School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Xiamen Institute for Food and Drug Quality Control, Xiamen 3161012, People's Republic of China.
Bioorg Chem. 2018 Apr;77:619-624. doi: 10.1016/j.bioorg.2018.02.017. Epub 2018 Feb 16.
One new 1,3-diphenylpropane (1) together with six known analogues (2-7) were firstly isolated from the stem and root bark of Daphne giraldii. Their structures were determined by comprehensive NMR and HRESIMS spectroscopic data analyses. All the isolates were evaluated for their cytotoxicity against two hepatocellular carcinoma cell lines (HepG2 and Hep3B). Among them, compound 5 showed the most significant cytotoxicity against Hep3B cells, with an IC value of 17.21 μM. A further study demonstrated that 5 obviously induced apoptotic cell death as well as the inactivation of nuclear factor kappa B p65 (NF-κB p65) in Hep3B cells. In addition, BAY 11-7082 (BAY), a NF-кB inhibitor, was used to determine the role of NF-кB signaling in 5-treated Hep3B cells. The results suggested that BAY could enhance 5-induced apoptosis of Hep3B cells. In conclusion, the data provided that 5 might be a potential candidate for the treatment of hepatocellular carcinoma through NF-κB inhibition.
首次从瑞香科芫花属植物芫花的茎和根皮中分离得到 1 个新的 1,3-二苯基丙烷（1）和 6 个已知类似物（2-7）。通过综合 NMR 和 HRESIMS 光谱数据分析确定了它们的结构。所有分离物均针对两种肝癌细胞系（HepG2 和 Hep3B）进行了细胞毒性评估。其中，化合物 5 对 Hep3B 细胞的细胞毒性最为显著，IC 值为 17.21μM。进一步的研究表明，5 明显诱导 Hep3B 细胞凋亡和核因子 kappa B p65（NF-κB p65）失活。此外，还使用 NF-κB 抑制剂 BAY 11-7082（BAY）来确定 NF-κB 信号通路在 5 处理的 Hep3B 细胞中的作用。结果表明，BAY 可以增强 5 诱导的 Hep3B 细胞凋亡。综上所述，这些数据表明 5 可能通过抑制 NF-κB 成为治疗肝癌的潜在候选药物。
