Abstract
Natural polyphenolic compounds have attractive consideration for their cancer preventive effect. As their anti-cancer effect, inhibitory effect on angiogenesis would be important. Recently, it has been shown that quercetin has anti-angiogenic activity and is a potent anti-cancer agent. However, the activity of its glycosylated forms and related derivatives has not been investigated yet. In this study, we examined the effect of glycosylated quercetin on angiogenesis. Interestingly, quercetin 3-O-β-D-glucose (isoquercitrin) showed the strongest inhibitory effect on an ex vivo angiogenesis assay, but quercetin 3-O-β-D-glucose-[1,6]-O-α-Lrhamnose (rutin) had no effect. Inhibitory effect of quercetin 7-O-β-D-glucose (quercimeritrin) was almost similar to that of quercetin. Furthermore, we compared the activity of acylated isoquercitrins (isoquercitrin cinnamate, dihydrocinnamate, p-coumarate, and 2-naphthalate). Consequently, anti-angiogenic activity of the isoquercitrin derivatives was weaker than that of isoquercitrin. The effects of quercetin and its derivatives on human umbilical endothelial cell (HUVEC) proliferation, HUVEC tube formation and chemotaxis assays were associated with their effects on the ex vivo angiogenesis assay.
Keywords: angiogenesis, quercetin, isoquercitrin, acylated isoquercitrin, rutin
Letters in Drug Design & Discovery
Title: Anti-Angiogenic Activity of Quercetin and its Derivatives
Volume: 1 Issue: 4
Author(s): Kiminori Matsubara, Kohji Ishihara, Yoshiyuki Mizushina, Masaharu Mori and Nobuyoshi Nakajima
Affiliation:
Keywords: angiogenesis, quercetin, isoquercitrin, acylated isoquercitrin, rutin
Abstract: Natural polyphenolic compounds have attractive consideration for their cancer preventive effect. As their anti-cancer effect, inhibitory effect on angiogenesis would be important. Recently, it has been shown that quercetin has anti-angiogenic activity and is a potent anti-cancer agent. However, the activity of its glycosylated forms and related derivatives has not been investigated yet. In this study, we examined the effect of glycosylated quercetin on angiogenesis. Interestingly, quercetin 3-O-β-D-glucose (isoquercitrin) showed the strongest inhibitory effect on an ex vivo angiogenesis assay, but quercetin 3-O-β-D-glucose-[1,6]-O-α-Lrhamnose (rutin) had no effect. Inhibitory effect of quercetin 7-O-β-D-glucose (quercimeritrin) was almost similar to that of quercetin. Furthermore, we compared the activity of acylated isoquercitrins (isoquercitrin cinnamate, dihydrocinnamate, p-coumarate, and 2-naphthalate). Consequently, anti-angiogenic activity of the isoquercitrin derivatives was weaker than that of isoquercitrin. The effects of quercetin and its derivatives on human umbilical endothelial cell (HUVEC) proliferation, HUVEC tube formation and chemotaxis assays were associated with their effects on the ex vivo angiogenesis assay.
Export Options
About this article
Cite this article as:
Matsubara Kiminori, Ishihara Kohji, Mizushina Yoshiyuki, Mori Masaharu and Nakajima Nobuyoshi, Anti-Angiogenic Activity of Quercetin and its Derivatives, Letters in Drug Design & Discovery 2004; 1 (4) . https://dx.doi.org/10.2174/1570180043398533
DOI https://dx.doi.org/10.2174/1570180043398533 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Microbial Biotransformation: Recent Developments on Steroid Drugs
Recent Patents on Biotechnology Biology and Clinical Management of Myeloproliferative Neoplasms and Development of the JAK Inhibitor Ruxolitinib
Current Medicinal Chemistry Strategies that Target Tight Junctions for Enhanced Drug Delivery
Current Pharmaceutical Design Atrial Remodeling and Novel Pharmacological Strategies for Antiarrhythmic Therapy in Atrial Fibrillation
Current Medicinal Chemistry Proteasome Inhibitors in Cancer Therapy
Current Drug Targets Coarctation of the Aorta - An Evolution of Therapeutic Options
Current Cardiology Reviews Anti-hyperglycemic Potential of Natural Products
Mini-Reviews in Medicinal Chemistry From Body Art to Anticancer Activities: Perspectives on Medicinal Properties of Henna
Current Drug Targets An Overview on Global Trends in Nanotechnological Approaches for Alzheimer Therapy
Current Drug Metabolism Vasoactive Intestinal Peptide in Neurodevelopmental Disorders:Therapeutic Potential
Current Pharmaceutical Design ABC Transporter Inhibitors in Reversing Multidrug Resistance to Chemotherapy
Current Drug Targets Peptides as Therapeutic Agents or Drug Leads for Autoimmune, Hormone Dependent and Cardiovascular Diseases
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Amygdalar Atrophy in Early Alzheimer’s Disease
Current Alzheimer Research A New Approach for β-cyclodextrin Conjugated Drug Delivery System in Cancer Therapy
Current Drug Delivery Anti-Platelet Treatment of Middle-Sized Abdominal Aortic Aneurysms
Current Vascular Pharmacology Recent Progress of Src Family Kinase Inhibitors as Anticancer Agents
Mini-Reviews in Medicinal Chemistry Cancer and Aids: New Trends in Drug Design and Chemotherapy
Current Computer-Aided Drug Design 3D-QSAR Study of Flavone Derivatives as Inhibitors of HeLa Cervix Adenocarcinoma Cell Lines
Letters in Drug Design & Discovery Thalidomide Analogues as Anticancer Drugs
Recent Patents on Anti-Cancer Drug Discovery Recent Advances in Permeation Enhancement Techniques for Transdermal Drug Delivery Systems: A Review
Current Drug Therapy