Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Taicheng Road, Yangling 712100, China.
Molecules. 2022 Aug 16;27(16):5230. doi: 10.3390/molecules27165230.
Flowers of Inula britannica commercially serve as pharmaceutical herbs in the manufacturing of medicinal products. In the current study, sesquiterpenoids of I. britannica flowers’ extract and their potential effects against triple-negative breast cancer (TNBC) cells were investigated. Eight structurally diverse sesquiterpenoids, including one sesquiterpenoid dimer (1) and seven sesquiterpenoid monomers (2−8) were isolated from this source. The structures of all compounds were elucidated by 1D/2D NMR data, and their absolute configurations were discerned by single crystal X-ray diffraction. All of the compounds were tested for their potential effects against TNBC. Specifically, 5 displayed strong antiproliferative potency against TNBC cells with a high selective index (SI) on MCF-7 cells (SI > 4 of IC50 on MDA-MB-468/IC50 on MCF-7), and dimer 1 (IC50 = 8.82 ± 0.85 μM) showed better antiproliferative potency against MCF-7 cells than the other monomers did (2−8) (IC50 > 20 μM). To our best knowledge, compound 5 is the first sesquiterpenoid targeting TNBC cells.
滨蒿花在商业上被用作制药草药，用于制造药品。在本研究中，研究了滨蒿花提取物中的倍半萜类化合物及其对三阴性乳腺癌 (TNBC) 细胞的潜在作用。从该来源中分离出了八种结构不同的倍半萜类化合物，包括一种倍半萜二聚体 (1) 和七种倍半萜单体 (2-8)。所有化合物的结构均通过 1D/2D NMR 数据阐明，并通过单晶 X 射线衍射确定其绝对构型。所有化合物均测试了其对 TNBC 的潜在作用。具体来说，化合物 5 对 TNBC 细胞表现出很强的增殖抑制作用，对 MCF-7 细胞具有高选择性指数 (SI) (SI > 4 的 IC50 对 MDA-MB-468/IC50 对 MCF-7)，二聚体 1 (IC50 = 8.82 ± 0.85 μM) 对 MCF-7 细胞的增殖抑制作用优于其他单体 (2-8) (IC50 > 20 μM)。据我们所知，化合物 5 是第一个针对 TNBC 细胞的倍半萜类化合物。
