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
-
Growth Differentiation Factor-15 as a Biomarker of Obese Pre-diabetes and Type 2 Diabetes Mellitus in Indian Subjects: A Case-control Study
Current Diabetes Reviews The PIK3CA Gene as a Mutated Target for Cancer Therapy
Current Cancer Drug Targets Protein Factors Mediating Selenoprotein Synthesis
Current Protein & Peptide Science Synthesis and Evaluation of 99mTc Chelate-conjugated Bevacizumab
Current Radiopharmaceuticals Pharmacotherapies to Manage Bone Loss-Associated Diseases: A Quest for the Perfect Benefit-to-Risk Ratio
Current Medicinal Chemistry Incidentally Discovered Thyroid Nodules by Routine Magnetic Resonance Imaging of the Cervical Spine: Incidence and Clinical Significance
Current Medical Imaging The PAX8 / PPARγ Fusion Oncogene as a Potential Therapeutic Target in Follicular Thyroid Carcinoma
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Tyrosine Kinase Receptors Signaling Revealed by Global Expression Profiles: Implications for Cancer Biology
Current Genomics An overview of ABC and SLC Drug Transporter Gene Regulation
Current Drug Metabolism Immunomodulatory Activities of Glucocorticoids: Insights from Transgenesis and Gene Targeting
Current Pharmaceutical Design CAR, The Continuously Advancing Receptor, in Drug Metabolism and Disease
Current Drug Metabolism GLP-1 Agonists Exenatide and Liraglutide: A Review About Their Safety and Efficacy
Current Clinical Pharmacology Treatment of Estrogen Receptor-Positive Breast Cancer
Current Medicinal Chemistry Effect on Serum Uric Acid Levels of Drugs Prescribed for Indications other than Treating Hyperuricaemia
Current Pharmaceutical Design Advancements in Predictive In Silico Models for ADME
Current Chemical Biology Impact of Antihypertensive Drug Use on Bone Mineral Density and Osteoporotic Fracture - From an Epidemiological Perspective
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Prediction of the Ebola Virus Infection Related Human Genes Using Protein-Protein Interaction Network
Combinatorial Chemistry & High Throughput Screening The Importance of Selenium Biofortification in Food Crops
Current Nutrition & Food Science Novel Oral Anticoagulants: Recommendations for Patient Evaluation, Treatment Initiation, Follow-up and Perioperative Management
Cardiovascular & Hematological Disorders-Drug Targets ATP Synthase: A Molecular Therapeutic Drug Target for Antimicrobial and Antitumor Peptides
Current Medicinal Chemistry