Department of Clinical Laboratory, The Fourth Affiliated Hospital of Harbin Medical University, 37 Yiyuan Street, Harbin, Heilongjiang 150001, China.
Institute of Characteristic Medicinal Resource of Ethnic Minorities, Qujing Normal University, Qujing 655011, China.
Fitoterapia. 2018 Oct;130:259-264. doi: 10.1016/j.fitote.2018.09.013. Epub 2018 Sep 20.
The ethanol extract of the twigs and leaves of Kopsia hainanensis afforded six new aspidofractinine alkaloids, kopsiahainanins A-F (1-6), among which alkaloids 1 and 2 possessed a lactone bridge with novel regiochemistry. The structures of the isolated compounds were established based on 1D and 2D (HH COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated compounds were tested in vitro for cytotoxic activity against seven tumor cell lines and antibacterial activities against two Gram-positive bacteria and five Gram-negative bacteria. As a result, alkaloids 1 and 2 exhibited cytotoxic activities (IC values <20 μM) against all tested tumor cell lines and significant antibacterial properties (MIC values from 0.12 to 0.26 mM).
海南柯木中的枝和叶的乙醇提取物中得到了六个新的 Aspidofractinine 生物碱，柯沙海因 A-F（1-6），其中生物碱 1 和 2 具有内酯桥，具有新颖的区域化学。基于 1D 和 2D（HH COSY、HMQC 和 HMBC）NMR 光谱以及高分辨率质谱，确定了分离化合物的结构。对分离得到的化合物进行了体外抗肿瘤活性测试，对七种肿瘤细胞系进行了测试，对两种革兰氏阳性菌和五种革兰氏阴性菌进行了抗菌活性测试。结果表明，生物碱 1 和 2 对所有测试的肿瘤细胞系均具有细胞毒性活性（IC 值<20 μM），并且具有显著的抗菌性能（MIC 值为 0.12 至 0.26 mM）。
