Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells

Piperine, a phytochemical alkaloid, exhibits notable anticancer properties in several cancer cell types. In this study, we investigated the mechanisms by which piperine induces cell death and apoptosis in colorectal cancer (CRC) cells, focusing on oxidative stress and key signaling pathways. Using M...

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Main Authors: Wan-Ling Chang, Jyun-Yu Peng, Chain-Lang Hong, Pei-Ching Li, Soi Moi Chye, Fung-Jou Lu, Huei-Yu Lin, Ching-Hsein Chen
Format: Article
Language:English
Published: MDPI AG 2025-07-01
Series:Antioxidants
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Online Access:https://www.mdpi.com/2076-3921/14/7/892
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author Wan-Ling Chang
Jyun-Yu Peng
Chain-Lang Hong
Pei-Ching Li
Soi Moi Chye
Fung-Jou Lu
Huei-Yu Lin
Ching-Hsein Chen
author_facet Wan-Ling Chang
Jyun-Yu Peng
Chain-Lang Hong
Pei-Ching Li
Soi Moi Chye
Fung-Jou Lu
Huei-Yu Lin
Ching-Hsein Chen
author_sort Wan-Ling Chang
collection DOAJ
description Piperine, a phytochemical alkaloid, exhibits notable anticancer properties in several cancer cell types. In this study, we investigated the mechanisms by which piperine induces cell death and apoptosis in colorectal cancer (CRC) cells, focusing on oxidative stress and key signaling pathways. Using MTT assay, flow cytometry, gene overexpression, and Western blot analysis, we observed that piperine significantly reduced cell viability, triggered G1 phase cell cycle arrest, and promoted apoptosis in DLD-1 cells. In addition, piperine effectively suppressed cell viability and induced apoptosis in other CRC cell lines, including SW480, HT-29, and Caco-2 cells. These effects were associated with increased intracellular reactive oxygen species (ROS) generation, mediated by the regulation of mitochondrial complex III, NADPH oxidase, and xanthine oxidase. Additionally, piperine modulated signaling pathways by inhibiting phosphoinositide 3-kinase (PI3K)/Akt, activating p38 and p-extracellular signal-regulated kinase (ERK). Pretreatment with antimycin A, apocynin, allopurinol, and PD98059, and the overexpression of p-Akt significantly recovered cell viability and reduced apoptosis, confirming the involvement of these pathways. This study is the first to demonstrate piperine induces apoptosis in CRC cells through a multifaceted oxidative stress mechanism and by critically modulating PI3K/Akt and ERK signaling pathways.
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spelling doaj-art-946bb282fb91436e84c39cfd8f3a49e92025-08-20T03:13:36ZengMDPI AGAntioxidants2076-39212025-07-0114789210.3390/antiox14070892Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer CellsWan-Ling Chang0Jyun-Yu Peng1Chain-Lang Hong2Pei-Ching Li3Soi Moi Chye4Fung-Jou Lu5Huei-Yu Lin6Ching-Hsein Chen7Department of Anesthesiology, Chang Gung Memorial Hospital at Chiayi, No. 8, West Section of Jiapu Road, Puzi City 613016, Chiayi County, TaiwanDepartment of Anesthesiology, Chang Gung Memorial Hospital at Chiayi, No. 8, West Section of Jiapu Road, Puzi City 613016, Chiayi County, TaiwanDepartment of Anesthesiology, Chang Gung Memorial Hospital at Chiayi, No. 8, West Section of Jiapu Road, Puzi City 613016, Chiayi County, TaiwanDepartment of Anesthesiology, Chang Gung Memorial Hospital at Chiayi, No. 8, West Section of Jiapu Road, Puzi City 613016, Chiayi County, TaiwanSchool of Health Science, Division of Applied Biomedical Science and Biotechnology, IMU University, No. 126, Jalan Jalil Perkasa 19, Bukit Jalil, Kuala Lumpur 57000, MalaysiaInstitute of Medicine, Chung Shan Medical University, No. 110, Section 1, Jianguo North Road, Taichung City 402306, TaiwanDepartment of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, A25-303 Room, Life Sciences Hall, No. 300, Syuefu Road, Chiayi City 600355, TaiwanDepartment of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, A25-303 Room, Life Sciences Hall, No. 300, Syuefu Road, Chiayi City 600355, TaiwanPiperine, a phytochemical alkaloid, exhibits notable anticancer properties in several cancer cell types. In this study, we investigated the mechanisms by which piperine induces cell death and apoptosis in colorectal cancer (CRC) cells, focusing on oxidative stress and key signaling pathways. Using MTT assay, flow cytometry, gene overexpression, and Western blot analysis, we observed that piperine significantly reduced cell viability, triggered G1 phase cell cycle arrest, and promoted apoptosis in DLD-1 cells. In addition, piperine effectively suppressed cell viability and induced apoptosis in other CRC cell lines, including SW480, HT-29, and Caco-2 cells. These effects were associated with increased intracellular reactive oxygen species (ROS) generation, mediated by the regulation of mitochondrial complex III, NADPH oxidase, and xanthine oxidase. Additionally, piperine modulated signaling pathways by inhibiting phosphoinositide 3-kinase (PI3K)/Akt, activating p38 and p-extracellular signal-regulated kinase (ERK). Pretreatment with antimycin A, apocynin, allopurinol, and PD98059, and the overexpression of p-Akt significantly recovered cell viability and reduced apoptosis, confirming the involvement of these pathways. This study is the first to demonstrate piperine induces apoptosis in CRC cells through a multifaceted oxidative stress mechanism and by critically modulating PI3K/Akt and ERK signaling pathways.https://www.mdpi.com/2076-3921/14/7/892piperineapoptosiscell cycle arrestoxidative stressPI3K/AktMAPK
spellingShingle Wan-Ling Chang
Jyun-Yu Peng
Chain-Lang Hong
Pei-Ching Li
Soi Moi Chye
Fung-Jou Lu
Huei-Yu Lin
Ching-Hsein Chen
Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
Antioxidants
piperine
apoptosis
cell cycle arrest
oxidative stress
PI3K/Akt
MAPK
title Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
title_full Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
title_fullStr Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
title_full_unstemmed Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
title_short Piperine Induces Apoptosis and Cell Cycle Arrest via Multiple Oxidative Stress Mechanisms and Regulation of PI3K/Akt and MAPK Signaling in Colorectal Cancer Cells
title_sort piperine induces apoptosis and cell cycle arrest via multiple oxidative stress mechanisms and regulation of pi3k akt and mapk signaling in colorectal cancer cells
topic piperine
apoptosis
cell cycle arrest
oxidative stress
PI3K/Akt
MAPK
url https://www.mdpi.com/2076-3921/14/7/892
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