Department of Surgery, Mackay Memorial Hospital, Taipei, Taiwan.
Institute of Traditional Medicine, School of Medicine, National Yang Ming Chiao Tung University, Taipei, Taiwan.
Mol Med. 2024 May 31;30(1):73. doi: 10.1186/s10020-024-00835-6.
Human malignant pleural mesothelioma (hMPM) is an aggressive, rare disease with a poor prognosis. Histologically, MPM is categorized into epithelioid, biphasic, and sarcomatoid subtypes, with the epithelioid subtype generally displaying a better response to treatment. Conversely, effective therapies for the non-epithelioid subtypes are limited. This study aimed to investigate the potential role of FK228, a histone deacetylase inhibitor, in the suppression of hMPM tumor growth. We conducted a comprehensive analysis of the histological and molecular characteristics of two MPM cell lines, CRL-5820 (epithelioid) and CRL-5946 (non-epithelioid). CRL-5946 cells and non-epithelioid patient-derived xenografted mice exhibited heightened growth rates compared to those with epithelioid MPM. Both CRL-5946 cells and non-epithelioid mice displayed a poor response to cisplatin. However, FK228 markedly inhibited the growth of both epithelioid and non-epithelioid tumor cells in vitro and in vivo. Cell cycle analysis revealed FK228-induced G1/S and mitotic arrest in MPM cells. Caspase inhibitor experiments demonstrated that FK228-triggered apoptosis occurred via a caspase-dependent pathway in CRL-5946 but not in CRL-5820 cells. Additionally, a cytokine array analysis showed that FK228 reduced the release of growth factors, including platelet-derived and vascular endothelial growth factors, specifically in CRL-5946 cells. These results indicate that FK228 exhibits therapeutic potential in MPM by inducing cytotoxicity and modulating the tumor microenvironment, potentially benefiting both epithelioid and non-epithelioid subtypes.
人恶性胸膜间皮瘤(hMPM)是一种侵袭性的罕见疾病,预后不良。组织学上,MPM 分为上皮型、双相型和肉瘤样型亚型,上皮型亚型通常对治疗反应更好。相反,对于非上皮型亚型,有效的治疗方法有限。本研究旨在探讨组蛋白去乙酰化酶抑制剂 FK228 抑制 hMPM 肿瘤生长的潜力。我们对两种 MPM 细胞系 CRL-5820(上皮型)和 CRL-5946(非上皮型)的组织学和分子特征进行了全面分析。与上皮型 MPM 相比,CRL-5946 细胞和非上皮型患者来源的异种移植小鼠的生长速度更快。CRL-5946 细胞和非上皮型小鼠对顺铂的反应较差。然而,FK228 显著抑制了上皮型和非上皮型肿瘤细胞在体外和体内的生长。细胞周期分析显示 FK228 诱导 MPM 细胞的 G1/S 和有丝分裂停滞。半胱天冬酶抑制剂实验表明,FK228 诱导的 CRL-5946 细胞凋亡是通过半胱天冬酶依赖性途径发生的,但在 CRL-5820 细胞中没有发生。此外,细胞因子阵列分析表明,FK228 减少了包括血小板衍生生长因子和血管内皮生长因子在内的生长因子的释放,特别是在 CRL-5946 细胞中。这些结果表明,FK228 通过诱导细胞毒性和调节肿瘤微环境,在 MPM 中具有治疗潜力,可能对上皮型和非上皮型亚型都有益。