PI3K-inhibitory new anthraquinone-xanthone heterodimers from a deep-sea Epichloe sp. SCSIO 41042
文献类型：期刊论文
| 作者 | Song, Ying-Ying4; Pang, Xiao-Yan3; Yang, De-Hua2; Gao, Cheng-Hai4; Wang, Jun-Feng1,3; Liu, Yong-Hong1,3 |
| 刊名 | FITOTERAPIA
 |
| 出版日期 | 2025-12-01 |
| 卷号 | 187页码:8 |
| 关键词 | Anthraquinone PI3K inhibition activity Deep-sea derived fungus |
| ISSN号 | 0367-326X |
| DOI | 10.1016/j.fitote.2025.106893 |
| 通讯作者 | Gao, Cheng-Hai(gaoch@gxtcmu.edu.cn) ; Wang, Jun-Feng(wangjunfeng@scsio.ac.cn) ; Liu, Yong-Hong(yonghongliu@scsio.ac.cn) |
| 英文摘要 | Two new xanthone-anthraquinone heterodimers (1 and 2), and eleven known anthraquinones (3-13) were isolated from the deep-sea derived Epichloe sp. SCSIO 41042 fermented on rice medium. Structurally, compounds 1-5 feature a unique bicyclo[3.2.2]nonane core formed through dual C-C linkages. Their structures and absolute configurations were determined by spectroscopic analyses and calculated electronic circular dichroism (ECD). Molecular docking was performed to characterize the affinity of anthraquinones for phosphatidylinositol 3-kinase (PI3K), identifying those with significant anti-PI3K activity. Active compounds were subsequently profiled via homogeneous time-resolved fluorescence (HTRF) assay for PI3K inhibition, followed by binding affinity validation using surface plasmon resonance (SPR). Activity assay revealed that 2 significantly inhibited both PI3K alpha WT and PI3K alpha H1047R enzymes, with IC50 values of 2.00 and 3.42 mu M, respectively. Further SPR analysis demonstrated a moderate binding affinity between 2 and PI3K, with a KD of 12.7 mu M. |
| WOS关键词 | FUNGUS ; ACREMONIDINS ; DISCOVERY ; INHIBITOR |
| 资助项目 | Middle-Aged Teachers Scientific Research Project of Guangxi Universities[2025KY0396] ; National Natural Science Foundation of China[42376124] ; National Natural Science Foundation of China[41776169] ; Hainan Provincial Natural Science Foundation of China[823CXTD393] ; Guangzhou Science and Technology Project[2024B03J0001] ; Department of Natural Resources of the Guangdong Province[[2024] 28] ; Key-Area Research and Development Program of Guangdong Province[2023B1111050008] ; Key Science and Technology Plan Projects in Nansha District[2023ZD010] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001587450000002 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/321636]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Gao, Cheng-Hai; Wang, Jun-Feng; Liu, Yong-Hong |
| 作者单位 | 1.Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drugs Screening, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, South China Sea Inst Oceanol, Guangdong Key Lab Marine Mat Med, State Key Lab Trop Oceanog, Guangzhou 510301, Peoples R China 4.Guangxi Univ Chinese Med, Inst Marine Drugs, Guangxi Key Lab Marine Drugs, Nanning 530200, Peoples R China |
| 推荐引用方式 GB/T 7714 | Song, Ying-Ying,Pang, Xiao-Yan,Yang, De-Hua,et al. PI3K-inhibitory new anthraquinone-xanthone heterodimers from a deep-sea Epichloe sp. SCSIO 41042[J]. FITOTERAPIA,2025,187:8. |
| APA | Song, Ying-Ying,Pang, Xiao-Yan,Yang, De-Hua,Gao, Cheng-Hai,Wang, Jun-Feng,&Liu, Yong-Hong.(2025).PI3K-inhibitory new anthraquinone-xanthone heterodimers from a deep-sea Epichloe sp. SCSIO 41042.FITOTERAPIA,187,8. |
| MLA | Song, Ying-Ying,et al."PI3K-inhibitory new anthraquinone-xanthone heterodimers from a deep-sea Epichloe sp. SCSIO 41042".FITOTERAPIA 187(2025):8. |
入库方式： OAI收割
来源：上海药物研究所
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