从贯叶连翘中分离得到的具有细胞毒性的多聚异戊烯基间苯三酚衍生物调节 RXRα 的反式激活。
Cytotoxic polyprenylated phloroglucinol derivatives from Hypericum elodeoides Choisy modulating the transactivation of RXRα.
机构信息
Fujian Provincial Key Laboratory of Innovative Drug Target, School of Pharmaceutical Sciences, Xiamen University, Xiamen 361005, People's Republic of China; Sichuan Province College Key Laboratory of Structure-Specific Small Molecule Drugs, School of Pharmacy, Chengdu Medical College, Chengdu 610500, People's Republic of China.
Fujian Provincial Key Laboratory of Innovative Drug Target, School of Pharmaceutical Sciences, Xiamen University, Xiamen 361005, People's Republic of China.
出版信息
Bioorg Chem. 2021 Feb;107:104578. doi: 10.1016/j.bioorg.2020.104578. Epub 2020 Dec 23.
Hyperelodione D (1), an undescribed polyprenylated phloroglucinol derivative possessing 6/6/5/5 fused tetracyclic core, together with hyperelodiones E-F (2-3), two unreported analogues bearing 6/5/5 fused tricyclic structure, were isolated from Hypericum elodeoides Choisy. Their planar structures were elucidated by spectroscopic analysis (HRESIMS, 1D and 2D NMR) and their absolute configurations were determined by comparison of experimental and calculated ECD data. The cytotoxicity and retinoid X receptor-α (RXRα) related activities of the isolates were evaluated and the plausible biogenetic pathways of 1-3 were proposed.
从贯叶连翘（Hypericum elodeoides Choisy）中分离得到了一个未被描述的多聚异戊二烯基间苯三酚衍生物 hyperelodione D（1），它具有 6/6/5/5 融合四环核心，以及 hyperelodiones E-F（2-3），这两个未被报道的类似物具有 6/5/5 融合的三环结构。通过光谱分析（HRESIMS、1D 和 2D NMR）阐明了它们的平面结构，并通过比较实验和计算的 ECD 数据确定了它们的绝对构型。评估了这些分离物的细胞毒性和视黄醇 X 受体-α（RXRα）相关活性，并提出了 1-3 的可能生物合成途径。
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