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
-
Angiogenesis Imaging Using 68Ga-RGD PET: Preliminary Report from Seoul National University Hospital
Current Medical Imaging Photodynamic Therapy: The Light Treatment for Cutaneous Non- Melanoma Malignancies
Current Cancer Therapy Reviews Engineered Polymer Nanoplatforms for Targeted Tumor Cells and Controlled Release Cargos to Enhance Cancer Treatment
Current Medicinal Chemistry Molecular Chaperone ORP150 in ER Stress–related Diseases
Current Pharmaceutical Design Anticancer Vitamin K3 Analogs: A Review
Anti-Cancer Agents in Medicinal Chemistry Inhibitors of Cyclin Dependent Kinases: Useful Targets for Cancer Treatment
Current Cancer Drug Targets Tumour-Derived Glutamate: Linking Aberrant Cancer Cell Metabolism to Peripheral Sensory Pain Pathways
Current Neuropharmacology OX40 and OX40L Interaction in Cancer
Current Medicinal Chemistry Glycosylation Pathways as Drug Targets for Cancer: Glycosidase Inhibitors
Mini-Reviews in Medicinal Chemistry Positron Emission Tomography Radiopharmaceuticals for Sex Steroid Hormone Receptor Imaging
Current Medicinal Chemistry Targeting Mitochondria in Fighting Cancer
Current Pharmaceutical Design Management of Antineutrophil Cytoplasmic Antibody Associated Vasculitis
Current Immunology Reviews (Discontinued) The Use of Biomarkers for Bladder Cancer Diagnosis and Surveillance
Mini-Reviews in Medicinal Chemistry Pharmacology of TRP Channels in the Vasculature
Current Vascular Pharmacology COX Selectivity and Animal Models for Colon Cancer
Current Pharmaceutical Design Pharmacokinetic Profiles of Anticancer Herbal Medicines in Humans and the Clinical Implications
Current Medicinal Chemistry PET Tracers Based on Zirconium-89
Current Radiopharmaceuticals Sorafenib (BAY 43-9006) in Hepatocellular Carcinoma Patients: From Discovery to Clinical Development
Current Medicinal Chemistry TRP Channels as Therapeutic Targets in Kidney Disease and Hypertension
Current Topics in Medicinal Chemistry Recent Advances and Challenges in Steroid Metabolomics for Biomarker Discovery
Current Medicinal Chemistry