Abstract
Triterpenes have been reported to induce cell death. One relevant group of this family of compounds is cucurbitacins, which have been studied as inducers of apoptosis in various cancer cell lines. The most significant mechanisms with regard to the apoptotic effects of cucurbitacins are their ability to modify transcriptional activities via nuclear factors or genes and their capability to activate or inhibit pro- or anti-apoptotic proteins. Still, while the majority of studies on these compounds have dealt with their apoptotic effects on cancer cell lines, several research groups have also explored their anti-inflammatory activities. In general, cucurbitacins are considered to be selective inhibitors of the JAK/STAT pathways; however, other mechanisms may be implicated in their apoptotic effects, including the MAPK pathway (known to be important for cancer cell proliferation and survival), PARP cleavage, expression of active caspase-3, decreased pSTAT3 and JAK3 levels, as well as decreases in various downstream STAT3 targets such as Mcl-1, Bcl-2, Bcl-xL, and cyclin D3, all of which are implicated in apoptosis and the cell cycle. Taking all these effects into account, cucurbitacins may prove useful in the treatment of different kinds of cancers, especially when used with other cytostatic agents.
Keywords: Cucurbitacins, cell death, apoptosis, JAK-STAT, cancer, triterpenes, transcriptional activities, anti-inflammatory activities, MAPK pathway, cytostatic agents
Current Pharmaceutical Design
Title:Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds
Volume: 18 Issue: 12
Author(s): J. L. Rios, I. Andujar, J. M. Escandell, R. M. Giner, M. C. Recio
Affiliation:
Keywords: Cucurbitacins, cell death, apoptosis, JAK-STAT, cancer, triterpenes, transcriptional activities, anti-inflammatory activities, MAPK pathway, cytostatic agents
Abstract: Triterpenes have been reported to induce cell death. One relevant group of this family of compounds is cucurbitacins, which have been studied as inducers of apoptosis in various cancer cell lines. The most significant mechanisms with regard to the apoptotic effects of cucurbitacins are their ability to modify transcriptional activities via nuclear factors or genes and their capability to activate or inhibit pro- or anti-apoptotic proteins. Still, while the majority of studies on these compounds have dealt with their apoptotic effects on cancer cell lines, several research groups have also explored their anti-inflammatory activities. In general, cucurbitacins are considered to be selective inhibitors of the JAK/STAT pathways; however, other mechanisms may be implicated in their apoptotic effects, including the MAPK pathway (known to be important for cancer cell proliferation and survival), PARP cleavage, expression of active caspase-3, decreased pSTAT3 and JAK3 levels, as well as decreases in various downstream STAT3 targets such as Mcl-1, Bcl-2, Bcl-xL, and cyclin D3, all of which are implicated in apoptosis and the cell cycle. Taking all these effects into account, cucurbitacins may prove useful in the treatment of different kinds of cancers, especially when used with other cytostatic agents.
Export Options
About this article
Cite this article as:
J. L. Rios, I. Andujar, J. M. Escandell, R. M. Giner, M. C. Recio , Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds , Current Pharmaceutical Design 2012; 18 (12) . https://dx.doi.org/10.2174/138161212799958549
DOI https://dx.doi.org/10.2174/138161212799958549 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Manipulation of Glycolysis in Malignant Tumors: Fantasy or Therapy?
Current Medicinal Chemistry Targeting Cytotoxic Conjugates of Somatostatin, Luteinizing Hormone- Releasing Hormone and Bombesin to Cancers Expressing Their Receptors: A “Smarter” Chemotherapy
Current Pharmaceutical Design Contrast Functions of αA- and αB-Crystallins in Cancer Development
Current Molecular Medicine Long Non-coding RNA HOTAIR Promotes Parkinson's Disease Induced by MPTP Through up-regulating the Expression of LRRK2
Current Neurovascular Research Osteopontin is a Prognostic Factor in Patients with Advanced Gastric Cancer
Combinatorial Chemistry & High Throughput Screening Ent-11α-Hydroxy-15-Oxo-Kaur-16-en-19-Oic-Acid Induces Apoptosis of Human Malignant Cancer Cells
Current Drug Targets Development and Applications of Optical Imaging Techniques in Cancer Diagnosis: Diffuse Optical Tomography and Microendoscopy
Current Medical Imaging Regioselective Synthesis of Biologically Important Scaffold Spiro [Indole- Perimidines]: An Antitumor Agents
Letters in Organic Chemistry ANTI-ADHESION Evolves To a Promising Therapeutic Concept in Oncology
Current Medicinal Chemistry Novel Drug-Induced Pulmonary Complications in Cancer Patients You Can Save Life!
Current Respiratory Medicine Reviews Melanoma Immunotherapy: Past, Present, and Future
Current Pharmaceutical Design The Potential Role of Claudins in Regulation of Metastasis and Development of Drug Resistance in Breast Cancer
Clinical Cancer Drugs Pro-Oncogenic Cell Signaling Machinery as a Target for Oncolytic Viruses
Current Pharmaceutical Biotechnology The Effect of Proton Pump Inhibitors on the Human Microbiota
Current Drug Metabolism Oxidative stress in carcinogenesis: new synthetic compounds with dual effects upon free radicals and cancer.
Current Medicinal Chemistry Antioxidant and Anti-proliferative Activities of Astaxanthin Extracted from the Shell Waste of Deep-water Pink Shrimp (Parapenaeus longirostris)
The Natural Products Journal HLA Class I Expression, Tumor Escape and Cancer Progression
Current Cancer Therapy Reviews Terpenes with Antitumor Activity: A Patent Review
Recent Patents on Anti-Cancer Drug Discovery Histone Deacetylase Inhibitors: A New Wave of Molecular Targeted Anticancer Agents
Recent Patents on Anti-Cancer Drug Discovery Cisplatin Properties in a Nanobiotechnological Approach to Cancer: A Mini-Review
Current Cancer Drug Targets