Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells

Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells

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...

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Main Authors: Jun Chen, Linli Zhang, Changhong Li, Ruochen Chen, Chengmei Liu, Mingshun Chen
Format: Article
Language:English
Published: MDPI AG 2019-12-01
Series:Nutrients
Subjects:
egcg
legcg
du145 cell
proliferation
apoptosis
Online Access:https://www.mdpi.com/2072-6643/12/1/92
id doaj-b9dc3547669f441fb014798dfae6f19d
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spelling doaj-b9dc3547669f441fb014798dfae6f19d2020-11-25T01:36:21ZengMDPI AGNutrients2072-66432019-12-011219210.3390/nu12010092nu12010092Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer CellsJun Chen0Linli Zhang1Changhong Li2Ruochen Chen3Chengmei Liu4Mingshun Chen5State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaState Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaState Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaState Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaState Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaState Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, ChinaEpigallocatechin 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&#8242;, 5&#8242;, 3&#8243;, 5&#8243;-4-<i>O</i>-lauroyl EGCG by <sup>1</sup>H and <sup>13</sup>C 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 <i>c</i> release, and the caspases cleavage on DU145 cells. The results provide theoretical support to prevent prostate cancer with LEGCG.https://www.mdpi.com/2072-6643/12/1/92egcglegcgdu145 cellproliferationapoptosis
collection DOAJ
language English
format Article
sources DOAJ
author Jun Chen
Linli Zhang
Changhong Li
Ruochen Chen
Chengmei Liu
Mingshun Chen
spellingShingle Jun Chen
Linli Zhang
Changhong Li
Ruochen Chen
Chengmei Liu
Mingshun Chen
Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
Nutrients
egcg
legcg
du145 cell
proliferation
apoptosis
author_facet Jun Chen
Linli Zhang
Changhong Li
Ruochen Chen
Chengmei Liu
Mingshun Chen
author_sort Jun Chen
title Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
title_short Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
title_full Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
title_fullStr Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
title_full_unstemmed Lipophilized Epigallocatechin Gallate Derivative Exerts Anti-Proliferation Efficacy through Induction of Cell Cycle Arrest and Apoptosis on DU145 Human Prostate Cancer Cells
title_sort lipophilized epigallocatechin gallate derivative exerts anti-proliferation efficacy through induction of cell cycle arrest and apoptosis on du145 human prostate cancer cells
publisher MDPI AG
series Nutrients
issn 2072-6643
publishDate 2019-12-01
description 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&#8242;, 5&#8242;, 3&#8243;, 5&#8243;-4-<i>O</i>-lauroyl EGCG by <sup>1</sup>H and <sup>13</sup>C 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 <i>c</i> release, and the caspases cleavage on DU145 cells. The results provide theoretical support to prevent prostate cancer with LEGCG.
topic egcg
legcg
du145 cell
proliferation
apoptosis
url https://www.mdpi.com/2072-6643/12/1/92
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AT changhongli lipophilizedepigallocatechingallatederivativeexertsantiproliferationefficacythroughinductionofcellcyclearrestandapoptosisondu145humanprostatecancercells
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AT chengmeiliu lipophilizedepigallocatechingallatederivativeexertsantiproliferationefficacythroughinductionofcellcyclearrestandapoptosisondu145humanprostatecancercells
AT mingshunchen lipophilizedepigallocatechingallatederivativeexertsantiproliferationefficacythroughinductionofcellcyclearrestandapoptosisondu145humanprostatecancercells
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