García-Morales Pilar, Gómez-Martínez Angeles, Carrato Alfredo, Martínez-Lacaci Isabel, Barberá Víctor M, Soto José L, Carrasco-García Estefanía, Menéndez-Gutierrez María P, Castro-Galache María D, Ferragut José A, Saceda Miguel
Instituto de Biologia Molecular y Celular, Ed. Torregaitan, Universidad Miguel Hernandez, 03202 Elche (Alicante), Spain.
Mol Cancer Ther. 2005 Aug;4(8):1222-30. doi: 10.1158/1535-7163.MCT-04-0186.
The antitumor activity of the histone deacetylase inhibitors was tested in three well-characterized pancreatic adenocarcinoma cell lines, IMIM-PC-1, IMIM-PC-2, and RWP-1. These cell lines have been previously characterized in terms of their origin, the status of relevant molecular markers for this kind of tumor, resistance to other antineoplastic drugs, and expression of differentiation markers. In this study, we report that histone deacetylase inhibitors induce apoptosis in pancreatic cancer cell lines, independently of their intrinsic resistance to conventional antineoplastic agents. The histone deacetylase inhibitor-induced apoptosis is due to a serine protease-dependent and caspase-independent mechanism. Initially, histone deacetylase inhibitors increase Bax protein levels without affecting Bcl-2 levels. Consequently, the apoptosis-inducing factor (AIF) and Omi/HtrA2 are released from the mitochondria, with the subsequent induction of the apoptotic program. These phenomena require AIF relocalization into the nuclei to induce DNA fragmentation and a serine protease activity of Omi/HtrA2. These data, together with previous results from other cellular models bearing the multidrug resistance phenotype, suggest a possible role of the histone deacetylase inhibitors as antineoplastic agents for the treatment of human pancreatic adenocarcinoma.
在三种特征明确的胰腺腺癌细胞系IMIM-PC-1、IMIM-PC-2和RWP-1中测试了组蛋白脱乙酰酶抑制剂的抗肿瘤活性。这些细胞系先前已根据其来源、此类肿瘤相关分子标志物的状态、对其他抗肿瘤药物的耐药性以及分化标志物的表达进行了表征。在本研究中,我们报告组蛋白脱乙酰酶抑制剂可诱导胰腺癌细胞系凋亡,而与它们对传统抗肿瘤药物的固有耐药性无关。组蛋白脱乙酰酶抑制剂诱导的凋亡是由于一种丝氨酸蛋白酶依赖性且不依赖于半胱天冬酶的机制。最初,组蛋白脱乙酰酶抑制剂增加Bax蛋白水平而不影响Bcl-2水平。因此,凋亡诱导因子(AIF)和Omi/HtrA2从线粒体释放,随后诱导凋亡程序。这些现象需要AIF重新定位到细胞核中以诱导DNA片段化以及Omi/HtrA2的丝氨酸蛋白酶活性。这些数据,连同先前来自其他具有多药耐药表型的细胞模型的结果,表明组蛋白脱乙酰酶抑制剂作为治疗人类胰腺腺癌的抗肿瘤药物可能发挥作用。