Gancochlearols E - I, meroterpenoids from Ganoderma cochlear against COX-2 and triple negative breast cancer cells and the absolute configuration assignment of ganomycin K
Gancochlearols E - I, meroterpenoids from Ganoderma cochlear against COX-2 and triple negative breast cancer cells and the absolute configuration assignment of ganomycin K
复制标题
Gancochlearols E – I，灵芝耳蜗中的类萜对 COX-2 和三阴性乳腺癌细胞的作用以及 ganomycin K 的绝对构型分配
DOI：
10.1016/j.bioorg.2021.104706
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发表时间：
2021-02-16
影响因子：
5.1
通讯作者：
Cheng, Yong-Xian
中科院分区：
文献类型：
--
作者：
Li, Yan-Peng;Jiang, Xiao-Ting;Cheng, Yong-Xian
从G. cochlear 子实体中分离得到5 种新的类萜化合物gancochlearols E - I (1, 3-6) 和1 种化合物ganomycin K (2)。它们的结构通过一维和二维核磁共振、质谱和圆二色分析确定。采用Rh-2(OCOCF3)(4)诱导的ECD法明确1和2中仲醇的绝对构型。生化评价表明，所有分离株在体外均显着抑制COX-2酶，IC50值范围为1.03 μM至2.71 μM。进一步的细胞分析表明(+)-3和(-)-6可通过阻碍三阴性乳腺癌(TNBC)细胞的转移表型。上皮间质转化（EMT）。
Five new meroterpenoids, gancochlearols E - I (1, 3-6), and one compound ganomycin K (2) were isolated from the fruiting bodies of G. cochlear. Their structures were assigned by 1D and 2D NMR, MS, and CD analysis. Rh-2(OCOCF3)(4)-induced ECD method was used to clarify the absolute configuration of secondary alcohol in 1 and 2. Biochemical evaluation showed that all the isolates significantly inhibit COX-2 enzyme in vitro with the IC50 values range from 1.03 mu M to 2.71 mu M. Further cellular assay revealed that (+)-3 and (-)-6 could suppress metastatic phenotype of triple-negative breast cancer (TNBC) cells via impeding the epithelial-mesenchymal transition (EMT).