Abstract
This review summarizes the current knowledge of the regulatory role of pure anthocyans in cellular signaling pathways and gene expression. The molecular basis for anthocyans pharmacological activity includes the regulation of plethora of mechanisms mainly involved in: (1) suppression of the inflammatory response through targeting the phospholipase A2 and PI3K/Akt and NF-κB pathways, (2) protection from cardiovascular disease by exerting (i) antihypertensive and endothelium-protective activity through targeting the Akt/eNOS and ACE pathways (ii) antiatherogenic activity through targeting NF-κB mediated VCAM and ICAM expression, (3) growth/differentiation control and tumor suppression by exerting (i) anticancerogenic activity through targeting the EGF and HGF signaling pathways (ii) tumor anti-invasive activity through targeting the VEGF signaling pathway and ECM degrading enzymes (iii) cell cycle arrest and induction of apoptosis through the JNK/p38 MAPK mediated caspase activation (iv) modulation of chemotherapeutic efficacy by affecting resistance to anticancer drugs, (4) reduction of diabetes incidence through modulation of insulin sensitivity and glucose utilization, (5) neuroprotection through amelioration of oxidative stress and Aβ deposition, and (6) hepatoprotective activity through interference with TNF-α and TGF-β in the liver. The estrogen-like activity of anthocyans could be utilized in cancer and hormone-replacement therapy. These data provide a concise insight into molecular mechanisms of protective and therapeutic activity of anthocyans in various pathological conditions, which may not be attributed solely to their antioxidant activity but also to direct blockage of signaling pathways. Structure-activity analysis reveals that the number of hydroxyl groups and presence of sugar moiety are crucial for their specific modulatory actions.
Keywords: Anthocyanins, anthocyanidins, signaling pathway, inflammation, cancer, cardiovascular disease, diabetes mellitus, neuronal, damage, liver fibrosis, neuronal damage
Current Medicinal Chemistry
Title: The Molecular Basis for the Pharmacological Activity of Anthocyans
Volume: 18 Issue: 29
Author(s): R. Domitrovic
Affiliation:
Keywords: Anthocyanins, anthocyanidins, signaling pathway, inflammation, cancer, cardiovascular disease, diabetes mellitus, neuronal, damage, liver fibrosis, neuronal damage
Abstract: This review summarizes the current knowledge of the regulatory role of pure anthocyans in cellular signaling pathways and gene expression. The molecular basis for anthocyans pharmacological activity includes the regulation of plethora of mechanisms mainly involved in: (1) suppression of the inflammatory response through targeting the phospholipase A2 and PI3K/Akt and NF-κB pathways, (2) protection from cardiovascular disease by exerting (i) antihypertensive and endothelium-protective activity through targeting the Akt/eNOS and ACE pathways (ii) antiatherogenic activity through targeting NF-κB mediated VCAM and ICAM expression, (3) growth/differentiation control and tumor suppression by exerting (i) anticancerogenic activity through targeting the EGF and HGF signaling pathways (ii) tumor anti-invasive activity through targeting the VEGF signaling pathway and ECM degrading enzymes (iii) cell cycle arrest and induction of apoptosis through the JNK/p38 MAPK mediated caspase activation (iv) modulation of chemotherapeutic efficacy by affecting resistance to anticancer drugs, (4) reduction of diabetes incidence through modulation of insulin sensitivity and glucose utilization, (5) neuroprotection through amelioration of oxidative stress and Aβ deposition, and (6) hepatoprotective activity through interference with TNF-α and TGF-β in the liver. The estrogen-like activity of anthocyans could be utilized in cancer and hormone-replacement therapy. These data provide a concise insight into molecular mechanisms of protective and therapeutic activity of anthocyans in various pathological conditions, which may not be attributed solely to their antioxidant activity but also to direct blockage of signaling pathways. Structure-activity analysis reveals that the number of hydroxyl groups and presence of sugar moiety are crucial for their specific modulatory actions.
Export Options
About this article
Cite this article as:
Domitrovic R., The Molecular Basis for the Pharmacological Activity of Anthocyans, Current Medicinal Chemistry 2011; 18 (29) . https://dx.doi.org/10.2174/092986711797287601
DOI https://dx.doi.org/10.2174/092986711797287601 |
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
-
The Pathogenic Role of Persistent Milk Signaling in mTORC1- and Milk- MicroRNA-Driven Type 2 Diabetes Mellitus
Current Diabetes Reviews Outpatient Treatment of Hemorrhoidal Disease: The Alternative Way to Treat Hemorrhoidal Disease in a Simple, Safe and Effective Manner
Reviews on Recent Clinical Trials Metabolic Syndrome, Mild Cognitive Impairment and Dementia
Current Alzheimer Research Aldose Reductase / Polyol Inhibitors for Diabetic Retinopathy
Current Pharmaceutical Biotechnology Advanced Glycation End Products as Environmental Risk Factors for the Development of Type 1 Diabetes
Current Drug Targets Erratum
Current Pharmaceutical Design Glucose Transport Regulators
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Role of Glycogen Synthase Kinase-3 in Insulin Resistance and Type 2 Diabetes
Current Drug Targets A Review of Biomarkers in Mood and Psychotic Disorders: A Dissection of Clinical vs. Preclinical Correlates
Current Neuropharmacology Lagenaria siceraria: A Potential Source of Anti-Hyperlipidemic and Other Pharmacological Agents
Current Nutrition & Food Science Angiotensin II in Type 2 Diabetes Mellitus
Current Protein & Peptide Science Preventive Antiretroviral Therapy in Non-Thalassemia Carrier Infants Exposed to Mother-to-Child Transmission of HIV Decreases Cord and After Delivery Red Blood Production without Altering the Development of Hemoglobin
Current HIV Research The Anti-Inflammatory Effects of Statins on Coronary Artery Disease: An Updated Review of the Literature
Current Cardiology Reviews Endoplasmic Reticulum Stress and Bipolar Disorder - Almost Forgotten Therapeutic Drug Targets in the Unfolded Protein Response Pathway Revisited
CNS & Neurological Disorders - Drug Targets Challenges with Insulin Use Among Patients with Type 2 Diabetes Mellitus: Focus on a Tertiary Healthcare Setting in South-East Nigeria
Current Diabetes Reviews Early Life Programming of Obesity: The Impact of the Perinatal Environment on the Development of Obesity and Metabolic Dysfunction in the Offspring.
Current Diabetes Reviews Intestinal Microbiota: A Regulator of Intestinal Inflammation and Cardiac Ischemia?
Current Drug Targets Estrogens and Progression of Diabetic Kidney Damage
Current Diabetes Reviews Type 2 Diabetes, Insulin Secretion and β-Cell Mass
Current Molecular Medicine Drug Transport Across the Placenta
Current Pharmaceutical Biotechnology