CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, 164 West Xingang Road, Guangzhou, 510301, Guangdong, China.
University of Chinese Academy of Sciences, Beijing, 100049, China.
J Nat Prod. 2022 Aug 26;85(8):2071-2081. doi: 10.1021/acs.jnatprod.2c00473. Epub 2022 Aug 5.
Seven new decahydrofluorene-class alkaloids, pyrrospirones K-Q (-), together with six known analogues (-) were isolated from the marine-derived fungal strain sp. SCSIO 41512. Their structures were determined by extensive spectroscopic analysis, and their absolute configurations were established by single-crystal X-ray diffraction analysis and quantum chemical calculations of electronic circular dichroism spectra. Compounds and possess a novel decahydrofluorene-class alkaloid skeleton with a 6/5/6/8/5/6/13 and a 6/5/6/5/6/13 polycyclic system, respectively. Biologically, displayed significant inhibitory activity against protein tyrosine phosphatases CD45, TCPTP, SHP1, and PTP1B with IC values of 8.1-17.8 μM, and , , , -, , and showed antibacterial activity against six pathogens. Their structure-activity relationship is also discussed.
从海洋来源真菌菌株 sp. SCSIO 41512 中分离得到了 7 种新的十氢芴类生物碱吡咯螺酮 K-Q(-)，以及 6 种已知类似物(-)。通过广泛的光谱分析确定了它们的结构，并通过单晶 X 射线衍射分析和电子圆二色谱光谱的量子化学计算确定了它们的绝对构型。化合物 和 分别具有新颖的十氢芴类生物碱骨架，分别具有 6/5/6/8/5/6/13 和 6/5/6/5/6/13 多环系统。在生物学方面， 对蛋白酪氨酸磷酸酶 CD45、TCPTP、SHP1 和 PTP1B 具有显著的抑制活性，IC 值为 8.1-17.8 μM， 、 、 、 、 、 对六种病原体具有抗菌活性。还讨论了它们的构效关系。
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