Abstract
Curcuminoids are safe natural yellow pigments used as food coloring agents and traditional drugs with a variety of biological functions such as antitumor, anti-inflammatory and antioxidant activities. Poor oral bioavailability and the low plasma concentration of curcuminoids limited their clinical use, and one of the major reasons is their rapid metabolism in vivo. The predominant metabolic pathways are reduction and conjugation, and some drug metabolizing enzymes such as alcohol dehydrogenase, UDP-glucuronosyltransferases (UGTs) or sulfotransferases (SULTs) involved in the metabolic reactions. Besides the major metabolic pathways, dehydroxylation, cyclization and methylation can also occur in vivo. In addition, more than thirty metabolites of curcuminoids have been identified in biological matrices including the plasma, urine and bile from rats or humans by LC-MS/MS analysis and other methods. Some metabolites such as tetrahydro-curcuminoids have been reported to be active, which may explain how and why curcuminoids with poor oral bioavailability display their effectiveness in vivo. The present review mainly summarizes curcuminoid metabolism and its contribution to the pharmacological effects.
Keywords: Curcuminoid, oral bioavailability, metabolism, tetrahydrocurcumin, pharmacological effects.
Current Drug Metabolism
Title:Curcuminoid Metabolism and its Contribution to the Pharmacological Effects
Volume: 14 Issue: 7
Author(s): Kun Wang and Feng Qiu
Affiliation:
Keywords: Curcuminoid, oral bioavailability, metabolism, tetrahydrocurcumin, pharmacological effects.
Abstract: Curcuminoids are safe natural yellow pigments used as food coloring agents and traditional drugs with a variety of biological functions such as antitumor, anti-inflammatory and antioxidant activities. Poor oral bioavailability and the low plasma concentration of curcuminoids limited their clinical use, and one of the major reasons is their rapid metabolism in vivo. The predominant metabolic pathways are reduction and conjugation, and some drug metabolizing enzymes such as alcohol dehydrogenase, UDP-glucuronosyltransferases (UGTs) or sulfotransferases (SULTs) involved in the metabolic reactions. Besides the major metabolic pathways, dehydroxylation, cyclization and methylation can also occur in vivo. In addition, more than thirty metabolites of curcuminoids have been identified in biological matrices including the plasma, urine and bile from rats or humans by LC-MS/MS analysis and other methods. Some metabolites such as tetrahydro-curcuminoids have been reported to be active, which may explain how and why curcuminoids with poor oral bioavailability display their effectiveness in vivo. The present review mainly summarizes curcuminoid metabolism and its contribution to the pharmacological effects.
Export Options
About this article
Cite this article as:
Wang Kun and Qiu Feng, Curcuminoid Metabolism and its Contribution to the Pharmacological Effects, Current Drug Metabolism 2013; 14 (7) . https://dx.doi.org/10.2174/13892002113149990102
DOI https://dx.doi.org/10.2174/13892002113149990102 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
- 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
-
Insulin Decreases Therapeutic Efficacy in Colon Cancer Cell Line HT29 Via the Activation of the PI3K/Akt Pathway
Current Drug Discovery Technologies Adverse Drug Reactions Related to Drug Administration in Hospitalized Patients
Current Drug Safety Iron Chelators in Medicinal Applications - Chemical Equilibrium Considerations in Pharmaceutical Activity
Current Medicinal Chemistry Shedding Light on Serum Vitamin D Concentrations and the Risk of Rarer Cancers
Anti-Cancer Agents in Medicinal Chemistry Management of the Menopausal Disturbances and Oxidative Stress
Current Pharmaceutical Design Exploiting Significance of Physical Exercise in Prevention of Gastrointestinal Disorders
Current Pharmaceutical Design Emerging Roles for Modulation of microRNA Signatures in Cancer Chemoprevention
Current Cancer Drug Targets Interplay between DNA Methyltransferase 1 and microRNAs During Tumorigenesis
Current Drug Targets EGFR and the Complexity of Receptor Crosstalk in the Cardiovascular System
Current Molecular Medicine Gankyrin Oncoprotein: Structure, Function, and Involvement in Cancer
Current Chemical Biology BRCA2 Dysfunction Promotes Malignant Transformation of Pancreatic Intraepithelial Neoplasia
Anti-Cancer Agents in Medicinal Chemistry The Immune Protective Effect of the Mediterranean Diet against Chronic Low-grade Inflammatory Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Recent Advances in Management of Diabetic Macular Edema
Current Diabetes Reviews Metal Containing Cytostatics and Their Interaction with Cellular Thiol Compounds Causing Chemoresistance
Anti-Cancer Agents in Medicinal Chemistry Prospects of Non-Coding Elements in Genomic DNA Based Gene Therapy
Current Gene Therapy Addressing the Challenge: Current and Future Directions in Ovarian Cancer Therapy
Current Gene Therapy Multiple Functions of Generic Drugs: Future Perspectives of Aureolic Acid Group of Anti-Cancer Antibiotics and Non-Steroidal Anti-Inflammatory Drugs
Mini-Reviews in Medicinal Chemistry Flavopiridol, the First Cyclin-Dependent Kinase Inhibitor: Recent Advances in Combination Chemotherapy
Mini-Reviews in Medicinal Chemistry Fibroblast Activation Protein in Remodeling Tissues
Current Molecular Medicine Potential Health Benefits of Berries
Current Nutrition & Food Science