Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University, Universitätsstraße 1, 40225 Düsseldorf, Germany.
Department of Marine Biology, Faculty of Marine Sciences, Tarbiat Modares University, 46414-356 Noor, Iran.
Mar Drugs. 2017 Nov 11;15(11):356. doi: 10.3390/md15110356.
Three new 2-methoxy acetylenic acids (1-3) and a known derivative (4), in addition to three new natural pyrazole alkaloids (5-7) were isolated from an Indonesian marine sponge of the genus Cinachyrella. Compounds 5 and 6 have previously been reported as synthetic compounds. The structures of the new compounds were established on the basis of one- and two-dimensional NMR spectroscopy as well as by mass spectrometric data. The absolute configuration of the new acetylenic acid derivatives (1-3) was established by ECD spectroscopy. All isolated compounds were evaluated for their cytotoxicity against L5178Y mouse lymphoma cells. Compounds 1-4 exhibited strong activity with an IC50 value of 0.3 µM. A plausible biosynthetic pathway for the pyrazole metabolites 5-7 is proposed.
从印度尼西亚 cinachyrella 属海洋海绵中分离得到三种新的 2-甲氧基炔酸(1-3)和一种已知衍生物(4),以及三种新的天然吡唑生物碱(5-7)。化合物 5 和 6 以前曾被报道为合成化合物。新化合物的结构是基于一维和二维 NMR 光谱以及质谱数据确定的。新的炔酸衍生物(1-3)的绝对构型是通过 ECD 光谱确定的。所有分离得到的化合物都进行了对 L5178Y 小鼠淋巴瘤细胞的细胞毒性评估。化合物 1-4 表现出很强的活性,IC50 值为 0.3 μM。提出了吡唑代谢物 5-7 的可能生物合成途径。