Abstract
Saponins enhance the cytotoxicity of the type I ribosome-inactivating protein (RIP-I) saporin. In the present study, the synergistic cytotoxicity of nine newly isolated gypsogenin-containing saponins from Gypsophila trichotoma in combination with RIP-I was evaluated in vitro and used to derive a quantitative structure – activity relationship (QSAR). The QSAR model distinguished two important structural features of the studied saponins necessary for their cytotoxicity enhancing activity: the branched trisaccharide moiety attached to C-3 should contain one xylose residue instead of an arabinose and the branched tetrasaccharide at C-28 should contain one acetyl group attached to the glucose residue.
Keywords: Cancer, cytotoxicity, saponins, saporin, targeted anticancer therapy, QSAR, PLS.
Letters in Drug Design & Discovery
Title:Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers
Volume: 12 Issue: 3
Author(s): Reneta Gevrenova, Alexander Weng, Laurence Voutguenne-Nazabadioko, Mayank Thakur and Irini Doytchinova
Affiliation:
Keywords: Cancer, cytotoxicity, saponins, saporin, targeted anticancer therapy, QSAR, PLS.
Abstract: Saponins enhance the cytotoxicity of the type I ribosome-inactivating protein (RIP-I) saporin. In the present study, the synergistic cytotoxicity of nine newly isolated gypsogenin-containing saponins from Gypsophila trichotoma in combination with RIP-I was evaluated in vitro and used to derive a quantitative structure – activity relationship (QSAR). The QSAR model distinguished two important structural features of the studied saponins necessary for their cytotoxicity enhancing activity: the branched trisaccharide moiety attached to C-3 should contain one xylose residue instead of an arabinose and the branched tetrasaccharide at C-28 should contain one acetyl group attached to the glucose residue.
Export Options
About this article
Cite this article as:
Gevrenova Reneta, Weng Alexander, Voutguenne-Nazabadioko Laurence, Thakur Mayank and Doytchinova Irini, Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers, Letters in Drug Design & Discovery 2015; 12 (3) . https://dx.doi.org/10.2174/1570180811666140915221432
DOI https://dx.doi.org/10.2174/1570180811666140915221432 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Glutamate Receptor Agonists: Stereochemical Aspects
Current Topics in Medicinal Chemistry Matrine: Bioactivities and Structural Modifications
Current Topics in Medicinal Chemistry Pharmacological Activities and Therapeutic Potential of Kaempferitrin in Medicine for the Treatment of Human Disorders: A Review of Medicinal Importance and Health Benefits
Cardiovascular & Hematological Disorders-Drug Targets Amyloid Beta Peptide 1-40 Stimulates the Na+ / Ca2+ Exchange Activity of SNCX
Current Neurovascular Research P38 MAPK Contributes to Resistance and Invasiveness of HER2- Overexpressing Breast Cancer
Current Medicinal Chemistry The Role of Glioma Microenvironment in Immune Modulation: Potential Targets for Intervention
Letters in Drug Design & Discovery Surface Markers of Cancer Stem Cells in Solid Tumors
Current Stem Cell Research & Therapy Advances in α(v)β(3) Integrin-Targeting Cancer Therapy and Imaging with Radiolabeled RGD Peptides
Current Radiopharmaceuticals A Review on Chitosan in Drug Delivery for Treatment of Neurological and Psychiatric Disorders
Current Pharmaceutical Biotechnology Passive and Active Tumour Targeting with Nanocarriers
Current Drug Discovery Technologies Recent Trends of Biocompatible and Biodegradable Nanoparticles in Drug Delivery: A Review
Current Medicinal Chemistry Vasculogenic and Angiogenic Pathways in Moyamoya Disease
Current Medicinal Chemistry Redox Environment and its Meaning for Breast Cancer Cells Fate
Current Cancer Drug Targets Advances in Characterization of Neuroprotective Peptide, Humanin
Current Medicinal Chemistry Can γH2AX be Used to Personalise Cancer Treatment?
Current Molecular Medicine Molecular Pharmacology of Malignant Pleural Mesothelioma: Challenges and Perspectives From Preclinical and Clinical Studies
Current Drug Targets Advances in Transient Receptor Potential Vanilloid-2 Channel Expression and Function in Tumor Growth and Progression
Current Protein & Peptide Science Cancer Stem Cells: A New Paradigm for Understanding Tumor Growth and Progression and Drug Resistance
Current Medicinal Chemistry Transposons for Gene Therapy!
Current Gene Therapy Modified cAMP Derivatives: Powerful Tools in Heart Research
Current Medicinal Chemistry