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两种新型二萜类杂二聚体，Bisebracteolasin A 和 B，来自大戟属Ebracteolata Hayata，以及 Bisebracteolasin A 的癌症化疗潜力。

Two novel diterpenoid heterodimers, Bisebracteolasins A and B, from Euphorbia ebracteolata Hayata, and the cancer chemotherapeutic potential of Bisebracteolasin A.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650204, P.R. China.

Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, P.R. China.

出版信息

Sci Rep. 2017 Nov 6;7(1):14507. doi: 10.1038/s41598-017-14637-w.

DOI:10.1038/s41598-017-14637-w
PMID:29109538
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5674023/
Abstract

Rare ent-abietane-rosane diterpenoid heterodimers, Bisebracteolasins A and B (1 and 2, respectively), were isolated from the roots of Euphorbia ebracteolata Hayata. Their structures and absolute configurations were elucidated from spectroscopic data and X-ray diffraction analysis. Compounds 1 and 2 exhibited moderate cytotoxic effects against five cancer cell lines. Compound 1 showed more effective antiproliferative activities against human tumour cells, HL-60 and SMMC-7721, with IC values of 2.61 and 4.08 μM, respectively, than 2. Both compounds 1 and 2 inhibit the colorectal cancer stem cell line P6C with IC values of 16.48 and 34.76 μM, respectively. Moreover, preliminary biological tests showed compound 1 exhibited inhibitory activity towards tumoursphere formation and migration of the P6C cell line. Overall, we identified two novel diterpenoid heterodimers, and Bisebracteolasin A exhibits therapeutic potential in impeding tumour growth and metastatic ability of cancer stem cells.

摘要

从大戟属植物Ebracteolata Hayata 的根部分离得到了两种罕见的 abietane-rosane 二萜杂二聚体，Bisebracteolasin A 和 B（分别为 1 和 2）。根据光谱数据和 X 射线衍射分析确定了它们的结构和绝对构型。化合物 1 和 2 对五种癌细胞系表现出中等的细胞毒性作用。化合物 1 对人肿瘤细胞 HL-60 和 SMMC-7721 的增殖抑制活性更为有效，IC 值分别为 2.61 和 4.08 μM，优于 2。两种化合物 1 和 2 对结直肠癌细胞系 P6C 的抑制活性 IC 值分别为 16.48 和 34.76 μM。此外，初步的生物学测试表明，化合物 1 对 P6C 细胞系的肿瘤球形成和迁移具有抑制作用。总之，我们鉴定了两种新型二萜杂二聚体，Bisebracteolasin A 具有阻碍肿瘤生长和抑制癌症干细胞转移能力的治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/ae40af330aab/41598_2017_14637_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/27f78a5c7aa9/41598_2017_14637_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/1f9cf2c468ca/41598_2017_14637_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/1eda7f2ae226/41598_2017_14637_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/4da1dba231e9/41598_2017_14637_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/ae40af330aab/41598_2017_14637_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/27f78a5c7aa9/41598_2017_14637_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/1f9cf2c468ca/41598_2017_14637_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/1eda7f2ae226/41598_2017_14637_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/4da1dba231e9/41598_2017_14637_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d876/5674023/ae40af330aab/41598_2017_14637_Fig5_HTML.jpg

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