Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-Ku, Hiroshima 734-8553, Japan.
Graduate School of Pharmacy, Yasuda Women's University, 6-13-1 Yasuhigashi, Asaminami-Ku, Hiroshima 731-0153, Japan.
Molecules. 2023 Dec 15;28(24):8108. doi: 10.3390/molecules28248108.
Previously, we reported two cytotoxic -santonin-amino acid conjugates isolated from the EtOAc layer of . However, a further phytochemical investigation seems to be required because of the few reports of similar derivatives. In this study, we targeted the 1-BuOH layer, which resulted in the isolation of seven new -santonin derivatives (-) together with ten known compounds (-). The structures of - were elucidated based on spectroscopic methods, including 1D and 2D NMR experiments (H, C, DEPT, COSY, HSQC, and HMBC), IR spectrum, and high-resolution electrospray ionization-mass spectrometry (HR-ESI-MS). The stereochemistry of new compounds was confirmed by NOESY and ECD calculations. All isolated compounds were evaluated by in vitro experiments for their anti-proliferative activities against , human lung cancer cell line A549, and Vero cells. As a result, most of the -santonin derivatives, especially -, showed significant cytotoxicity against with a lower IC than the positive control we used (miltefosine).
此前，我们从. 的 EtOAc 层中分离出两种细胞毒性 - 青蒿素- 氨基酸缀合物。然而，由于类似衍生物的报道很少，似乎需要进一步进行植物化学研究。在这项研究中，我们针对 1-BuOH 层进行了研究，结果分离出了七种新的 - 青蒿素衍生物 (-) 以及十种已知化合物 (-)。通过包括 1D 和 2D NMR 实验 (H、C、DEPT、COSY、HSQC 和 HMBC)、IR 光谱和高分辨率电喷雾电离质谱 (HR-ESI-MS) 在内的光谱方法阐明了 - 的结构。新化合物的立体化学通过 NOESY 和 ECD 计算得到确认。通过体外实验评估了所有分离出的化合物对 、人肺癌细胞系 A549 和 Vero 细胞的抗增殖活性。结果表明，大多数 - 青蒿素衍生物，特别是 - ，对 表现出显著的细胞毒性，其 IC 低于我们使用的阳性对照 (米替福新)。
