Abstract
Glibenclamide is widely used and remains a cornerstone and an effective antihyperglycemic drug. After the casual discovery of its hypoglycemic potential, this compound was introduced for diabetes treatment. However, the long-term side effects reveal that glibenclamide should be replaced by new molecules able to maintain the health of β-cells, protecting them from hyperstimulation/hyperexcitability, hyperinsulinemia, functional failure and cell death. The aim of this review was to highlight the main mechanism of action of glibenclamide and the influence of its derivatives, such as acylhydrazones, sulfonamides and sulfonylthioureas on β-cells potassium and calcium channels for insulin secretion as well as the contribution of these new compounds to restore glucose homeostasis. Furthermore, the role of glibenclamide-based novel structures that promise less excitability of β-cell in a long-term treatment with effectiveness and safety for diabetes therapy was discussed.
Keywords: Acyl-hydrazones, glibenclamide derivatives, glucose homeostasis, insulin, pancreatic β-cell, sulfonamides, sulfonylthioureas, sulfonylureas.
Graphical Abstract
Current Drug Targets
Title:Mechanism of Action of Novel Glibenclamide Derivatives on Potassium and Calcium Channels for Insulin Secretion
Volume: 18 Issue: 6
Author(s): Marisa Jadna Silva Frederico, Allisson Jhonatan Gomes Castro, Danusa Menegaz, Cahue De Bernardis Murat, Camila Pires Mendes, Alessandra Mascarello, Ricardo Jose Nunes and Fatima Regina Mena Barreto Silva
Affiliation:
Keywords: Acyl-hydrazones, glibenclamide derivatives, glucose homeostasis, insulin, pancreatic β-cell, sulfonamides, sulfonylthioureas, sulfonylureas.
Abstract: Glibenclamide is widely used and remains a cornerstone and an effective antihyperglycemic drug. After the casual discovery of its hypoglycemic potential, this compound was introduced for diabetes treatment. However, the long-term side effects reveal that glibenclamide should be replaced by new molecules able to maintain the health of β-cells, protecting them from hyperstimulation/hyperexcitability, hyperinsulinemia, functional failure and cell death. The aim of this review was to highlight the main mechanism of action of glibenclamide and the influence of its derivatives, such as acylhydrazones, sulfonamides and sulfonylthioureas on β-cells potassium and calcium channels for insulin secretion as well as the contribution of these new compounds to restore glucose homeostasis. Furthermore, the role of glibenclamide-based novel structures that promise less excitability of β-cell in a long-term treatment with effectiveness and safety for diabetes therapy was discussed.
Export Options
About this article
Cite this article as:
Frederico Jadna Silva Marisa, Castro Jhonatan Gomes Allisson, Menegaz Danusa, Murat De Bernardis Cahue, Mendes Pires Camila, Mascarello Alessandra, Nunes Jose Ricardo and Silva Regina Mena Barreto Fatima, Mechanism of Action of Novel Glibenclamide Derivatives on Potassium and Calcium Channels for Insulin Secretion, Current Drug Targets 2017; 18 (6) . https://dx.doi.org/10.2174/1389450117666160615084752
DOI https://dx.doi.org/10.2174/1389450117666160615084752 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
- 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
-
Lipotoxicity on the Basis of Metabolic Syndrome and Lipodystrophy in HIV-1-Infected Patients Under Antiretroviral Treatment
Current Pharmaceutical Design Role of Nitrosative Stress and Poly(ADP-ribose) Polymerase Activation in Diabetic Vascular Dysfunction
Current Vascular Pharmacology Antioxidants and Neuroprotection in the Adult and Developing Central Nervous System
Current Medicinal Chemistry Genomics and the Prospects of Existing and Emerging Therapeutics for Cardiovascular Diseases
Current Pharmaceutical Design Synthesis of Benzophenonehydrazone Schiff Bases and their In Vitro Antiglycating Activities
Medicinal Chemistry Physiological Mechanisms of Action of Incretin and Insulin in Regulating Skeletal Muscle Metabolism
Current Diabetes Reviews Determination of Glimepiride in Pharmaceutical Formulations by Square-Wave Voltammetric Method
Current Analytical Chemistry Thyroid Hormones and their Metabolites: Biological Roles and Association with Non-Alcoholic Fatty Liver Disease
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Adverse HBOC-Endothelial Dysfunction Synergism: A Possible Contributor to Adverse Clinical Outcomes?
Current Drug Discovery Technologies Leptin G-2548A and Leptin Receptor Q223R Gene Polymorphisms are Differently Associated with Oxidative Process in Mexican Mestizo and Indigenous with Obesity
Endocrine, Metabolic & Immune Disorders - Drug Targets Fatty Acid Intakes and Coronary Heart Disease Mortality in Japan: NIPPON DATA90, 1990-2005
Current Nutrition & Food Science Association between HbA1C (Glycated Hemoglobin) and Clinical Outcomes in Patients with Subarachnoid Hemorrhage After Neuro-intervention
Current Neurovascular Research Zoledronic Acid Use and Risk of Cognitive Decline among Elderly Women and Men with Osteoporosis
Endocrine, Metabolic & Immune Disorders - Drug Targets Editorial (Thematic Issue: Current Update on Association Between Alzheimer’s Disease and Type 2 Diabetes: Volume I)
CNS & Neurological Disorders - Drug Targets Obesity and Cardiovascular Physiology: Impact of some Pharmacological Agents
Current Vascular Pharmacology Self-care improvement after a pharmaceutical intervention in elderly type 2 diabetic patients
Current Diabetes Reviews The Current View on the Helicase Activity of RNA Helicase A and Its Role in Gene Expression
Current Protein & Peptide Science Metformin: A Growing Journey from Glycemic Control to the Treatment of Alzheimer’s Disease and Depression
Current Medicinal Chemistry Nucleic Acid Aptamers: Clinical Applications and Promising New Horizons
Current Medicinal Chemistry Cubilin, the Intrinsic Factor-Vitamin B12 Receptor in Development and Disease
Current Medicinal Chemistry