Lecanicilliums A-F，来源于红树林沉积物真菌的硫代二酮哌嗪类生物碱。
Lecanicilliums A-F, Thiodiketopiperazine-Class Alkaloids from a Mangrove Sediment-Derived Fungus .
机构信息
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, Guangzhou 510301, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
出版信息
Mar Drugs. 2023 Oct 31;21(11):575. doi: 10.3390/md21110575.
Six new thiodiketopiperazine-class alkaloids lecanicilliums A-F were isolated from the mangrove sediment-derived fungus SCSIO41702, together with thirteen known analogues. Their structures were determined by spectroscopic analysis. The absolute configurations were determined by quantum chemical calculations. Electronic circular dichroism (ECD) spectra and the structure of Lecanicillium C were further confirmed by a single-crystal X-ray diffraction analysis. Lecanicillium A contained an unprecedented 6/5/6/5/7/6 cyclic system with a spirocyclic center at C-2'. Biologically, lecanicillium E, emethacin B, and versicolor A displayed significant cytotoxicity against human lung adenocarcinoma cell line H1975, with IC values of 7.216.9 μM, and lecanicillium E also showed antibacterial activity against four pathogens with MIC values of 1040 μg/mL. Their structure-activity relationship is also discussed.
从红树林沉积物来源的真菌 SCSIO41702 中分离得到了六种新的噻二酮哌嗪类生物碱 Lecanicillium A-F，以及十三种已知类似物。通过光谱分析确定了它们的结构。通过量子化学计算确定了绝对构型。通过单晶 X 射线衍射分析进一步证实了 Lecanicillium C 的电子圆二色性（ECD）光谱和结构。Lecanicillium A 含有一个前所未有的 6/5/6/5/7/6 环系，其螺环中心位于 C-2'。在生物活性方面，Lecanicillium E、emethacin B 和 versicolor A 对人肺腺癌细胞系 H1975 表现出显著的细胞毒性，IC 值为 7.216.9 μM，Lecanicillium E 还对四种病原体具有抗菌活性，MIC 值为 1040 μg/mL。还讨论了它们的构效关系。
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