In this section, you can access to the latest technical information related to the FUTURE project topic.

Stereoisomeric guaiacylglycerol-?-coniferyl aldehyde ether induces distinctive apoptosis by downregulation of MEK/ERK pathway in hepatocellular carcinoma cells

Two 8-O-4?-type neolignan epimers erythro-guaiacylglycerol-?-coniferyl aldehyde ether (1) and threo-guaiacylglycerol-?-coniferyl aldehyde ether (2) were isolated from the stems of Picrasma quassioides. Further chiral separation gave two pairs of enantiomers 1a/1b and 2a/2b. The cytotoxicity assay against hepatocellular carcinoma Hep3B and HepG2 cells was evaluated by MTT assay. The results showed that 1b (IC50?=?45.56??M) and 2b (IC50?=?39.02??M) had more cytotoxic effect than its enantiomers 1a (IC50?=?82.66??M) and 2a (IC50?=?67.97??M) in Hep3B cells, respectively. Moreover, 1b and 2b could induce more apoptotic cells as well as higher reactive oxygen species (ROS) generation than 1a and 2a at 50??M. In addition, a further study on the phosphoinositide 3-kinase (PI3K)/AKT and mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) signaling pathways was investigated. The results revealed that all compounds had no significant effect on PI3K/AKT pathway, however, 1b and 2b attenuated the relative levels of p-MEK and p-ERK when compared with 1a and 2a. Taken together, the absolute configurations of guaiacylglycerol-?-coniferyl aldehyde ether had an impact on the inhibitory effect on Hep3B cells. The inactivation of MEK/ERK signaling pathway might contribute to apoptosis induction and ROS generation in 1b- and 2b-treated cells.

» Author: Guo-Dong Yao, Jie Wang, Xiao-Yu Song, Le Zhou, Li-Li Lou, Wen-Yu Zhao, Bin Lin, Xiao-Xiao Huang, Shao-Jiang Song

» Reference: 10.1016/j.bioorg.2018.08.033

» Publication Date: 01/12/2018

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