Abstract
Background: Curcumin, a polyphenol from turmeric, is a dietary phytochemical with a diversity of health benefits including strong anti-tumor effects. Curcumin undergoes a rapid metabolism resulting in a low oral bioavailability. 3, 4-difluorobenzylidene curcumin or (CDF) is a novel fluorinated curcumin analogue which has been shown to be about 3 times more bioavailable than curcumin. This review aimed to summarize the findings of studies related to pharmacokinetic and pharmacological characteristics of CDF. Methods: A systematic literature search was prformed in Scopus and Medline to identify all published articles dealing with CDF. Results: Biodistribution assays have revealed that curcumin is mostly distributed to the heart and lung tissues while CDF is preferentially accumulated in pancreas where its tissue concentrations reach two folds higher than that of curcumin. Moreover, CDF has been reported to possess stronger cytotoxic effects compared with CMN in both monolayer and spheroid cultures of different tumor cell lines including chemo-resistant ones. CDF can promote tumor suppression through multiple mechanisms including inhibition of self-renewal capacity of cancer stem/stem-like cells, clonogenicity invasiveness and angiogenesis of tumor cells, while increasing the sensitivity of cells to chemotherapy. These effects are the results of the modulatory action of CDF on diverse targets, such as miRNAs (miR-21, miR-101, miR-210, miR34a and miR34c), PTEN, CD44, EGFR, EpCAM, EZH2, HIF-1α, and VEGF. Conclusion: This review presents an overview of the findings on metabolism and pharmacological activities of CDF, and also highlights potential opportunities to use this novel curcumin analogue in the treatment of cancer.
Keywords: Antitumor activity, cytotoxicity, Curcuma longa L., fluorination, pharmacokinetics, MicroRNA.
Current Pharmaceutical Design
Title:Difluorinated Curcumin: A Promising Curcumin Analogue with Improved Anti-Tumor Activity and Pharmacokinetic Profile
Volume: 22 Issue: 28
Author(s): Amir Abbas Momtazi and Amirhossein Sahebkar
Affiliation:
Keywords: Antitumor activity, cytotoxicity, Curcuma longa L., fluorination, pharmacokinetics, MicroRNA.
Abstract: Background: Curcumin, a polyphenol from turmeric, is a dietary phytochemical with a diversity of health benefits including strong anti-tumor effects. Curcumin undergoes a rapid metabolism resulting in a low oral bioavailability. 3, 4-difluorobenzylidene curcumin or (CDF) is a novel fluorinated curcumin analogue which has been shown to be about 3 times more bioavailable than curcumin. This review aimed to summarize the findings of studies related to pharmacokinetic and pharmacological characteristics of CDF. Methods: A systematic literature search was prformed in Scopus and Medline to identify all published articles dealing with CDF. Results: Biodistribution assays have revealed that curcumin is mostly distributed to the heart and lung tissues while CDF is preferentially accumulated in pancreas where its tissue concentrations reach two folds higher than that of curcumin. Moreover, CDF has been reported to possess stronger cytotoxic effects compared with CMN in both monolayer and spheroid cultures of different tumor cell lines including chemo-resistant ones. CDF can promote tumor suppression through multiple mechanisms including inhibition of self-renewal capacity of cancer stem/stem-like cells, clonogenicity invasiveness and angiogenesis of tumor cells, while increasing the sensitivity of cells to chemotherapy. These effects are the results of the modulatory action of CDF on diverse targets, such as miRNAs (miR-21, miR-101, miR-210, miR34a and miR34c), PTEN, CD44, EGFR, EpCAM, EZH2, HIF-1α, and VEGF. Conclusion: This review presents an overview of the findings on metabolism and pharmacological activities of CDF, and also highlights potential opportunities to use this novel curcumin analogue in the treatment of cancer.
Export Options
About this article
Cite this article as:
Momtazi Abbas Amir and Sahebkar Amirhossein, Difluorinated Curcumin: A Promising Curcumin Analogue with Improved Anti-Tumor Activity and Pharmacokinetic Profile, Current Pharmaceutical Design 2016; 22 (28) . https://dx.doi.org/10.2174/1381612822666160527113501
DOI https://dx.doi.org/10.2174/1381612822666160527113501 |
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
-
Viral Based Gene Therapy for Prostate Cancer
Current Gene Therapy Biomarkers to Assess the Targeting of DNA Repair Pathways to Augment Tumor Response to Therapy
Current Molecular Medicine Pentacyclic Triterpenoids and Their Saponins with Apoptosis-Inducing Activity
Current Topics in Medicinal Chemistry P2X7 Receptors: Channels, Pores and More
CNS & Neurological Disorders - Drug Targets Intranasal Drug Delivery for Brain Targeting
Current Drug Delivery Chemoresistance in Non-Small Cell Lung Cancer
Current Medicinal Chemistry - Anti-Cancer Agents Diversity-Oriented Synthetic Approaches for Furoindoline: A Review
Current Organic Synthesis Chirality - A New Era of Therapeutics
Mini-Reviews in Medicinal Chemistry Key Questions in Metastasis: New Insights in Molecular Pathways and Therapeutic Implications
Current Pharmaceutical Biotechnology Cancer Prevention with Promising Natural Products: Mechanisms of Action and Molecular Targets
Anti-Cancer Agents in Medicinal Chemistry Development of Specific New ELISA for Bioanalysis of Cetuximab: A Monoclonal Antibody Used for Cancer Immunotherapy
Current Pharmaceutical Analysis Identification of AHSA1 as a Potential Therapeutic Target for Breast Cancer: Bioinformatics Analysis and <i>in vitro</i> Studies
Current Cancer Drug Targets Evolving Novel Chemical Entities for Management of Benign Prostatic Hyperplasia#
Mini-Reviews in Medicinal Chemistry The Canalicular Bile Salt Export Pump BSEP (ABCB11) as a Potential Therapeutic Target
Current Drug Targets Medical Image Processing Technology for Diagnosing and Treating Cancers
Recent Patents on Biomedical Engineering (Discontinued) Targeting Tumor Suppressor p53 for Cancer Therapy: Strategies, Challenges and Opportunities
Current Drug Targets The CLCA Gene Family: Putative Therapeutic Target for Respiratory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Psoriasin, A Multifunctional Player in Different Diseases
Current Protein & Peptide Science MicroRNAs Regulate the Epithelial to Mesenchymal Transition (EMT) in Cancer Progression
MicroRNA NBN Polymorphysms and Cancer Susceptibility: A Systematic Review
Current Genomics