Abstract
7-Difluoromethyl-5, 4’-dimethoxygenistein (DFMG), prepared by the difluoromethylation and alkylation of Genistein, is a new active chemical entity. In this study, we investigated the inhibitory effect of DFMG on Lysophosphatidyl choline (LPC)-induced apoptosis of human umbilical vein endothelial cells-12 (HUVEC-12) through mitochondrial apoptosis pathway. Lysophosphatidyl choline (LPC) was used to build apoptosis model in HUVEC-12 cells. The apoptosis rate in each group was determined by using flow cytometry of ANNEXIN V/PI staining. The mean ffluorescence intensity (MFI) of mitochondria mmembrane ppotential (MMP) was determined by using flow cytometry. The expression levels of cytochrome C (CytC), p-JNK and PARP were detected by performing western blotting assay. The activities of caspase-3 and caspase-9 were detected by a colorimetric method with caspase colorimetric assay kits. As compared with the control group, DFMG notably decreased the apoptosis rate, the MFI of the MMP, and the generation of Reactive Oxygen Species (ROS) induced by LPC. In addition, DFMG had suppressive effects on the expressions of CytC, P-JNK, and PARP, as well as on the activities of caspase-3 and caspase-9 in LPC-treated HUVEC-12 cells. DFMG can antagonize LPC-induced apoptosis of HUVE-12 cells. The underlying mechanism may be involved in the inhibition of mitochondrial apoptosis pathway.
Keywords: Apoptosis, 7-Difluoromethyl-5, 4'-dimethoxygenistein, mitochondrial, Cytochrome C, Lysophosphatidyl choline.
Current Signal Transduction Therapy
Title:7-Difluoromethyl-5, 4’-Dimethoxygenistein Reverses LPC-Induced Apoptosis of HUVE-12 Cells Through Regulating Mitochondrial Apoptosis Pathway
Volume: 9 Issue: 1
Author(s): Shiwei Liu, Lesai Li, Jing Zhang, He Huang, Shuting Yang, Changjie Ren, Xiaohua Fu and Yong Zhang
Affiliation:
Keywords: Apoptosis, 7-Difluoromethyl-5, 4'-dimethoxygenistein, mitochondrial, Cytochrome C, Lysophosphatidyl choline.
Abstract: 7-Difluoromethyl-5, 4’-dimethoxygenistein (DFMG), prepared by the difluoromethylation and alkylation of Genistein, is a new active chemical entity. In this study, we investigated the inhibitory effect of DFMG on Lysophosphatidyl choline (LPC)-induced apoptosis of human umbilical vein endothelial cells-12 (HUVEC-12) through mitochondrial apoptosis pathway. Lysophosphatidyl choline (LPC) was used to build apoptosis model in HUVEC-12 cells. The apoptosis rate in each group was determined by using flow cytometry of ANNEXIN V/PI staining. The mean ffluorescence intensity (MFI) of mitochondria mmembrane ppotential (MMP) was determined by using flow cytometry. The expression levels of cytochrome C (CytC), p-JNK and PARP were detected by performing western blotting assay. The activities of caspase-3 and caspase-9 were detected by a colorimetric method with caspase colorimetric assay kits. As compared with the control group, DFMG notably decreased the apoptosis rate, the MFI of the MMP, and the generation of Reactive Oxygen Species (ROS) induced by LPC. In addition, DFMG had suppressive effects on the expressions of CytC, P-JNK, and PARP, as well as on the activities of caspase-3 and caspase-9 in LPC-treated HUVEC-12 cells. DFMG can antagonize LPC-induced apoptosis of HUVE-12 cells. The underlying mechanism may be involved in the inhibition of mitochondrial apoptosis pathway.
Export Options
About this article
Cite this article as:
Liu Shiwei, Li Lesai, Zhang Jing, Huang He, Yang Shuting, Ren Changjie, Fu Xiaohua and Zhang Yong, 7-Difluoromethyl-5, 4’-Dimethoxygenistein Reverses LPC-Induced Apoptosis of HUVE-12 Cells Through Regulating Mitochondrial Apoptosis Pathway, Current Signal Transduction Therapy 2014; 9 (1) . https://dx.doi.org/10.2174/157436240901140924105409
DOI https://dx.doi.org/10.2174/157436240901140924105409 |
Print ISSN 1574-3624 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-389X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Molecular Targeting of Acid Ceramidase: Implications to Cancer Therapy
Current Drug Targets Clinical and Pharmacological Aspects of Inflammatory Demyelinating Diseases in Childhood: An Update
Current Neuropharmacology Development and Medical Application of Unsaturated Carbaglycosylamine Glycosidase Inhibitors
Mini-Reviews in Medicinal Chemistry Predicted Contributions of Flavin-containing Monooxygenases to the N-oxygenation of Drug Candidates Based on their Estimated Base Dissociation Constants
Current Drug Metabolism Metastatic Breast Cancer, Organotropism and Therapeutics: A Review
Current Cancer Drug Targets Lactones: Generic Inhibitors of Enzymes?
Mini-Reviews in Medicinal Chemistry IgG4-Related Disease (IgG4+MOLPS) – Diagnostic Criteria and Diagnostic Problems
Current Immunology Reviews (Discontinued) Protein Aggregation in Neurodegenerative Diseases: Insights from Computational Analyses
Current Bioinformatics The Antagonists of Endothelin Receptors: Results and Perspectives
Current Pharmaceutical Analysis An Overview of Phytotherapeutic Approaches for the Treatment of Benign Prostatic Hyperplasia
Mini-Reviews in Medicinal Chemistry Management of Incidental Findings in the Era of Next-generation Sequencing
Current Genomics Developing Histone Deacetylase Inhibitors as Anti-Cancer Therapeutics
Current Medicinal Chemistry Mechanisms of Phospholipase C-Regulated Calcium Entry
Current Molecular Medicine Folate-Linked Lipid-Based Nanoparticle for Targeted Gene Delivery
Current Drug Delivery Graphical Abstracts:
Current Medical Imaging Zinc Dependent Histone Deacetylase Inhibitors in Cancer Therapeutics: Recent Update
Current Medicinal Chemistry Patent Annotations
Recent Patents on Anti-Infective Drug Discovery 1,3,4-Thiadiazole Based Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Organoselenium Compounds as Catalysts in Nature and Laboratory
Current Organic Chemistry General Molecular Biology and Architecture of Nuclear Receptors
Current Topics in Medicinal Chemistry