Benzophenones from Bge. Exhibit Anticancer Activity in HepG2 Cells via the NF-κB Signaling Pathway.

De-Ling Wu, Zhen-Dong Liao, Fang-Fang Chen, Wei Zhang, Ya-Shuo Ren, Can-Can Wang, Xiao-Xiao Chen, Dai-Yin Peng, Ling-Yi Kong

Journal: Molecules (Basel, Switzerland) 2019;24(12):2246

PMID: 31208101

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Abstract

A chemical investigation of the fibrous roots of Bge. led to the isolation of four benzophenones, including one new compound () and three known ones (). Comprehensive D, D NMR and HRESIMS data established the structures of the isolated compounds. The absolute configurations were determined by comparison of the calculated optical rotation (OR) with experimental data. All the isolates were evaluated for their cytotoxicities on hepatocellular carcinoma cell lines (HepG2 and Hep3B). Compound showed strong cytotoxicity against HepG2 and Hep3B cells, with IC values at 153.1 and 180.6 nM. Through MTT assay, flow cytometry and Western blot analysis, compound demonstrated the ability to stimulate apoptosis via the NF-κB signaling pathway in HepG2 cells. These benzophenones are potential lead compounds for the development of better treatments for hepatocellular carcinoma.

Address: Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; Anhui Province Key Laboratory of Traditional Chinese Medicine Decoction Pieces of New Manufacturing Technology, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; Anhui Province Key Laboratory of Traditional Chinese Medicine Decoction Pieces of New Manufacturing Technology, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; Anhui Province Key Laboratory of Traditional Chinese Medicine Decoction Pieces of New Manufacturing Technology, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China. [email protected].; Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. [email protected].

DOI: 10.3390/molecules24122246

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MeSH Terms: Anemarrhena, Antineoplastic Agents, Phytogenic, Apoptosis, Benzophenones, Cell Survival, Hep G2 Cells, Humans, Magnetic Resonance Spectroscopy, Molecular Structure, NF-kappa B, Plant Extracts, Plant Roots, Signal Transduction, Structure-Activity Relationship