Di Martile Marta, Garzoli Stefania, Sabatino Manuela, Valentini Elisabetta, D'Aguanno Simona, Ragno Rino, Del Bufalo Donatella
Preclinical Models and New Therapeutic Agents Unit, IRCCS Regina Elena National Cancer Institute, Via Elio Chianesi 53, Rome, Italy.
Rome Center for Molecular Design, Department of Drug Chemistry and Technology, Sapienza University, Piazzale Aldo Moro 5, Rome, Italy.
Cell Death Discov. 2021 May 31;7(1):127. doi: 10.1038/s41420-021-00510-3.
Essential oils (EOs) have been recently emerging for their promising biological activities in preventing tumorigenesis or progression of different tumor histotypes, including melanoma. In this study, we investigated the antitumor activity of a panel of EOs in different tumor models. The ability of Melaleuca alternifolia (tea tree oil) and its main component, terpinen-4-ol, to sensitize the target therapy currently used for melanoma treatment was also assessed. Our results demonstrated that EOs differently affect the viability of human cancer cells and led us to select six EOs effective in melanoma and lung cancer cells, without toxic effects in human fibroblasts. When combined with dabrafenib and/or trametinib, Melaleuca alternifolia synergistically reduced the viability of melanoma cells by activating apoptosis. Through machine learning classification modeling, α-terpineol, tepinolene, and terpinen-4-ol, three components of Melaleuca alternifolia, were identified as the most likely relevant components responsible for the EO's antitumor effect. Among them, terpinen-4-ol was recognized as the Melaleuca alternifolia component responsible for its antitumor and proapoptotic activity. Overall, our study holds promise for further analysis of EOs as new anticancer agents and supports the rationale for their use to improve target therapy response in melanoma.
精油（EOs）因其在预防不同肿瘤组织类型（包括黑色素瘤）的肿瘤发生或进展方面具有有前景的生物活性而最近崭露头角。在本研究中，我们调查了一组精油在不同肿瘤模型中的抗肿瘤活性。还评估了互叶白千层（茶树油）及其主要成分萜品-4-醇使目前用于黑色素瘤治疗的靶向疗法敏感化的能力。我们的结果表明，精油对人类癌细胞的活力有不同影响，并促使我们选择了六种对黑色素瘤细胞和肺癌细胞有效的精油，且对人类成纤维细胞无毒性作用。当与达拉非尼和/或曲美替尼联合使用时，互叶白千层通过激活凋亡协同降低了黑色素瘤细胞的活力。通过机器学习分类建模，互叶白千层的三种成分α-萜品醇、萜品烯和萜品-4-醇被确定为最有可能与精油的抗肿瘤作用相关的成分。其中，萜品-4-醇被认为是互叶白千层中负责其抗肿瘤和促凋亡活性的成分。总体而言，我们的研究有望进一步分析精油作为新型抗癌剂，并支持其用于改善黑色素瘤靶向治疗反应的基本原理。
Zotero 插件
