α2b 单独或与 GEM 和 PEG-IFN-α2b 联合使用对细胞增殖的抑制作用。这种抑制作用可能是由于 p21(Waf1)表达的上调所致。