Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway

Objective: Multidrug resistance (MDR) is one main cause of chemotherapy failure. Baicalin is an important active ingredient with anticancer potential in many Chinese herbal medicines. In order to understand the function of baicalin reversing MDR in hepatocellular carcinoma (HCC) and the molecular me...

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Main Authors: Fei Li, Zilin Lan, Weiwei Jiang, Jianheng Zhou, Jiumao Lin, Jinyan Zhao
Format: Article
Language:English
Published: KeAi Communications Co., Ltd. 2025-06-01
Series:Journal of Holistic Integrative Pharmacy
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Online Access:http://www.sciencedirect.com/science/article/pii/S2707368825000202
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author Fei Li
Zilin Lan
Weiwei Jiang
Jianheng Zhou
Jiumao Lin
Jinyan Zhao
author_facet Fei Li
Zilin Lan
Weiwei Jiang
Jianheng Zhou
Jiumao Lin
Jinyan Zhao
author_sort Fei Li
collection DOAJ
description Objective: Multidrug resistance (MDR) is one main cause of chemotherapy failure. Baicalin is an important active ingredient with anticancer potential in many Chinese herbal medicines. In order to understand the function of baicalin reversing MDR in hepatocellular carcinoma (HCC) and the molecular mechanisms that underlie it, the current study was designed. Methods: Bel-7402 and Bel-7402/5-FU cells were cultured, and MTT assay was applied to detect cell viability and the cross-resistance of Bel-7402/5-FU cells. The pump function, apoptosis, and autophagy were detected by flow cytometry. The related proteins were detected by Western blot assay. The PI3K agonist (740Y-P) was used to verify whether baicalin overcomes the drug resistance of HCC cells by blocking the PI3K/AKT pathway. Results: The findings showed that Bel-7402/5-FU cells were cross-resistant to different chemotherapeutic drugs. Baicalin inhibited cell viability in both Bel-7402/5-FU and Bel-7402 ​cells, and baicalin increased sensitivity of Bel-7402/5-FU cells to 5-FU in time- and dose-dependent manners. Baicalin increased the accumulation of doxorubicin and rhodamine-123 in Bel-7402/5-FU cells and inhibited the protein expression of ABCG2, ABCB1, and ABCC1, associated with pump function. In addition, baicalin induced apoptosis of Bel-7402/5-FU cells via up-regulating Bax expression. Furthermore, baicalin increased autophagy through regulating LC3-Ⅱ, p62, and Beclin-1. Baicalin reversed drug resistance in Bel-7402/5-FU cells by inhibiting the PI3K/AKT pathway, which promoted autophagy and apoptosis to restore chemosensitivity. Conclusion: Baicalin increased accumulation of chemotherapy drugs and induced apoptosis and autophagy in Bel-7402/5-FU cells by inhibiting the PI3K/AKT signaling pathway, that may be the important mechanism by which baicalin reverses the MDR of HCC.
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spelling doaj-art-2bf530bbc7e04c9fb596598aa57154c32025-08-20T03:58:14ZengKeAi Communications Co., Ltd.Journal of Holistic Integrative Pharmacy2707-36882025-06-016215015810.1016/j.jhip.2025.05.001Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathwayFei Li0Zilin Lan1Weiwei Jiang2Jianheng Zhou3Jiumao Lin4Jinyan Zhao5Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Fujian Key Laboratory of Integrative Medicine on Geriatric, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, ChinaAcademy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Fujian Key Laboratory of Integrative Medicine on Geriatric, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, ChinaAcademy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Fujian Key Laboratory of Integrative Medicine on Geriatric, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, ChinaAcademy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; College of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, ChinaAcademy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Fujian Key Laboratory of Integrative Medicine on Geriatric, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, ChinaAcademy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Fujian Key Laboratory of Integrative Medicine on Geriatric, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China; Corresponding author. Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China.Objective: Multidrug resistance (MDR) is one main cause of chemotherapy failure. Baicalin is an important active ingredient with anticancer potential in many Chinese herbal medicines. In order to understand the function of baicalin reversing MDR in hepatocellular carcinoma (HCC) and the molecular mechanisms that underlie it, the current study was designed. Methods: Bel-7402 and Bel-7402/5-FU cells were cultured, and MTT assay was applied to detect cell viability and the cross-resistance of Bel-7402/5-FU cells. The pump function, apoptosis, and autophagy were detected by flow cytometry. The related proteins were detected by Western blot assay. The PI3K agonist (740Y-P) was used to verify whether baicalin overcomes the drug resistance of HCC cells by blocking the PI3K/AKT pathway. Results: The findings showed that Bel-7402/5-FU cells were cross-resistant to different chemotherapeutic drugs. Baicalin inhibited cell viability in both Bel-7402/5-FU and Bel-7402 ​cells, and baicalin increased sensitivity of Bel-7402/5-FU cells to 5-FU in time- and dose-dependent manners. Baicalin increased the accumulation of doxorubicin and rhodamine-123 in Bel-7402/5-FU cells and inhibited the protein expression of ABCG2, ABCB1, and ABCC1, associated with pump function. In addition, baicalin induced apoptosis of Bel-7402/5-FU cells via up-regulating Bax expression. Furthermore, baicalin increased autophagy through regulating LC3-Ⅱ, p62, and Beclin-1. Baicalin reversed drug resistance in Bel-7402/5-FU cells by inhibiting the PI3K/AKT pathway, which promoted autophagy and apoptosis to restore chemosensitivity. Conclusion: Baicalin increased accumulation of chemotherapy drugs and induced apoptosis and autophagy in Bel-7402/5-FU cells by inhibiting the PI3K/AKT signaling pathway, that may be the important mechanism by which baicalin reverses the MDR of HCC.http://www.sciencedirect.com/science/article/pii/S2707368825000202BaicalinHepatocellular carcinomaMultidrug resistanceApoptosisAutophagyPI3K/AKT signaling pathway
spellingShingle Fei Li
Zilin Lan
Weiwei Jiang
Jianheng Zhou
Jiumao Lin
Jinyan Zhao
Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
Journal of Holistic Integrative Pharmacy
Baicalin
Hepatocellular carcinoma
Multidrug resistance
Apoptosis
Autophagy
PI3K/AKT signaling pathway
title Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
title_full Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
title_fullStr Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
title_full_unstemmed Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
title_short Baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line Bel-7402/5-FU cells via PI3K/AKT pathway
title_sort baicalin induces apoptosis and autophagy in resistant human hepatocellular carcinoma cell line bel 7402 5 fu cells via pi3k akt pathway
topic Baicalin
Hepatocellular carcinoma
Multidrug resistance
Apoptosis
Autophagy
PI3K/AKT signaling pathway
url http://www.sciencedirect.com/science/article/pii/S2707368825000202
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