Verruculosins A-B, New Oligophenalenone Dimers from the Soft Coral-Derived Fungus Talaromyces verruculosus
Verruculosins A-B, New Oligophenalenone Dimers from the Soft Coral-Derived Fungus Talaromyces verruculosus
复制标题
Verruculosins A–B，来自软珊瑚衍生真菌 Talaromyces verruculosus 的新型寡苯烯酮二聚体
DOI：
10.3390/md17090516
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发表时间：
2019-09-01
期刊：
影响因子：
5.4
通讯作者：
Wang, Zhaokai
中科院分区：
文献类型：
--
作者：
Wang, Minghui;Yang, Longhe;Wang, Zhaokai
为了发现新的生物活性抗肿瘤先导化合物，我们选择了特异性酪氨酸磷酸酶CDC25B和Erb家族受体EGFR作为药物筛选靶点。这项工作导致了软珊瑚衍生真菌疣状藻的研究，并鉴定了两种新的寡酚烯酮二聚体，疣状藻素A-B(1-2)，以及三种已知的类似物，bacillisporin F (3), duclauxin(4)和xenoclausin(5)。化合物1是低邻苯二烯酮二聚体的第一个结构，具有独特的八环骨架。根据光谱数据、x射线晶体学、旋光性、电子圆二色性（ECD）分析和核磁共振（NMR）计算，阐明了新化合物的详细结构和绝对构型。其中化合物1、3、5对CDC25B表现出适度的抑制活性，IC50值分别为0.38±0.03、0.40±0.02、0.26±0.06µM。
In an effort to discover new bioactive anti-tumor lead compounds, a specific tyrosine phosphatase CDC25B and an Erb family receptor EGFR were selected as drug screening targets. This work led to the investigation of the soft coral-derived fungus Talaromyces verruculosus and identification of two new oligophenalenone dimers, verruculosins A–B (1–2), along with three known analogues, bacillisporin F (3), duclauxin (4), and xenoclauxin (5). Compound 1 was the first structure of the oligophenalenone dimer possessing a unique octacyclic skeleton. The detailed structures and absolute configurations of the new compounds were elucidated on the basis of spectroscopic data, X-ray crystallography, optical rotation, Electronic Circular Dichroism (ECD) analysis, and nuclear magnetic resonance (NMR) calculations. Among which, compounds 1, 3, and 5 exhibited modest inhibitory activity against CDC25B with IC50 values of 0.38 ± 0.03, 0.40 ± 0.02, and 0.26 ± 0.06 µM, respectively.