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Hyperelodiones A-C, monoterpenoid polyprenylated acylphoroglucinols from Hypericum elodeoides, induce cancer cells apoptosis by targeting RXRα
Phytochemistry ( IF 3.2 ) Pub Date : 2020-02-01 , DOI: 10.1016/j.phytochem.2019.112216 Daren Qiu 1 , Mi Zhou 1 , Junjie Chen 1 , Guanghui Wang 1 , Ting Lin 1 , Yujie Huang 1 , Furong Yu 1 , Rong Ding 1 , Cuiling Sun 1 , Wenjing Tian 1 , Haifeng Chen 1
Phytochemistry ( IF 3.2 ) Pub Date : 2020-02-01 , DOI: 10.1016/j.phytochem.2019.112216 Daren Qiu 1 , Mi Zhou 1 , Junjie Chen 1 , Guanghui Wang 1 , Ting Lin 1 , Yujie Huang 1 , Furong Yu 1 , Rong Ding 1 , Cuiling Sun 1 , Wenjing Tian 1 , Haifeng Chen 1
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Hyperelodiones A-C, three undescribed monoterpenoid polyprenylated acylphloroglucinols possessing 6/6/6 fused tricyclic core, were isolated from Hypericum elodeoides Choisy. Their gross structures were elucidated by HRESIMS and NMR data. The absolute configurations of hyperelodiones A-C were assigned by their calculated and compared electronic circular dichroism (ECD) spectra combined with their common biosynthetic origin. A fluorescence quenching assay suggested that hyperelodiones A-C could bind to RXRα-LBD, whereas hyperelodione C showed the strongest interaction with a KD of 12.81 μΜ. In addition, hyperelodiones A-C dose-dependently inhibited RXRα transactivation and the growth of HeLa and MCF-7 cells. Among them, hyperelodione C showed the most potent inhibitory activities and dose-dependent PARP cleavage. Molecular docking results suggested that hyperelodione C showed a different interaction mode compared with hyperelodione A and hyperelodione B. Thus, hyperelodione C can be considered as a promising lead compound for cancer therapy, which can bind to RXRα-LBD and induce HeLa and MCF-7 cell apoptosis.
中文翻译：
Hyperelodiones AC，来自金丝桃属植物的单萜类聚异戊二烯化酰基三聚葡萄糖，通过靶向 RXRα 诱导癌细胞凋亡
Hyperelodiones AC 是三种未描述的单萜类聚异戊二烯化酰基间苯三酚，具有 6/6/6 稠合三环核心，是从金丝桃属植物中分离出来的。通过 HRESIMS 和 NMR 数据阐明了它们的总体结构。hyperelodiones AC 的绝对构型是通过其计算和比较的电子圆二色性 (ECD) 光谱结合其共同的生物合成来源来分配的。荧光猝灭分析表明，hyperelodione AC 可以与 RXRα-LBD 结合，而 hyperelodione C 显示与 12.81 μM 的 KD 的最强相互作用。此外，hyperelodiones AC 剂量依赖性地抑制 RXRα 反式激活以及 HeLa 和 MCF-7 细胞的生长。其中，hyperelodione C 显示出最有效的抑制活性和剂量依赖性 PARP 裂解。
更新日期：2020-02-01
中文翻译：
Hyperelodiones AC，来自金丝桃属植物的单萜类聚异戊二烯化酰基三聚葡萄糖，通过靶向 RXRα 诱导癌细胞凋亡
Hyperelodiones AC 是三种未描述的单萜类聚异戊二烯化酰基间苯三酚，具有 6/6/6 稠合三环核心，是从金丝桃属植物中分离出来的。通过 HRESIMS 和 NMR 数据阐明了它们的总体结构。hyperelodiones AC 的绝对构型是通过其计算和比较的电子圆二色性 (ECD) 光谱结合其共同的生物合成来源来分配的。荧光猝灭分析表明，hyperelodione AC 可以与 RXRα-LBD 结合，而 hyperelodione C 显示与 12.81 μM 的 KD 的最强相互作用。此外，hyperelodiones AC 剂量依赖性地抑制 RXRα 反式激活以及 HeLa 和 MCF-7 细胞的生长。其中，hyperelodione C 显示出最有效的抑制活性和剂量依赖性 PARP 裂解。
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