Abstract
We report here a new class of compounds, quinoline derivatives, as potential inhibitors of in vitro bovine serum albumin-methylglyoxal glycation. Among compounds 1-19, compound 14 was found to be the most active analog with IC50 of 282.98 ± 8.4 µM. Compounds 12 (IC50 = 661.78 ± 8.7 µM) and 15 (IC50 = 629.43 ± 7.85 7 µM) were also identified as modest inhibitors, in comparison to the standard inhibitor, rutin (IC50 = 294.50 ± 1.5 µM). When evaluated for antioxidant activity through in vitro DPPH radical scavenging assay, compounds 3 (IC50 = 2.19 ± 0.27 µM), 6 (IC50 = 7.35 ± 2.27 µM), 11 (IC50 = 8.96 ± 0.56 µM), and 12 (IC50 = 10.11 ± 2.03 µM), and 15 (IC50 = 7.01 ± 3.87 µM) were found to be more active than the standard i.e. gallic acid (IC50 = 23.34 ± 0.43 µM). These compounds were also evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line). All compounds were found to be non-toxic in cellular model. This study identifies quinoline derivatives as a new class of inhibitors of protein glycation in vitro, along with antioxidant and non-toxic nature. These properties make them interesting leads for further studies as potential anti-diabetic agents.
Keywords: Advanced glycation end products (AGEs), antioxidant, diabetes, glycation inhibitors, quinoline, reactive oxygen species.
Medicinal Chemistry
Title:Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications
Volume: 11 Issue: 1
Author(s): Bilquees Bano, Sanaullah Abbasi, Jalaluddin A. J. Khan, Shafqat Hussain, Saima Rasheed, Shahnaz Perveen, Khalid Mohammed Khan and M. Iqbal Choudhary
Affiliation:
Keywords: Advanced glycation end products (AGEs), antioxidant, diabetes, glycation inhibitors, quinoline, reactive oxygen species.
Abstract: We report here a new class of compounds, quinoline derivatives, as potential inhibitors of in vitro bovine serum albumin-methylglyoxal glycation. Among compounds 1-19, compound 14 was found to be the most active analog with IC50 of 282.98 ± 8.4 µM. Compounds 12 (IC50 = 661.78 ± 8.7 µM) and 15 (IC50 = 629.43 ± 7.85 7 µM) were also identified as modest inhibitors, in comparison to the standard inhibitor, rutin (IC50 = 294.50 ± 1.5 µM). When evaluated for antioxidant activity through in vitro DPPH radical scavenging assay, compounds 3 (IC50 = 2.19 ± 0.27 µM), 6 (IC50 = 7.35 ± 2.27 µM), 11 (IC50 = 8.96 ± 0.56 µM), and 12 (IC50 = 10.11 ± 2.03 µM), and 15 (IC50 = 7.01 ± 3.87 µM) were found to be more active than the standard i.e. gallic acid (IC50 = 23.34 ± 0.43 µM). These compounds were also evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line). All compounds were found to be non-toxic in cellular model. This study identifies quinoline derivatives as a new class of inhibitors of protein glycation in vitro, along with antioxidant and non-toxic nature. These properties make them interesting leads for further studies as potential anti-diabetic agents.
Export Options
About this article
Cite this article as:
Bano Bilquees, Abbasi Sanaullah, Khan A. J. Jalaluddin, Hussain Shafqat, Rasheed Saima, Perveen Shahnaz, Khan Mohammed Khalid and Choudhary Iqbal M., Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications, Medicinal Chemistry 2015; 11 (1) . https://dx.doi.org/10.2174/1573406410666140526151254
DOI https://dx.doi.org/10.2174/1573406410666140526151254 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
Animal Models in Neurology: Drawbacks and Opportunities
Current Pharmaceutical Design Targeting Abnormal Nrf2/HO-1 Signaling in Amyotrophic Lateral Sclerosis: Current Insights on Drug Targets and Influences on Neurological Disorders
Current Molecular Medicine Evaluation of Structure, Chaperone-Like Activity and Allergenicity of Reduced Glycated Adduct of Bovine β-casein
Protein & Peptide Letters Flaxseed and Diabetes
Current Pharmaceutical Design Withdrawn: Mesenchymal Stem Cell-derived Exosomes for Treatment of Ischemic Stroke
Current Stem Cell Research & Therapy Control and Role of Plateau Potential Properties in the Spinal Cord
Current Pharmaceutical Design Non-Celiac Gluten Sensitivity Triggers Gut Dysbiosis, Neuroinflammation, Gut-Brain Axis Dysfunction, and Vulnerability for Dementia
CNS & Neurological Disorders - Drug Targets Clinical Management of Diabetes Mellitus in the Older Adult Patient
Current Diabetes Reviews Genome-Scale Technologies Foster Advances in Neurological and Behavioral Research
Current Psychiatry Reviews Anti-IL-1 β Therapies
Recent Patents on DNA & Gene Sequences Polyphenols Beyond Barriers: A Glimpse into the Brain
Current Neuropharmacology Pathophysiology of Diabetic Dyslipidaemia
Current Vascular Pharmacology Advanced Glycation End Products (AGEs) and their Receptor (RAGE) System in Diabetic Retinopathy
Current Drug Discovery Technologies Editorial: Alzheimer's Disease: From Molecular Mechanisms to Psychobiological Perspectives
Current Alzheimer Research Cannabinoid Receptor Type 2 Activation Yields Delayed Tolerance to Focal Cerebral Ischemia
Current Neurovascular Research Preclinical Studies and Clinical Trials with Mesenchymal Stem Cell for Demyelinating Diseases: A Systematic Review
Current Stem Cell Research & Therapy Therapeutic Potential of Janus Kinase 3 (JAK3) Inhibitors
Current Pharmaceutical Design Management of Exercise-induced Glycemic Imbalances in Type 1 Diabetes
Current Diabetes Reviews Is rTMS an Effective Therapeutic Strategy that Can Be Used to Treat Parkinson's Disease?
CNS & Neurological Disorders - Drug Targets Potential Therapeutic Targets for Neurodegenerative Diseases: Lessons Learned from Calorie Restriction
Current Drug Targets