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
-
Targeting Indoleamine 2,3-dioxygenase (IDO) to Counteract Tumour- Induced ImmuneDysfunction: From Biochemistry to Clinical Development
Endocrine, Metabolic & Immune Disorders - Drug Targets Cachexia and Herbal Medicine: Perspective
Current Pharmaceutical Design Replicative Oncolytic Herpes Simplex Viruses in Combination Cancer Therapies
Current Gene Therapy Inflammatory Cytokines Pathways as Potential Therapeutic Targets for Gastric Cancer
Current Cancer Therapy Reviews Immune Modulation by Ionizing Radiation and its Implications for Cancer Immunotherapy
Current Pharmaceutical Design Laminin-332-Integrin Interaction: A Target For Cancer Therapy?
Current Medicinal Chemistry Cyclophilins in Atherosclerosis: A New Therapeutic Target?
Current Pharmaceutical Design Nitric Oxide in Cancer Therapeutics: Interaction with Cytotoxic Chemotherapy
Current Pharmaceutical Design Role of Cardiolipin in Mitochondrial Diseases and Apoptosis
Current Medicinal Chemistry Advancing Drug Therapy for Brain Tumours: A Current Review of the Pro-inflammatory Peptide Substance P and its Antagonists as Anti-cancer Agents
Recent Patents on CNS Drug Discovery (Discontinued) Human Amniotic Fluid Stem Cells as an Attractive Tool for Clinical Applications
Current Stem Cell Research & Therapy Targeting the JAK/STAT Signaling Pathway for Breast Cancer
Current Medicinal Chemistry PPARγ and Early Human Placental Development
Current Medicinal Chemistry Stimuli-Responsive Nanoparticles for siRNA Delivery
Current Pharmaceutical Design Brain Segmentation Using Deep Neural Networks
International Journal of Sensors, Wireless Communications and Control Multi-parametric MR Imaging Biomarkers Associated to Clinical Outcomes in Gliomas: A Systematic Review
Current Medical Imaging Molecular Probes for Malignant Melanoma Imaging
Current Pharmaceutical Biotechnology Current Targeting Strategies for Adenovirus Vectors in Cancer Gene Therapy
Current Cancer Drug Targets Perspectives on Brain-Targeting Drug Delivery Systems
Current Pharmaceutical Biotechnology PET and SPECT Imaging of Tumor Biology: New Approaches Towards Oncology Drug Discovery and Development
Current Computer-Aided Drug Design