Oncogenomic and Epigenetic Unit, Department of Research, Diagnosis and Innovative Technologies, IRCCS Regina Elena National Cancer Institute, Via Elio Chianesi, 53, 00144, Rome, Italy.
Department of Chemistry, University of Rome, "La Sapienza", Rome, Italy.
J Exp Clin Cancer Res. 2019 Aug 9;38(1):349. doi: 10.1186/s13046-019-1352-3.
Over the past decade, newly designed cancer therapies have not significantly improved the survival of patients diagnosed with Malignant Pleural Mesothelioma (MPM). Among a limited number of genes that are frequently mutated in MPM several of them encode proteins that belong to the HIPPO tumor suppressor pathway.
The anticancer effects of the top flower standardized extract of Filipendula vulgaris (Dropwort) were characterized in "in vitro" and "in vivo" models of MPM. At the molecular level, two "omic" approaches were used to investigate Dropwort anticancer mechanism of action: a metabolomic profiling and a phosphoarray analysis.
We found that Dropwort significantly reduced cell proliferation, viability, migration and in vivo tumor growth of MPM cell lines. Notably, Dropwort affected viability of tumor-initiating MPM cells and synergized with Cisplatin and Pemetrexed in vitro. Metabolomic profiling revealed that Dropwort treatment affected both glycolysis/tricarboxylic acid cycle as for the decreased consumption of glucose, pyruvate, succinate and acetate, and the lipid metabolism. We also document that Dropwort exerted its anticancer effects, at least partially, promoting YAP and TAZ protein ubiquitination.
Our findings reveal that Dropwort is a promising source of natural compound(s) for targeting the HIPPO pathway with chemo-preventive and anticancer implications for MPM management.
在过去的十年中,新设计的癌症疗法并没有显著改善恶性胸膜间皮瘤(MPM)患者的生存率。在 MPM 中频繁突变的少数基因中,有几个基因编码属于 HIPPO 肿瘤抑制途径的蛋白质。
采用“体外”和“体内”MPM 模型研究 Filipendula vulgaris(垂序商陆)的顶级花标准化提取物的抗癌作用。在分子水平上,采用两种“组学”方法研究垂序商陆的抗癌作用机制:代谢组学分析和磷酸阵列分析。
我们发现垂序商陆可显著降低 MPM 细胞系的细胞增殖、活力、迁移和体内肿瘤生长。值得注意的是,垂序商陆影响肿瘤起始 MPM 细胞的活力,并与顺铂和培美曲塞在体外协同作用。代谢组学分析表明,垂序商陆处理影响糖酵解/三羧酸循环,降低葡萄糖、丙酮酸、琥珀酸和醋酸盐的消耗,以及脂质代谢。我们还证明,垂序商陆通过促进 YAP 和 TAZ 蛋白泛素化发挥其抗癌作用。
我们的研究结果表明,垂序商陆是一种有前途的天然化合物来源,可靶向 HIPPO 途径,对 MPM 管理具有化学预防和抗癌意义。