Department of General Practice, The Second Hospital of DaLian Medical University, DaLian 116023, China.
Department of Experimental Medicine, Northern Hospital, Shenyang 110016, China.
Fitoterapia. 2018 Sep;129:145-149. doi: 10.1016/j.fitote.2018.06.017. Epub 2018 Jun 21.
A chemical investigation on the 80% EtOH extract of the aerial parts of Kopsia fruticosa led to five new indole alkaloids, kopsifolines G-K (1-5), and one known alkaloid, kopsifoline A (6). Structural elucidation of all the compounds were performed by spectral methods such as 1D and 2D (H-H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated components were evaluated in vitro for cytotoxic activities against seven tumor cell lines, antimicrobial activities against two Gram-positive bacteria and five Gram-negative bacteria, and antifungal activities against five pathogens. As a result, alkaloids 3-5 exhibited some cytotoxicity against all of seven tested tumor cell lines (HS-1, HS-4, SCL-1, A431, BGC-823, MCF-7, and W480) with IC values of 11.8-13.8, 10.3-12.5, and 7.3-9.5 μM, respectively. Alkaloids 3-5 also possessed significant antimicrobial and antifungal activities which was reported for the first time for the alkaloids isolated from Kopsia genus.
对小钩叶藤（Kopsia fruticosa）地上部分 80%乙醇提取物进行化学研究，得到了五个新的吲哚生物碱，分别命名为 kopsifolines G-K（1-5），以及一个已知生物碱 kopsifoline A（6）。通过光谱方法，如 1D 和 2D（H-H COSY、HMQC 和 HMBC）NMR 光谱，以及高分辨质谱，对所有化合物的结构进行了阐明。对分离得到的化合物进行了体外细胞毒性实验，以评估其对七种肿瘤细胞系的活性、对两种革兰氏阳性菌和五种革兰氏阴性菌的抗菌活性，以及对五种病原体的抗真菌活性。结果表明，生物碱 3-5 对所有七种测试的肿瘤细胞系（HS-1、HS-4、SCL-1、A431、BGC-823、MCF-7 和 W480）均表现出一定的细胞毒性，IC 值分别为 11.8-13.8、10.3-12.5 和 7.3-9.5µM。生物碱 3-5 还具有显著的抗菌和抗真菌活性，这是首次报道从小钩叶藤属中分离得到的生物碱具有这些活性。
