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双苯甲酮类化合物来源于 Bge. 通过 NF-κB 信号通路在 HepG2 细胞中显示出抗癌活性。

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

机构信息

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.

School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.

出版信息

Molecules. 2019 Jun 15;24(12):2246. doi: 10.3390/molecules24122246.

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.

摘要

对 Bge. 的纤维根进行的化学研究导致了四种二苯甲酮的分离,包括一种新化合物 () 和三种已知化合物 ()。综合的 D、D NMR 和 HRESIMS 数据确定了分离化合物的结构。通过比较计算的旋光度 (OR) 与实验数据确定了绝对构型。所有分离物均对肝癌细胞系 (HepG2 和 Hep3B) 进行了细胞毒性评估。化合物 对 HepG2 和 Hep3B 细胞表现出强烈的细胞毒性,IC 值分别为 153.1 和 180.6 nM。通过 MTT 测定、流式细胞术和 Western blot 分析,化合物 显示通过 NF-κB 信号通路刺激 HepG2 细胞凋亡的能力。这些二苯甲酮是开发更好的肝癌治疗方法的潜在先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9f11/6630431/c2b06e331c2b/molecules-24-02246-g001.jpg

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