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Abstract
Five 3-formyl-2-arylbenzofuran derivatives, including three new compounds (1-3) and two known analogues (4-5), were identified from the 95% EtOH extract of Itea yunnanensis. Extensive spectroscopic analyses were performed for the structure elucidation of all new benzofurans, and single-crystal X-ray diffraction analyses were further employed for the structure verification of iteafuranals C (1) and D (2). In MTT assay, iteafuranal E (3) and iteafuranal A (4) displayed significant growth inhibition effect on SK-Hep-1 cells with IC50 values of 5.365 μM and 6.013 μM, respectively. The colony formation assay of 3 and 4 further confirmed their remarkable inhibitory effect on cell growth. Preliminary mechanism study demonstrated that 3 remarkably down-regulated the phosphorylation level of ERK, which suggested 3 could inhibit cell growth and induce apoptosis of SK-Hep-1 cells by blocking RAS/RAF/MEK/ERK signaling pathway. This study highlighted the potential of 3-fomyl-2-benzofuran derivatives as novel lead compounds to treat Hepatocellular carcinoma.
Acknowledgements
This work was financially supported by the National Natural Science Foundation of China (81860764), the Department of Science and Technology of Guizhou Province for Basic Research (QKHJC[2016]1017; QKHJC[2019]1036), the 1000 Talent Plan (Qian Cengci) of Guizhou Province, and the Special Project for Academic Seed Training and Innovation Exploration of Guizhou University of Traditional Chinese Medicine (QKHPTRC-[2017]5735-23).
Disclosure statement
The authors declared no potential conflict of interest.