School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China.
School of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China.
Int J Mol Sci. 2023 Oct 19;24(20):15375. doi: 10.3390/ijms242015375.
Natural products are irreplaceable reservoirs for cancer treatments. In this study, 12 phenanthrene compounds were extracted and isolated from . Each chemical structure was identified using comprehensive NMR analysis. All compounds were evaluated for their cytotoxic activities against five tumor cell lines, i.e., HeLa, MCF-7, SK-N-AS, Capan-2 and Hep G2. Compound 5, 1,5,6-trimethoxy-2,7-dihydroxyphenanthrene, displayed the most significant cytotoxic effect against HeLa and Hep G2 cells, with an IC of 0.42 and 0.20 μM. For Hela cells, further experiments demonstrated that compound 5 could obviously inhibit cell migration, block cell cycle in the G0/G1 phase and induce apoptosis. Expression measurements for p53 indicated that knock down of p53 by siRNA could mitigate the apoptosis induced by compound 5. Therefore, the compound 5 is a potential candidate drug for HeLa cells in cervical cancer.
天然产物是癌症治疗中不可替代的资源库。在这项研究中，从 中提取并分离出 12 种菲类化合物。通过综合 NMR 分析确定了每种化学结构。所有化合物都针对五种肿瘤细胞系（即 HeLa、MCF-7、SK-N-AS、Capan-2 和 Hep G2）进行了细胞毒性活性评估。化合物 5，1,5,6-三甲氧基-2,7-二羟基菲，对 HeLa 和 Hep G2 细胞表现出最显著的细胞毒性作用，IC 分别为 0.42 和 0.20 μM。对于 HeLa 细胞，进一步的实验表明，化合物 5 可以明显抑制细胞迁移，将细胞周期阻滞在 G0/G1 期并诱导细胞凋亡。p53 的表达测定表明，siRNA 敲低 p53 可以减轻化合物 5 诱导的细胞凋亡。因此，化合物 5 是宫颈癌 HeLa 细胞的潜在候选药物。
