酪胺酰-DNA磷酸二酯酶1(TDP1)是目前公认的潜在的肿瘤治疗新靶点, 但未见有相关药物上市或进入临床研究报道。为了寻找潜在的TDP1抑制剂, 本文采用大米培养基对海洋本草软珊瑚共附生真菌Aspergillus terreus EGF7-0-1进行规模发酵, 运用多种色谱技术(TLC, CC和HPLC等)对发酵产物进行分离纯化, 通过多种光谱学方法(NMR, HR-ESI-MS, ORD等), 并结合文献数据比对确定了8个γ-芳环丁烯内酯类化合物：butyrolactones I-V(1~5)、aspernolide E(6)、asperteretal D(7)和 terrusnolide A(8)。首次对化合物1~8进行体外抑制TDP1活性测试, 均无抑制作用。本研究为TDP1抑制剂的发现提供借鉴。

Tyrosyl-DNA phosphodiesterase 1 (TDP1) is currently recognized as a potential target for cancer treatment. However, no related drugs have been marketed or reported in clinical research. In order to discover potential TDP1 inhibitors, the soft coral-associated symbiotic and epiphytic fungi Aspergillus terreus EGF7-0-1 were fermented with rice media. The secondary metabolites were isolated with the various chromatography technologies (such as TLC, CC, HPLC, etc.) to afford eight γ-aromatic butenolide lignans. Based on NMR, HR-ESI-MS, OR and compare with the literature, their structures were determined as butyrolactones I~V (1~5), aspernolide E (6), asperteretal D (7) and terrusnolide A (8). In this study, the inhibitory activity of these compounds against tyrosyl -DNA phosphodiesterase 1 (TDP1) in vitro was studied for the first time, but it was unfortunate that compounds 1~8 did not show any inhibitory abilities against TDP1. This study provides theoretical data for the discovery of TDP1 inhibitors.