Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells.
Jun ChenLinli ZhangChanghong LiRuochen ChenChengmei LiuMingshun ChenPublished in: Nutrients (2019)
Epigallocatechin gallate (EGCG) is the predominant tea polyphenol and it exhibits a hydrophilic character. The lipophilized EGCG derivative (LEGCG) was synthesized by enzymatic esterification of EGCG with lauric acid to enhance its bioactivity. The tetralauroyl EGCG was confirmed by high-performance liquid chromatography-tandem mass spectrometry and further identified as 3', 5', 3″, 5″-4-O-lauroyl EGCG by 1H and 13C nuclear magnetic resonance. The anti-proliferation effect of LEGCG on DU145 human prostate carcinoma cells was evaluated by MTT assay. In addition, the underlying molecular mechanism by which LEGCG exerts anti-proliferation efficacy was elucidated by flow cytometry and immunoblot analysis. Results suggested that LEGCG exhibited a dose-dependent anti-proliferation effect on DU145 cells by G0/G1 phase arrest and induction of apoptosis. LEGCG induced cell cycle arrest via p53/p21 activation, which down-regulated the cyclin D1 and CDK4 expression. In addition, LEGCG induced apoptosis by increasing the Bax/Bcl-2 ratio, the cytochrome c release, and the caspases cleavage on DU145 cells. The results provide theoretical support to prevent prostate cancer with LEGCG.
Keyphrases
- cell cycle arrest
- signaling pathway
- pi k akt
- induced apoptosis
- cell death
- prostate cancer
- liquid chromatography tandem mass spectrometry
- endothelial cells
- magnetic resonance
- endoplasmic reticulum stress
- flow cytometry
- oxidative stress
- poor prognosis
- cell cycle
- radical prostatectomy
- simultaneous determination
- high glucose
- pluripotent stem cells
- nitric oxide
- transcription factor
- magnetic resonance imaging
- hydrogen peroxide
- solid phase extraction
- high throughput
- computed tomography
- long non coding rna
- mass spectrometry