Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells
Background/Aim: Flavonoids are a group of polyphenols, abundantly present in our diet. Although, based on their chemoprotective effects, intake of flavonoids is associated with a high anticancer potential as evidenced in in vitro and in vivo models, the molecular mechanism is still elusive. This stu...
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2025-01-01
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| author | Chujie Li Yue Wang Jian Liang Guido R. M. M. Haenen Yonger Chen Zhengwen Li Ming Zhang Ludwig J. Dubois |
| author_facet | Chujie Li Yue Wang Jian Liang Guido R. M. M. Haenen Yonger Chen Zhengwen Li Ming Zhang Ludwig J. Dubois |
| author_sort | Chujie Li |
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| description | Background/Aim: Flavonoids are a group of polyphenols, abundantly present in our diet. Although, based on their chemoprotective effects, intake of flavonoids is associated with a high anticancer potential as evidenced in in vitro and in vivo models, the molecular mechanism is still elusive. This study explores the antiproliferative and cytotoxic effects of the semi-synthetic flavonoid MonoHER (7-mono-O-(β-hydroxyethyl)-rutoside) in vitro on cancer cells. Materials and Methods: HepG2 liver, MCF7 breast, and H1299 lung cancer cells were grown under ambient conditions with or without MonoHER exposure. CCK8 assay was used to assess cell viability. Apoptosis, JC-1, and mitochondrial mass were determined using flow cytometry and confocal analysis. The effects of monoHER on apoptosis proteins were detected by confocal microscopy analysis and Western blot. Results: It was found that MonoHER can reduce HepG2 cells’ and MCF7 cells’ viability, but not H1299 cells’, and induced apoptosis only in HepG2 cells. MonoHER has the potential to enhance the expression of caspase-9 and caspase-3, to damage mitochondria, and to provoke the release of cytochrome C from the mitochondria. Conclusion: MonoHER can inhibit cell growth and induce apoptosis especially in HepG2 human liver cancer cells by triggering the mitochondrial signal transduction pathway, leading to the release of cytochrome C in the cytoplasm and the subsequent activation of caspase-9 and caspase-3. Future research should further explore MonoHER’s mechanism of action, efficacy, and potential for clinical translation. |
| format | Article |
| id | doaj-art-65d97a0d335942a08e5fd437d0ee1c7a |
| institution | Kabale University |
| issn | 1467-3037 1467-3045 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
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| series | Current Issues in Molecular Biology |
| spelling | doaj-art-65d97a0d335942a08e5fd437d0ee1c7a2025-01-24T13:27:29ZengMDPI AGCurrent Issues in Molecular Biology1467-30371467-30452025-01-014713610.3390/cimb47010036Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 CellsChujie Li0Yue Wang1Jian Liang2Guido R. M. M. Haenen3Yonger Chen4Zhengwen Li5Ming Zhang6Ludwig J. Dubois7Department of Pharmacology and Personalized Medicine, Research Institute for Nutrition and Translational Research in Metabolism (NUTRIM), Faculty of Health, Medicine and Life Sciences, Maastricht University, 6200MD Maastricht, The NetherlandsDepartment of Pharmacology and Personalized Medicine, Research Institute for Nutrition and Translational Research in Metabolism (NUTRIM), Faculty of Health, Medicine and Life Sciences, Maastricht University, 6200MD Maastricht, The NetherlandsGuangdong Provincial Key Laboratory of New Drug Development and Research of Chinese Medicine, Mathematical Engineering Academy of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, ChinaDepartment of Pharmacology and Personalized Medicine, Research Institute for Nutrition and Translational Research in Metabolism (NUTRIM), Faculty of Health, Medicine and Life Sciences, Maastricht University, 6200MD Maastricht, The NetherlandsSchool of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, ChinaSchool of Pharmacy, Chengdu University, 2025 Chengluo Avenue, Chengdu 610106, ChinaHainan University-HSF/LWL Collaborative Innovation Laboratory, College of Food Sciences & Engineering, Hainan University, 58 People Road, Haikou 570228, ChinaThe M-Lab, Department of Precision Medicine, GROW—Research Institute for Oncology and Reproduction, Maastricht University, 6200MD Maastricht, The NetherlandsBackground/Aim: Flavonoids are a group of polyphenols, abundantly present in our diet. Although, based on their chemoprotective effects, intake of flavonoids is associated with a high anticancer potential as evidenced in in vitro and in vivo models, the molecular mechanism is still elusive. This study explores the antiproliferative and cytotoxic effects of the semi-synthetic flavonoid MonoHER (7-mono-O-(β-hydroxyethyl)-rutoside) in vitro on cancer cells. Materials and Methods: HepG2 liver, MCF7 breast, and H1299 lung cancer cells were grown under ambient conditions with or without MonoHER exposure. CCK8 assay was used to assess cell viability. Apoptosis, JC-1, and mitochondrial mass were determined using flow cytometry and confocal analysis. The effects of monoHER on apoptosis proteins were detected by confocal microscopy analysis and Western blot. Results: It was found that MonoHER can reduce HepG2 cells’ and MCF7 cells’ viability, but not H1299 cells’, and induced apoptosis only in HepG2 cells. MonoHER has the potential to enhance the expression of caspase-9 and caspase-3, to damage mitochondria, and to provoke the release of cytochrome C from the mitochondria. Conclusion: MonoHER can inhibit cell growth and induce apoptosis especially in HepG2 human liver cancer cells by triggering the mitochondrial signal transduction pathway, leading to the release of cytochrome C in the cytoplasm and the subsequent activation of caspase-9 and caspase-3. Future research should further explore MonoHER’s mechanism of action, efficacy, and potential for clinical translation.https://www.mdpi.com/1467-3045/47/1/36anticancerapoptosisflavonoidsMonoHERmitochondrial dysfunction |
| spellingShingle | Chujie Li Yue Wang Jian Liang Guido R. M. M. Haenen Yonger Chen Zhengwen Li Ming Zhang Ludwig J. Dubois Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells Current Issues in Molecular Biology anticancer apoptosis flavonoids MonoHER mitochondrial dysfunction |
| title | Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells |
| title_full | Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells |
| title_fullStr | Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells |
| title_full_unstemmed | Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells |
| title_short | Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells |
| title_sort | exploring the anticancer potential of monoher 7 mono o β hydroxyethyl rutoside mitochondrial dependent apoptosis in hepg2 cells |
| topic | anticancer apoptosis flavonoids MonoHER mitochondrial dysfunction |
| url | https://www.mdpi.com/1467-3045/47/1/36 |
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