School of Chemistry and Chemical Engineering, Anhui University of Technology, Ma'anshan, 243002, P. R. China.
College of Life Sciences, Shanghai Normal University, Shanghai, P. R. China.
Chem Biodivers. 2024 Apr;21(4):e202400288. doi: 10.1002/cbdv.202400288. Epub 2024 Mar 15.
Triple-negative breast cancer (TNBC) is characterized by strong invasiveness, high relapse rates, and poor overall survival. It occurs in approximately 15-20 % of all breast cancer cases. Natural compounds are a promising option for managing breast cancer. ent-8(14),15-Pimaradiene-2β,19-diol (JXE-23), is a pimaradiene isolated from the fern Aleuritopteris albofusca. However, the effects and molecular mechanisms of JXE-23 on cancer cells are still unknown. Thus, this study was designed to determine the potential of JXE-23 for its anticancer properties in TNBC cells. JXE-23 was evaluated for its antiproliferative activity in vitro against human breast cancer cell lines, and showed selectively cytotoxic activity against MDA-MB-468, an EGFR-overexpressing TNBC cancer cell line, with an IC value of 1.17±0.04 μM. Moreover, mechanistic investigations indicated that JXE-23 was significantly capable of inhibiting cell proliferation and viability in MDA-MB-468 cells. In addition, JXE-23 exerted an anticancer effect against MDA-MB-468 cells via restraining cell migration in a dose-dependent mode. Moreover, after treatment with JXE-23, the protein expressions of pEGFR, pERK, pAkt and p-p70 were significantly reduced in MDA-MB-468 cells. The results underscored that JXE-23 could be a potential lead compound for the treatment of EGFR-overexpressing TNBC cells.
三阴性乳腺癌（TNBC）的特点是侵袭性强、复发率高、总体生存率低。它发生在大约 15-20%的所有乳腺癌病例中。天然化合物是治疗乳腺癌的一种很有前途的选择。ent-8(14),15- 松烷二烯-2β,19-二醇（JXE-23）是一种从肾蕨 Aleuritopteris albofusca 中分离出的松香烷二烯。然而，JXE-23 对癌细胞的作用和分子机制尚不清楚。因此，本研究旨在确定 JXE-23 在 TNBC 细胞中的抗癌特性。在体外评估 JXE-23 对人乳腺癌细胞系的增殖抑制活性，结果表明 JXE-23 对 EGFR 过表达的 TNBC 癌细胞 MDA-MB-468 具有选择性细胞毒性作用，IC 值为 1.17±0.04 μM。此外，机制研究表明，JXE-23 能够显著抑制 MDA-MB-468 细胞的增殖和活力。此外，JXE-23 以剂量依赖性方式抑制 MDA-MB-468 细胞迁移，从而发挥抗癌作用。此外，用 JXE-23 处理后，MDA-MB-468 细胞中 pEGFR、pERK、pAkt 和 p-p70 的蛋白表达明显降低。结果表明，JXE-23 可能是治疗 EGFR 过表达的 TNBC 细胞的潜在先导化合物。
