Abstract
Background: Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat several diseases, among whom cancer. Triterpenes are secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by several authors. Furthermore, during recent years synthetic triterpenoid derivatives have also been developed to implement potency and efficacy of starting compounds, allowing the obtainment of new agents having promising anticancer activity.
Objective: In this review we report the latest results regarding anticancer activity of some of the most studied triterpenes in the field, as well as of their semi-synthetic derivatives, with the aim to summarize the role of triterpenes as molecular leads for the development of new classes of antitumor agents.
Methods: We focused on the most recent literature regarding triterpenes in cancer treatment, highlighting the potential of developing new drugs starting from these natural compounds.
Conclusion: Several “old” triterpenes as ursolic, betulinic and oleanolic acids were recently reconsidered as model compounds for the development of innovative anticancer agents. Their activity against proteins involved in tumor development enhances the opportunity to exploit these compounds as new multi-target therapeutic agents. Furthermore, the possibility to synthetize new compounds from their natural-occurring structures could be an alternative to overcome cellular resistance to drugs and could improve their therapeutic efficacy.
Keywords: Triterpenes, cancer, bioactive secondary metabolites, antitumor activity, therapeutic agents, synthetic triterpenoids.
Current Medicinal Chemistry
Title:Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer
Volume: 25 Issue: 10
Author(s): Gregorio Peron*, Giovanni Marzaro and Stefano Dall`Acqua
Affiliation:
- Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo 5, 35131 Padova,Italy
Keywords: Triterpenes, cancer, bioactive secondary metabolites, antitumor activity, therapeutic agents, synthetic triterpenoids.
Abstract: Background: Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat several diseases, among whom cancer. Triterpenes are secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by several authors. Furthermore, during recent years synthetic triterpenoid derivatives have also been developed to implement potency and efficacy of starting compounds, allowing the obtainment of new agents having promising anticancer activity.
Objective: In this review we report the latest results regarding anticancer activity of some of the most studied triterpenes in the field, as well as of their semi-synthetic derivatives, with the aim to summarize the role of triterpenes as molecular leads for the development of new classes of antitumor agents.
Methods: We focused on the most recent literature regarding triterpenes in cancer treatment, highlighting the potential of developing new drugs starting from these natural compounds.
Conclusion: Several “old” triterpenes as ursolic, betulinic and oleanolic acids were recently reconsidered as model compounds for the development of innovative anticancer agents. Their activity against proteins involved in tumor development enhances the opportunity to exploit these compounds as new multi-target therapeutic agents. Furthermore, the possibility to synthetize new compounds from their natural-occurring structures could be an alternative to overcome cellular resistance to drugs and could improve their therapeutic efficacy.
Export Options
About this article
Cite this article as:
Peron Gregorio*, Marzaro Giovanni and Dall`Acqua Stefano , Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer, Current Medicinal Chemistry 2018; 25 (10) . https://dx.doi.org/10.2174/0929867324666170818111933
DOI https://dx.doi.org/10.2174/0929867324666170818111933 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
- Announcements
Related Articles
-
Signal Transduction Therapy Targeting Apoptosis Pathways in Cancers
Current Signal Transduction Therapy Metformin and Energy Metabolism in Breast Cancer: From Insulin Physiology to Tumour-initiating Stem Cells
Current Molecular Medicine Evaluation of Melatonin Effect on Human Breast Cancer Stem Cells Using a Threedimensional Growth Method of Mammospheres
Anti-Cancer Agents in Medicinal Chemistry New Molecular Targets of Anticancer Therapy – Current Status and Perspectives
Current Medicinal Chemistry Nanomedicine as a Strategy for Natural Compound Delivery to Prevent and Treat Cancers
Current Pharmaceutical Design PI3K Inhibitors for Cancer Therapy: What has been Achieved So Far?
Current Medicinal Chemistry MARK1 is a Novel Target for miR-125a-5p: Implications for Cell Migration in Cervical Tumor Cells
MicroRNA Application of Baculovirus-Insect Cell Expression System for Human Therapy
Current Pharmaceutical Biotechnology Chemotherapy Delivery Strategies to the Central Nervous System: neither Optional nor Superfluous
Current Cancer Drug Targets Critical Questions for Preclinical Trials on Safety and Efficacy of Vascular Endothelial Growth Factor-Based Therapeutic Angiogenesis for Ischemic Stroke
CNS & Neurological Disorders - Drug Targets Recent Approaches for Studying the Role of Glia
CNS & Neurological Disorders - Drug Targets Reduction of Oxidative/Nitrosative Stress in Brain and its Involvement in the Neuroprotective Effect of n-3 PUFA in Alzheimer’s Disease
Current Alzheimer Research Double Layered Hydroxides as Potential Anti-Cancer Drug Delivery Agents
Mini-Reviews in Medicinal Chemistry Targeted Tumor Immunotherapy: Are Vaccines the Future of Cancer Treatment?
Current Drug Therapy α-Melanocyte Stimulating Hormone as a Potential Therapy for Alzheimer's Disease
Current Alzheimer Research 1-Cyclohexylpiperazine and 3,3-Dimethylpiperidine Derivatives as Sigma-1 (σ1) and Sigma-2 (σ2) Receptor Ligands: A Review
Central Nervous System Agents in Medicinal Chemistry Regulating TRAIL Receptor-Induced Cell Death at the Membrane: A Deadly Discussion
Recent Patents on Anti-Cancer Drug Discovery Heterocyclic Drug-polymer Conjugates for Cancer Targeted Drug Delivery
Anti-Cancer Agents in Medicinal Chemistry C-glycosyl Flavone from Urginea indica Inhibits Growth and Dissemination of Ehrlich Ascites Carcinoma Cells in Mice
Anti-Cancer Agents in Medicinal Chemistry Molecular Imaging of Brain Tumors Personal Experience and Review of the Literature
Current Molecular Medicine