Abstract
Hyperpigmentation disorders constitute important medical and aesthetical conditions. Dark areas or dark spots on the skin result from inappropriate amount and/or deposition of skin pigments - melanins. Several depigmenting agents, such as kojic acid, arbutin, aloesin, ellagic acid, resveratrol, azelaic acid, niacinamide, tretinoin, glycolic acid, lactic acid, and citric acid, have already been identified and are used in topical drugs or cosmetic formulations for the treatment of hyperpigmentations. However, these compounds are characterized by insufficient effectiveness and multiple adverse effects. As a result, there is still a need for searching for new active substances. The current paper summarizes strategies for searching for novel melanogenesis inhibitors. In the review, they are divided according to approach, into in silico, in vitro and in vivo experiments. In silico research includes computational studies with models of tyrosinase and di-copper complexes. The in vitro approach is based on tests using tyrosinase (a key enzyme in melanin biosynthesis), cell cultures, cell co-cultures, pigmented human skin equivalents or Streptomyces bikiniensis model. In vivo studies involve zebrafish, rodents or humans. Examples of protocols and laboratory procedures are presented, with a focus on utilization of various models for evaluation of mechanisms of action of tested compounds. The potential limitations of the methods are also discussed, together with future perspectives in the field of searching for melanogenesis inhibitors.
Keywords: Depigmenting agents, hyperpigmentations, in silico, in vitro, in vivo, melanogenesis, melanogenesis inhibitors, tyrosinase.
Current Medicinal Chemistry
Title:Melanogenesis Inhibitors: Strategies for Searching for and Evaluation of Active Compounds
Volume: 23 Issue: 31
Author(s): Agnieszka Gunia-Krzyżak, Justyna Popiol and Henryk Marona
Affiliation:
Keywords: Depigmenting agents, hyperpigmentations, in silico, in vitro, in vivo, melanogenesis, melanogenesis inhibitors, tyrosinase.
Abstract: Hyperpigmentation disorders constitute important medical and aesthetical conditions. Dark areas or dark spots on the skin result from inappropriate amount and/or deposition of skin pigments - melanins. Several depigmenting agents, such as kojic acid, arbutin, aloesin, ellagic acid, resveratrol, azelaic acid, niacinamide, tretinoin, glycolic acid, lactic acid, and citric acid, have already been identified and are used in topical drugs or cosmetic formulations for the treatment of hyperpigmentations. However, these compounds are characterized by insufficient effectiveness and multiple adverse effects. As a result, there is still a need for searching for new active substances. The current paper summarizes strategies for searching for novel melanogenesis inhibitors. In the review, they are divided according to approach, into in silico, in vitro and in vivo experiments. In silico research includes computational studies with models of tyrosinase and di-copper complexes. The in vitro approach is based on tests using tyrosinase (a key enzyme in melanin biosynthesis), cell cultures, cell co-cultures, pigmented human skin equivalents or Streptomyces bikiniensis model. In vivo studies involve zebrafish, rodents or humans. Examples of protocols and laboratory procedures are presented, with a focus on utilization of various models for evaluation of mechanisms of action of tested compounds. The potential limitations of the methods are also discussed, together with future perspectives in the field of searching for melanogenesis inhibitors.
Export Options
About this article
Cite this article as:
Gunia-Krzyżak Agnieszka, Popiol Justyna and Marona Henryk, Melanogenesis Inhibitors: Strategies for Searching for and Evaluation of Active Compounds, Current Medicinal Chemistry 2016; 23 (31) . https://dx.doi.org/10.2174/0929867323666160627094938
DOI https://dx.doi.org/10.2174/0929867323666160627094938 |
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
-
In Vivo, Cardiac-Specific Knockdown of a Target Protein, Malic Enzyme- 1, in Rat via Adenoviral Delivery of DNA for Non-Native miRNA
Current Gene Therapy Exosomes in Therapy: Engineering, Pharmacokinetics and Future Applications
Current Drug Targets Lipids and Their Derivatives: By-Products Used as Essential Building Blocks for Modern Drug Delivery Systems
Current Drug Targets A New Strategy to Target Acute Myeloid Leukemia Stem and Progenitor Cells Using Chidamide, a Histone Deacetylase Inhibitor
Current Cancer Drug Targets Translational Peptide-associated Nanosystems: Promising Role as Cancer Vaccines
Current Topics in Medicinal Chemistry Transcriptional and Post-Transcriptional Regulations of Junction Proteins in Mammalian estes – Implications on Male Contraceptive Development
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Review of Recent Clinical Developments and Patents for the Treatment of Autoimmune and Inflammatory Diseases by Mesenchymal Stromal Cells
Recent Patents on Regenerative Medicine A Personalized Approach to Systemic Treatment of Unresectable or Metastatic Pancreatic Adenocarcinoma
Current Pharmacogenomics and Personalized Medicine Delivery of Curcumin and Medicinal Effects of the Copper(II)-Curcumin Complexes
Current Pharmaceutical Design Targeting Autophagic Pathways by Plant Natural Compounds in Cancer Treatment
Current Drug Targets Mitochondrial Dysfunction and Targeted Drugs: A Focus on Diabetes
Current Pharmaceutical Design CXCL12-CXCR4 Axis in Angiogenesis, Metastasis and Stem Cell Mobilization
Current Pharmaceutical Design Molecular Approaches Target to Immunotherapy for HPV-Associated Cancers
Current Cancer Drug Targets Fibroblast Growth Factors, Fibroblast Growth Factor Receptors, Diseases, and Drugs
Recent Patents on Cardiovascular Drug Discovery Animal Venoms have Potential to Treat Cancer
Current Topics in Medicinal Chemistry Ligand Docking and Structure-based Virtual Screening in Drug Discovery
Current Topics in Medicinal Chemistry Controlled-release Particulate Cytokine Adjuvants for Cancer Therapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Differential Expression of miR-20a and miR-145 in Colorectal Tumors as Potential Location-specific miRNAs
MicroRNA In Vitro Regulatory Effect of Epididymal Serpin CRES on Protease Activity of Proprotein Convertase PC4/PCSK4
Current Molecular Medicine Biochemistry and Physiology of Anabolic Androgenic Steroids Doping
Mini-Reviews in Medicinal Chemistry