Benzyl sulforaphane is superior to sulforaphane in inhibiting the Akt/MAPK and activating the Nrf2/ARE signalling pathways in HepG2 cells. (25th September 2018)

• Record Type: Journal Article
• Authors: Ren, Jie; Yuan, Ling; Wang, Yue; Chen, Guangtong; Hu, Kun
• Is Part Of: Journal of pharmacy and pharmacology. Volume 70:Number 12(2018)
• Page Start: 1643
• Page End: 1653
• Publication Date: 2018-09-25
• Subjects: Akt/MAPK -- apoptosis -- benzyl sulforaphane -- mitochondria -- Nrf2; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.13015
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: Sulforaphane (SFN), an isothiocyanate found in cruciferous vegetables, has been reported to own anticarcinogenic, antiinflammatory and cancer chemopreventive properties. Benzyl sulforaphane (BSFN) was a derivative of SFN which was designed and synthesized by our laboratory. Here, the cancer prevention and anticancer effects of BSFN on human hepatoma (HepG2) cells were investigated. Methods: The following effects of BSFN on components of the mitochondrial apoptotic pathway were examined: generation of reactive oxygen species and mitochondrial membrane potential (ΔΨm) changes by flow cytometry, the expression changes of Bcl-2 family proteins and Akt/MAPK proteins by western blot. The protein levels of Nrf2 and Keap1 were also tested via Western blot. The effects of BSFN on Nrf2 nuclear translocation and ARE-reporter gene activity were examined by fluorescence microscope and multifunctional spectrophotometer. Key findings: Benzyl sulforaphane could induce cell apoptosis by mitochondrion-dependent pathway, which inhibited HepG2 cells growth in a manner of time- and concentration -dependent. Furthermore, BSFN could inhibit the Akt/MAPK and activate the Nrf2/ARE pathway in HepG2 cells. Conclusions: Benzyl sulforaphane was superior to SFN in inhibiting Akt/MAPK and activating Nrf2/ARE signalling pathways in HepG2 cells, which indicated that BSFN could be a safe therapeutic strategy for the prevention and treatment of liver cancer.