Biomedical Industry Ph.D. Program, School of Life Sciences, National Yang Ming Chiao Tung University, Taipei 112304, Taiwan.
Department of Chemistry, Tamkang University, New Taipei City 251301, Taiwan.
Molecules. 2024 Apr 28;29(9):2041. doi: 10.3390/molecules29092041.
A series of flavanols were synthesized to assess their biological activity against human non-small cell lung cancer cells (A549). Among the sixteen synthesized compounds, it was observed that compounds (3.14 ± 0.29 µM) and (0.46 ± 0.02 µM) exhibited higher potency compared to 5-fluorouracil (5-Fu, 4.98 ± 0.41 µM), a clinical anticancer drug which was used as a positive control. Moreover, compound 6l (4'-bromoflavonol) markedly induced apoptosis of A549 cells through the mitochondrial- and caspase-3-dependent pathways. Consequently, compound might be developed as a candidate for treating or preventing lung cancer.
合成了一系列黄烷醇，以评估它们对人非小细胞肺癌细胞（A549）的生物活性。在所合成的十六种化合物中，观察到化合物 （3.14 ± 0.29 µM）和 （0.46 ± 0.02 µM）比临床抗癌药物 5-氟尿嘧啶（5-Fu，4.98 ± 0.41 µM）具有更高的活性，5-氟尿嘧啶被用作阳性对照。此外，化合物 6l（4'-溴黄酮醇）通过线粒体和 caspase-3 依赖性途径显著诱导 A549 细胞凋亡。因此，化合物 可能被开发为治疗或预防肺癌的候选药物。
