Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8553, Japan.
Department of Protozoology, Institute of Tropical Medicine (NEKKEN), Nagasaki University, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan.
Molecules. 2023 Jun 11;28(12):4696. doi: 10.3390/molecules28124696.
The Asteraceae family is a promising source of bioactive compounds, such as the famous Asteraceae plants (pyrethrin) and (artemisinin). As a result of our series of phytochemical studies of the subtropical plants, two novel sesquiterpenes, named crossoseamines A and B in this study ( and , respectively), one undescribed coumarin-glucoside (), and eighteen known compounds (-) were isolated from the aerial part of (Asteraceae). The structures of isolated compounds were elucidated by spectroscopic methods, including 1D and 2D NMR experiments (H, C, DEPT, COSY, HSQC, HMBC, and NOESY), IR spectrum, circular dichroism spectrum (CD), and high-resolution electrospray ionization-mass spectrometry (HR-ESI-MS). All isolated compounds were evaluated for their cytotoxic activities against , , ( and ), and human lung cancer cell line A549 because of the high demand for the discovery of new drug leads to overcome the present side effects and emerging drug-resistant strains. As a result, the new compounds ( and ) showed significant activities against A549 (IC, : 3.3 ± 0.3; : 12.3 ± 1.0 μg/mL), (IC, : 6.9 ± 0.6; : 24.9 ± 2.2 μg/mL), and (IC, : 12.1 ± 1.1; : 15.6 ± 1.2 μg/mL).
菊科是生物活性化合物的有前途的来源，例如著名的菊科植物 （除虫菊）和 （青蒿素）。由于我们对亚热带植物的一系列植物化学研究，从 （菊科）的地上部分分离得到了两个新型倍半萜，在本研究中分别命名为交叉胺 A 和 B（和 ）、一个未描述的香豆素-葡萄糖苷（）和十八个已知化合物（-）。通过包括 1D 和 2D NMR 实验（H、C、DEPT、COSY、HSQC、HMBC 和 NOESY）、IR 光谱、圆二色光谱（CD）和高分辨率电喷雾电离质谱（HR-ESI-MS）等光谱方法阐明了分离化合物的结构。由于对发现新的药物先导物以克服当前的副作用和新兴的耐药菌株的需求很高，因此评估了所有分离化合物对 、 、 （和 ）和人肺癌细胞系 A549 的细胞毒性活性。结果，新化合物（和 ）对 A549 （IC ：3.3 ± 0.3；：12.3 ± 1.0 μg/mL）、 （IC ：6.9 ± 0.6；：24.9 ± 2.2 μg/mL）和 （IC ：12.1 ± 1.1；：15.6 ± 1.2 μg/mL）显示出显著的活性。
