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:Laboratory of Cosmetic Chemistry, Department of Bioorganic Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
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.
