Abstract
The Langmuir monolayer technique is one of the methods used to build models of cellular membranes and enables to investigate the interactions of membrane components with other biomolecules. This method has been applied to study the effect of edelfosine - a synthetic alkyl-lysophospholipid analog - on model lipid membranes in order to get insight into its mode of action and selectivity. Edelfosine is mainly known for its anticancer properties, although it is also applied in the treatment of other diseases, like autoimmune, anti-HIV and antiparasitic. In this review we focus on its antitumor activity (although some other aspects of its therapeutic effects are also indicated) and summarize the results obtained so far with use of the monolayer technique. The application of this method evidenced for a key role of cholesterol and membrane rafts in the mechanism of anticancer activity of edelfosine. As regards the selectivity of this drug, the obtained results proved that the difference in fluidity of tumor versus normal cell membrane is important but probably not the only factor determining an easier incorporation of edelfosine into cancer cells. Further studies show that edelfosine is of strong affinity to gangliosides, which may be considered as molecules targeting edelfosine into cancer cell membrane.
Keywords: Edelfosine, interactions, langmuir monolayers, model lipids membranes.
Anti-Cancer Agents in Medicinal Chemistry
Title:Edelfosine in Membrane Environment - the Langmuir Monolayer Studies
Volume: 14 Issue: 4
Author(s): Patrycja Dynarowicz-Latka and Katarzyna Hac-Wydro
Affiliation:
Keywords: Edelfosine, interactions, langmuir monolayers, model lipids membranes.
Abstract: The Langmuir monolayer technique is one of the methods used to build models of cellular membranes and enables to investigate the interactions of membrane components with other biomolecules. This method has been applied to study the effect of edelfosine - a synthetic alkyl-lysophospholipid analog - on model lipid membranes in order to get insight into its mode of action and selectivity. Edelfosine is mainly known for its anticancer properties, although it is also applied in the treatment of other diseases, like autoimmune, anti-HIV and antiparasitic. In this review we focus on its antitumor activity (although some other aspects of its therapeutic effects are also indicated) and summarize the results obtained so far with use of the monolayer technique. The application of this method evidenced for a key role of cholesterol and membrane rafts in the mechanism of anticancer activity of edelfosine. As regards the selectivity of this drug, the obtained results proved that the difference in fluidity of tumor versus normal cell membrane is important but probably not the only factor determining an easier incorporation of edelfosine into cancer cells. Further studies show that edelfosine is of strong affinity to gangliosides, which may be considered as molecules targeting edelfosine into cancer cell membrane.
Export Options
About this article
Cite this article as:
Dynarowicz-Latka Patrycja and Hac-Wydro Katarzyna, Edelfosine in Membrane Environment - the Langmuir Monolayer Studies, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (4) . https://dx.doi.org/10.2174/1871520614666140309230722
DOI https://dx.doi.org/10.2174/1871520614666140309230722 |
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
-
Plant Glycosides and Aglycones Displaying Antiproliferative and Antitumour Activities – A Review
Current Bioactive Compounds Encapsulation of Imatinib in Targeted KIT-5 Nanoparticles for Reducing its Cardiotoxicity and Hepatotoxicity
Anti-Cancer Agents in Medicinal Chemistry Pathobiology and Prevention of Cancer Chemotherapy-Induced Bone Growth Arrest, Bone Loss, and Osteonecrosis
Current Molecular Medicine Overcoming the Drug Resistance Problem with Second-Generation Tyrosine Kinase Inhibitors: From Enzymology to Structural Models
Current Medicinal Chemistry Protein Kinase B/AKT and Focal Adhesion Kinase: Two Close Signaling Partners in Cancer
Anti-Cancer Agents in Medicinal Chemistry Functional Nanoplatforms for Enhancement of Chemotherapeutic Index
Anti-Cancer Agents in Medicinal Chemistry Ribonucleotide Reductase: A Critical Enzyme for Cancer Chemotherapy and Antiviral Agents
Recent Patents on Anti-Cancer Drug Discovery Adeno-Associated Virus-Mediated Gene Transfer in Hematopoietic Stem/Progenitor Cells as a Therapeutic Tool
Current Gene Therapy T Cell Receptor Bias in Humans
Current Immunology Reviews (Discontinued) State of the Art of the Therapeutic Perspective of Sorafenib Against Hematological Malignancies
Current Medicinal Chemistry The Biological Effects of Diagnostic Cardiac Imaging
Current Pharmaceutical Design Transient Abnormal Myelopoiesis in Down’s Syndrome - A Diagnostic Dilemma
Applied Clinical Research, Clinical Trials and Regulatory Affairs Cancer Stem Cells in Prostate Cancer Chemoresistance
Current Cancer Drug Targets Transport of Nucleoside Analogs Across the Plasma Membrane: A Clue to Understanding Drug-Induced Cytotoxicity
Current Drug Metabolism Clinical Applications and Biosafety of Human Adult Mesenchymal Stem Cells
Current Pharmaceutical Design Novel Lipid and Polymeric Materials as Delivery Systems for Nucleic Acid Based Drugs
Current Drug Metabolism Plasticity and Therapeutic Potential of Mesenchymal Stem Cells in the Nervous System
Current Pharmaceutical Design NMN/NaMN Adenylyltransferase (NMNAT) and NAD Kinase (NADK) Inhibitors: Chemistry and Potential Therapeutic Applications
Current Medicinal Chemistry Molecular Aspects of FKBP51 that Enable Melanoma Dissemination
Current Molecular Pharmacology Pharmacological and Clinical Studies on Purine Nucleoside Analogs- New Anticancer Agents
Mini-Reviews in Medicinal Chemistry