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二苯并呋喃、4-色满酮、苯乙酮和二硫代环丁烷衍生物: 的细胞毒性成分。

Dibenzofuran, 4-Chromanone, Acetophenone, and Dithiecine Derivatives: Cytotoxic Constituents from .

机构信息

Institute of Biopharmaceutical Sciences, School of Pharmaceutical Sciences, National Yang Ming Chiao Tung University, Taipei 112, Taiwan.

Department of Life Science, Chinese Culture University, Taipei 110, Taiwan.

出版信息

Int J Mol Sci. 2021 Jul 12;22(14):7448. doi: 10.3390/ijms22147448.

Abstract

Five new compounds, eupatodibenzofuran A (), eupatodibenzofuran B (), 6-acetyl-8-methoxy-2,2-dimethylchroman-4-one (), eupatofortunone (), and eupatodithiecine (), have been isolated from the aerial part of , together with 11 known compounds (‒). Compounds and featured a new carbon skeleton with an unprecedented 1-(9-(4-methylphenyl)-6-methyldibe nzo[,]furan-2-yl)ethenone. Among the isolates, compound exhibited potent inhibitory activity with IC values of 5.95 ± 0.89 and 5.55 ± 0.23 μM, respectively, against A549 and MCF-7 cells. The colony-formation assay demonstrated that compound (5 μM) obviously decreased A549 and MCF-7 cell proliferation, and Western blot test confirmed that compound markedly induced apoptosis of A549 and MCF-7 cells through mitochondrial- and caspase-3-dependent pathways.

摘要

从 的地上部分分离得到了 5 个新化合物,分别为:eupatodibenzofuran A ()、eupatodibenzofuran B ()、6-乙酰基-8-甲氧基-2,2-二甲基色满-4-酮 ()、eupatofortunone ()和 eupatodithiecine (),此外还分离得到了 11 个已知化合物(‒)。化合物 和 具有全新的碳骨架,包含一个前所未有的 1-(9-(4-甲基苯基)-6-甲基二苯并[,]呋喃-2-基)乙烯酮。在所分离得到的化合物中,化合物 对 A549 和 MCF-7 细胞表现出了较强的抑制活性,IC 值分别为 5.95 ± 0.89 和 5.55 ± 0.23 μM。集落形成实验表明,化合物 (5 μM)可明显降低 A549 和 MCF-7 细胞的增殖,Western blot 实验证实化合物 通过线粒体和 caspase-3 依赖的途径显著诱导了 A549 和 MCF-7 细胞的凋亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb6a/8307038/35f3e5fa76fa/ijms-22-07448-g001.jpg

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