Abstract
Description: Two new ruthenium(II) complexes containing guanidinium as ligands, [Ru(dip)2 (L1)]3+ (Ru1) and [Ru(dip)2(L2)]3+ (Ru2) (dip=4,7-diphenyl-1,10-phenanthroline; L1=1-(4-(1H-imidazo[4,5- f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation; L2 = 1-(3-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl) phenyl)guanidine cation) have been synthesized and characterized. Both complexes display higher cytotoxicity against several cancer cell lines compared to cisplatin and are less cytotoxic on the nontumorigenic cell line LO2. Intracellular distribution studies show that these complexes are selectively localized in the cytoplasm.
Findings: Further analysis revealed that Ru1 and Ru2 had no obvious effects on the cell cycle and induced apoptosis in HeLa cells via the mitochondrial pathway, which involved reactive oxygen species (ROS) accumulation, mitochondrial dysfunction, and Bcl-2 family member activation. Taken together, the two complexes have the potential to be utilized as anticancer agents.
Keywords: Synthesis, Ru(II) complexes, cytotoxicity, apoptosis, protein, tumor cell.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis, Characterization, and Inducing Tumor Cell Apoptosis of Two Ru(II) Complexes Containing Guanidinium as Ligands
Volume: 18 Issue: 1
Author(s): Jing Sun*, Wen-Xiu Chen, Xing-Dong Song, Shu-Fen He, Jia-Xi Chen, Jun Mei, Xiao-Xian Zhu and Tie Wu
Affiliation:
- School of Pharmacy, Guangdong Medical University, Dongguan, 523808,China
Keywords: Synthesis, Ru(II) complexes, cytotoxicity, apoptosis, protein, tumor cell.
Abstract: Description: Two new ruthenium(II) complexes containing guanidinium as ligands, [Ru(dip)2 (L1)]3+ (Ru1) and [Ru(dip)2(L2)]3+ (Ru2) (dip=4,7-diphenyl-1,10-phenanthroline; L1=1-(4-(1H-imidazo[4,5- f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation; L2 = 1-(3-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl) phenyl)guanidine cation) have been synthesized and characterized. Both complexes display higher cytotoxicity against several cancer cell lines compared to cisplatin and are less cytotoxic on the nontumorigenic cell line LO2. Intracellular distribution studies show that these complexes are selectively localized in the cytoplasm.
Findings: Further analysis revealed that Ru1 and Ru2 had no obvious effects on the cell cycle and induced apoptosis in HeLa cells via the mitochondrial pathway, which involved reactive oxygen species (ROS) accumulation, mitochondrial dysfunction, and Bcl-2 family member activation. Taken together, the two complexes have the potential to be utilized as anticancer agents.
Export Options
About this article
Cite this article as:
Sun Jing*, Chen Wen-Xiu, Song Xing-Dong , He Shu-Fen, Chen Jia-Xi, Mei Jun, Zhu Xiao-Xian and Wu Tie , Synthesis, Characterization, and Inducing Tumor Cell Apoptosis of Two Ru(II) Complexes Containing Guanidinium as Ligands, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (1) . https://dx.doi.org/10.2174/1871520617666170419122056
DOI https://dx.doi.org/10.2174/1871520617666170419122056 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- 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
Related Articles
-
Effects of Extracellular Matrix and Integrin Interactions on Airway Smooth Muscle Phenotype and Function: It Takes Two to Tango!
Current Respiratory Medicine Reviews Applications of Metabonomics in Pesticide Toxicology
Current Drug Metabolism Lectin Techniques for Glycoproteomics
Current Proteomics Testicular Germ Cell Tumors: A Paradigm for the Successful Treatment of Solid Tumor Stem Cells
Current Cancer Therapy Reviews Chondroitin Sulfate Glycosaminoglycans for CNS Homeostasis-Implications for Material Design
Current Medicinal Chemistry Distinct Epigenetic Reprogramming, Mitochondrial Patterns, Cellular Morphology, and Cytotoxicity after Bee Venom Treatment
Recent Patents on Anti-Cancer Drug Discovery A Review of Ensemble Methods in Bioinformatics
Current Bioinformatics A Rapid and Sensitive HPLC-FLD Method for the Determination of Retinol and Vitamin E Isomers in Human Serum
Current Pharmaceutical Analysis The Effect of Protein Restriction in the In Vitro Metabolism of Albendazole in Rats
Drug Metabolism Letters Assays for Eukaryotic Cell Chemotaxis
Combinatorial Chemistry & High Throughput Screening Modulation of Signaling Enhances the Efficacy of the Combination of Satraplatin and Erlotinib
Current Drug Targets Live Impedance Measurements and Time-lapse Microscopy Observations of Cellular Adhesion, Proliferation and Migration after Ionizing Radiation
Current Pharmaceutical Biotechnology Activated Surfaces for Laser Desorption Mass Spectrometry: Application for Peptide and Protein Analysis
Current Pharmaceutical Design Electrochemical DNA Biosensors in Drug Analysis
Current Pharmaceutical Analysis When Does Food Refusal Require Professional Intervention?
Current Nutrition & Food Science Four Major Factors Regulate Phosphatidylinositol 3-kinase Signaling Pathway in Cancers Induced by Infection of Human Papillomaviruses
Current Medicinal Chemistry Imaging Reporters and Multimodal Molecular Bio-Imaging: A Database of Available Probes for Multi-Modality Bio-Imaging of Reporter Gene Expression
Recent Patents on Medical Imaging Pharmacokinetic and Metabolism Determinants of Fluoropyrimidines and Oxaliplatin Activity in Treatment of Colorectal Patients
Current Drug Metabolism Simultaneous Estimation of Artemisinin and Dexamethasone in Nanodispersions and Assessment of Ex-vivo Corneal Transport Study by RP- HPLC
Current Pharmaceutical Analysis Sodium Dependent Multivitamin Transporter (SMVT): A Potential Target for Drug Delivery
Current Drug Targets