Madrid Alejandro, Cardile Venera, González César, Montenegro Ivan, Villena Joan, Caggia Silvia, Graziano Adriana, Russo Alessandra
Departamento de Química, Facultad de Ciencias Naturales y Exactas, Universidad de Playa Ancha, Avda. Leopoldo Carvallo 270, Playa Ancha, 2340000 Valparaíso, Chile.
Department of Biomedical Sciences, University of Catania, V. le A. Doria 6, 95125 Catania, Italy.
Int J Mol Sci. 2015 Apr 9;16(4):7944-59. doi: 10.3390/ijms16047944.
With the aim of identifying novel agents with antigrowth and pro-apoptotic activity on melanoma cancer, the present study was undertaken to investigate the biological activity of the resinous exudate of aerial parts from Psoralea glandulosa, and its active components (bakuchiol (1), 3-hydroxy-bakuchiol (2) and 12-hydroxy-iso-bakuchiol (3)) against melanoma cells (A2058). In addition, the effect in cancer cells of bakuchiol acetate (4), a semi-synthetic derivative of bakuchiol, was examined. The results obtained show that the resinous exudate inhibited the growth of cancer cells with IC50 value of 10.5 μg/mL after 48 h of treatment, while, for pure compounds, the most active was the semi-synthetic compound 4. Our data also demonstrate that resin is able to induce apoptotic cell death, which could be related to an overall action of the meroterpenes present. In addition, our data seem to indicate that the apoptosis correlated to the tested products appears, at least in part, to be associated with an increase of reactive oxygen species (ROS) production. In summary, our study provides the first evidence that P. glandulosa may be considered a source of useful molecules in the development of analogues with more potent efficacy against melanoma cells.
为了鉴定对黑色素瘤具有抗生长和促凋亡活性的新型药物，本研究旨在调查腺叶补骨脂地上部分树脂状渗出物及其活性成分（补骨脂酚（1）、3-羟基补骨脂酚（2）和12-羟基异补骨脂酚（3））对黑色素瘤细胞（A2058）的生物学活性。此外，还检测了补骨脂酚乙酸酯（4）（补骨脂酚的半合成衍生物）对癌细胞的作用。所得结果表明，树脂状渗出物在处理48小时后抑制癌细胞生长，IC50值为10.5μg/mL，而对于纯化合物，活性最强的是半合成化合物4。我们的数据还表明，该树脂能够诱导凋亡性细胞死亡，这可能与存在的杂萜类化合物的整体作用有关。此外，我们的数据似乎表明，与测试产品相关的凋亡至少部分与活性氧（ROS）生成增加有关。总之，我们的研究提供了首个证据，表明腺叶补骨脂可被视为开发对黑色素瘤细胞具有更强效力类似物的有用分子来源。
