Dipartimento di Patologia e Oncologia Sperimentali, Università degli Studi di Firenze, Istituto Toscano Tumori, Firenze, Italy.
Epigenetics. 2013 Feb;8(2):210-9. doi: 10.4161/epi.23538. Epub 2013 Jan 15.
We analyzed the activity of the histone deacetylase inhibitor (HDACi) suberoyl-anilide hydroxamic acid (SAHA) on Kasumi-1 acute myeloid leukemia (AML) cells expressing AML1/ETO. We also compared the effects of SAHA to those of valproic acid (VPA), a short-chain fatty acid HDACi. SAHA and VPA induced histone H3 and H4 acetylation, myeloid differentiation and massive early apoptosis. The latter effects were not determined by either drug in AML cell lines, such as NB4 or THP-1, not expressing AML1/ETO. SAHA was more rapid and effective than VPA in increasing H3 and H4 acetylation in total Kasumi-1 cell lysates and more effective than VPA in inducing acetylation of H4K8, H4K12, H4K16 residues. At the promoter of IL3, a transcriptionally-silenced target of AML1/ETO, SAHA was also more rapid than VPA in inducing total H4, H4K5, H4K8 and H3K27 acetylation, while VPA was more effective than SAHA at later times in inducing acetylation of total H4, H4K12, H4K16, as well as total H3. Consistent with these differences, SAHA induced the expression of IL3 mRNA more rapidly than VPA, while the effect of VPA was delayed. These differences might be exploited to design clinical trials specifically directed to AML subtypes characterized by constitutive HDAC activation. Our results led to include SAHA, an FDA-approved drug, among the HDACi active in the AML1/ETO-expressing AML cells.
我们分析了组蛋白去乙酰化酶抑制剂(HDACi)丁酸钠对表达 AML1/ETO 的 Kasumi-1 急性髓系白血病(AML)细胞的活性。我们还比较了 SAHA 与丙戊酸(VPA)的作用,VPA 是一种短链脂肪酸 HDACi。SAHA 和 VPA 诱导组蛋白 H3 和 H4 乙酰化、髓样分化和大量早期细胞凋亡。在不表达 AML1/ETO 的 AML 细胞系(如 NB4 或 THP-1)中,这两种药物均未确定后两种作用。与 VPA 相比,SAHA 在增加总 Kasumi-1 细胞裂解物中的 H3 和 H4 乙酰化方面更为迅速和有效,在诱导 H4K8、H4K12、H4K16 残基乙酰化方面比 VPA 更有效。在 AML1/ETO 转录沉默靶基因 IL3 的启动子上,与 VPA 相比,SAHA 也能更快地诱导总 H4、H4K5、H4K8 和 H3K27 乙酰化,而 VPA 在诱导总 H4、H4K12、H4K16 以及总 H3 乙酰化方面的作用在后期更为有效。与这些差异一致,SAHA 比 VPA 更快地诱导 IL3 mRNA 的表达,而 VPA 的作用则延迟。这些差异可能被用来设计专门针对 AML 亚型的临床试验,这些亚型的 AML 具有组成性的 HDAC 激活。我们的研究结果导致将 FDA 批准的药物 SAHA 纳入表达 AML1/ETO 的 AML 细胞中有效的 HDACi 之列。