Abstract
The natural flavonoids as human digestive enzymes, such as α-glucosidase, α-amylase and aldose reductases inhibitors, have attracted great interest among researchers. The objective of this review is to overview the structures required of flavonoids for inhibiting these digestive enzymes. The hydroxylation on rings A and B of flavonoids improved the inhibition against these digestive enzymes. The hydroxylation on A-ring of flavones and isoflavones, especially at C-5 and C-7, significantly enhanced the inhibitory activities against digestive enzymes and the hydroxylation on positions C-3′ and C-4′ of B-ring of flavonoids remarkably improved the inhibition. The hydrogenation of the C2=C3 double bond on flavonoids decreased the inhibitory effects. The glycosylation of hyroxyl group on flavonoids weakened the inhibition against α-amylases and α-glucosidases. The glycosylation on 7-OH and 4'-OH of flavonoids significantly decreased the inhibition for aldose reductases. The glycosylation on 3-OH of flavonoids significantly increased or little affected the inhibition on aldose reductases. The methylation and methoxylation of flavonoids obviously weakened the inhibitory effects against α-amylase. The methylation and methoxylation of the hydroxyl group at C-3, C-3' and C-4' of flavonoids decreased or little affected the inhibitory potency against aldose reductases. And, the methylation and methoxylation of the hydroxyl groups at 5, 6, and 8 significantly increased the inhibitory capacity for aldose reductases. The methylation and methoxylation of flavonoids obviously affected the inhibitory effect for α-glucosidase in vitro depending on the replaced site.
Keywords: Flavonoids, α-glucosidase, α-amylase, Aldose reductase, Structure-activity relationship, isoflavones, apigenin, Soybean, D-sorbitol, α-amylases
Anti-Cancer Agents in Medicinal Chemistry
Title:Structures Required of Flavonoids for Inhibiting Digestive Enzymes
Volume: 12 Issue: 8
Author(s): Hui Cao and Xiaoqing Chen
Affiliation:
Keywords: Flavonoids, α-glucosidase, α-amylase, Aldose reductase, Structure-activity relationship, isoflavones, apigenin, Soybean, D-sorbitol, α-amylases
Abstract: The natural flavonoids as human digestive enzymes, such as α-glucosidase, α-amylase and aldose reductases inhibitors, have attracted great interest among researchers. The objective of this review is to overview the structures required of flavonoids for inhibiting these digestive enzymes. The hydroxylation on rings A and B of flavonoids improved the inhibition against these digestive enzymes. The hydroxylation on A-ring of flavones and isoflavones, especially at C-5 and C-7, significantly enhanced the inhibitory activities against digestive enzymes and the hydroxylation on positions C-3′ and C-4′ of B-ring of flavonoids remarkably improved the inhibition. The hydrogenation of the C2=C3 double bond on flavonoids decreased the inhibitory effects. The glycosylation of hyroxyl group on flavonoids weakened the inhibition against α-amylases and α-glucosidases. The glycosylation on 7-OH and 4'-OH of flavonoids significantly decreased the inhibition for aldose reductases. The glycosylation on 3-OH of flavonoids significantly increased or little affected the inhibition on aldose reductases. The methylation and methoxylation of flavonoids obviously weakened the inhibitory effects against α-amylase. The methylation and methoxylation of the hydroxyl group at C-3, C-3' and C-4' of flavonoids decreased or little affected the inhibitory potency against aldose reductases. And, the methylation and methoxylation of the hydroxyl groups at 5, 6, and 8 significantly increased the inhibitory capacity for aldose reductases. The methylation and methoxylation of flavonoids obviously affected the inhibitory effect for α-glucosidase in vitro depending on the replaced site.
Export Options
About this article
Cite this article as:
Cao Hui and Chen Xiaoqing, Structures Required of Flavonoids for Inhibiting Digestive Enzymes, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (8) . https://dx.doi.org/10.2174/187152012802650110
DOI https://dx.doi.org/10.2174/187152012802650110 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Pleiotropic Effects of Drugs Inhibiting the Renin-Angiotensin-Aldosterone System
Current Pharmaceutical Design HMGB1-Directed Drug Discovery Targeting Cutaneous Inflammatory Dysregulation
Current Drug Metabolism Stem Cell Regenerative Potential Combined with Nanotechnology and Tissue Engineering for Myocardial Regeneration
Current Stem Cell Research & Therapy Antidiabetics: Structural Diversity of Molecules with a Common Aim
Current Medicinal Chemistry Complement and Complement Regulatory Proteins as Potential Molecular Targets for Vascular Diseases
Current Pharmaceutical Design Human Cognitive and Neuro-Psychiatric Bio-Markers in the Cardiac Peri-Operative Patient
Current Molecular Medicine Matrix Metalloproteinases and their Tissue Inhibitors in Diabetes, Atherosclerosis and Prediction of the Cardiovascular Risk
Current Enzyme Inhibition Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Periodontal Disease and Potential Association with Systemic Diseases and Conditions (Mini-review)
Applied Clinical Research, Clinical Trials and Regulatory Affairs Editorial (Thematic Issue: Neuroglia as a Central Element of Neurological Diseases: An Underappreciated Target for Therapeutic Intervention)
Current Neuropharmacology Pitavastatin and 4-Hydroxy-3-Methoxyacetophenone (HMAP) Reduce Cognitive Dysfunction in Vascular Dementia During Experimental Diabetes
Current Neurovascular Research Recent Advances and Patents for Nerve Scaffold Biomaterials and their Use for Local, Non-Viral Delivery of Growth Factors and Nucleic Acids
Recent Patents on Biomedical Engineering (Discontinued) Editorial (Mini-Thematic Issue: Social Media and Smart Technology in Diabetes: - One Small Step…..One Giant Leap.)
Current Diabetes Reviews Contribution of Spinal Cord Oligodendrocytes to Neuroinflammatory Diseases and Pain
Current Medicinal Chemistry Editorial [Hot Topic: Vascular Complications of Diabetes (Executive Editor: Olga I. Stenina)]
Current Pharmaceutical Design Misoprostol Reverse Hippocampal Neuron Cyclooxygenase-2 Downstream Signaling Imbalance in Aluminum-Overload Rats
Current Alzheimer Research New Challenges in CNS Repair: The Immune and Nervous Connection
Current Immunology Reviews (Discontinued) Role of Sulfur Containing Amino Acids as an Adjuvant Therapy in the Prevention of Diabetes and its Associated Complications
Current Diabetes Reviews Creatine and the Liver: Metabolism and Possible Interactions
Mini-Reviews in Medicinal Chemistry “SLY AS A FOXO”: New Paths with Forkhead Signaling in the Brain
Current Neurovascular Research