Hypopigmenting agents: An updated review on biological, chemical and clinical aspects

Francisco Solano, Stefania Briganti, Mauro Picardo, Ghanem Ghanem

Research output: Contribution to journalArticle

Abstract

An overview of agents causing hypopigmentation in human skin is presented. The review is organized to put forward groups of biological and chemical agents. Their mechanisms of action cover (i) tyrosinase inhibition, maturation and enhancement of its degradation; (ii) Mitf inhibition; (iii) downregulation of MC1R activity; (iv) interference with melanosome maturation and transfer; (v) melanocyte loss, desquamation and chemical peeling. Tyrosinase inhibition is the most common approach to achieve skin hypopigmentation as this enzyme catalyses the rate-limiting step of pigmentation. Despite the large number of tyrosinase inhibitors in vitro, only a few are able to induce effects in clinical trials. The gap between in-vitro and in-vivo studies suggests that innovative strategies are needed for validating their efficacy and safety. Successful treatments need the combination of two or more agents acting on different mechanisms to achieve a synergistic effect. In addition to tyrosinase inhibition, other parameters related to cytotoxicity, solubility, cutaneous absorption, penetration and stability of the agents should be considered. The screening test system is also very important as keratinocytes play an active role in modulating melanogenesis within melanocytes. Mammalian skin or at least keratinocytes/melanocytes co-cultures should be preferred rather than pure melanocyte cultures or soluble tyrosinase.

Original languageEnglish
Pages (from-to)550-571
Number of pages22
JournalPigment Cell Research
Volume19
Issue number6
DOIs
Publication statusPublished - Dec 2006

Fingerprint

melanocytes
Monophenol Monooxygenase
Melanocytes
skin (animal)
keratinocytes
Hypopigmentation
Skin
Keratinocytes
melanogenesis
peeling
coculture
Melanosomes
Skin Absorption
in vivo studies
Peeling
pigmentation
Pigmentation
cytotoxicity
Biological Factors
solubility

Keywords

  • Antioxidants
  • Depigmentation
  • Flavonoids
  • Hypopigmentation
  • Melanocyte
  • Tyrosinase inhibitors

ASJC Scopus subject areas

  • Cell Biology
  • Agronomy and Crop Science
  • Plant Science
  • Clinical Biochemistry
  • Developmental Biology

Cite this

Hypopigmenting agents : An updated review on biological, chemical and clinical aspects. / Solano, Francisco; Briganti, Stefania; Picardo, Mauro; Ghanem, Ghanem.

In: Pigment Cell Research, Vol. 19, No. 6, 12.2006, p. 550-571.

Research output: Contribution to journalArticle

@article{a7d4e2fbf6104ea89e08e28072a3c8b8,
title = "Hypopigmenting agents: An updated review on biological, chemical and clinical aspects",
abstract = "An overview of agents causing hypopigmentation in human skin is presented. The review is organized to put forward groups of biological and chemical agents. Their mechanisms of action cover (i) tyrosinase inhibition, maturation and enhancement of its degradation; (ii) Mitf inhibition; (iii) downregulation of MC1R activity; (iv) interference with melanosome maturation and transfer; (v) melanocyte loss, desquamation and chemical peeling. Tyrosinase inhibition is the most common approach to achieve skin hypopigmentation as this enzyme catalyses the rate-limiting step of pigmentation. Despite the large number of tyrosinase inhibitors in vitro, only a few are able to induce effects in clinical trials. The gap between in-vitro and in-vivo studies suggests that innovative strategies are needed for validating their efficacy and safety. Successful treatments need the combination of two or more agents acting on different mechanisms to achieve a synergistic effect. In addition to tyrosinase inhibition, other parameters related to cytotoxicity, solubility, cutaneous absorption, penetration and stability of the agents should be considered. The screening test system is also very important as keratinocytes play an active role in modulating melanogenesis within melanocytes. Mammalian skin or at least keratinocytes/melanocytes co-cultures should be preferred rather than pure melanocyte cultures or soluble tyrosinase.",
keywords = "Antioxidants, Depigmentation, Flavonoids, Hypopigmentation, Melanocyte, Tyrosinase inhibitors",
author = "Francisco Solano and Stefania Briganti and Mauro Picardo and Ghanem Ghanem",
year = "2006",
month = "12",
doi = "10.1111/j.1600-0749.2006.00334.x",
language = "English",
volume = "19",
pages = "550--571",
journal = "Pigment Cell Research",
issn = "0893-5785",
publisher = "Wiley-Blackwell",
number = "6",

}

TY - JOUR

T1 - Hypopigmenting agents

T2 - An updated review on biological, chemical and clinical aspects

AU - Solano, Francisco

AU - Briganti, Stefania

AU - Picardo, Mauro

AU - Ghanem, Ghanem

PY - 2006/12

Y1 - 2006/12

N2 - An overview of agents causing hypopigmentation in human skin is presented. The review is organized to put forward groups of biological and chemical agents. Their mechanisms of action cover (i) tyrosinase inhibition, maturation and enhancement of its degradation; (ii) Mitf inhibition; (iii) downregulation of MC1R activity; (iv) interference with melanosome maturation and transfer; (v) melanocyte loss, desquamation and chemical peeling. Tyrosinase inhibition is the most common approach to achieve skin hypopigmentation as this enzyme catalyses the rate-limiting step of pigmentation. Despite the large number of tyrosinase inhibitors in vitro, only a few are able to induce effects in clinical trials. The gap between in-vitro and in-vivo studies suggests that innovative strategies are needed for validating their efficacy and safety. Successful treatments need the combination of two or more agents acting on different mechanisms to achieve a synergistic effect. In addition to tyrosinase inhibition, other parameters related to cytotoxicity, solubility, cutaneous absorption, penetration and stability of the agents should be considered. The screening test system is also very important as keratinocytes play an active role in modulating melanogenesis within melanocytes. Mammalian skin or at least keratinocytes/melanocytes co-cultures should be preferred rather than pure melanocyte cultures or soluble tyrosinase.

AB - An overview of agents causing hypopigmentation in human skin is presented. The review is organized to put forward groups of biological and chemical agents. Their mechanisms of action cover (i) tyrosinase inhibition, maturation and enhancement of its degradation; (ii) Mitf inhibition; (iii) downregulation of MC1R activity; (iv) interference with melanosome maturation and transfer; (v) melanocyte loss, desquamation and chemical peeling. Tyrosinase inhibition is the most common approach to achieve skin hypopigmentation as this enzyme catalyses the rate-limiting step of pigmentation. Despite the large number of tyrosinase inhibitors in vitro, only a few are able to induce effects in clinical trials. The gap between in-vitro and in-vivo studies suggests that innovative strategies are needed for validating their efficacy and safety. Successful treatments need the combination of two or more agents acting on different mechanisms to achieve a synergistic effect. In addition to tyrosinase inhibition, other parameters related to cytotoxicity, solubility, cutaneous absorption, penetration and stability of the agents should be considered. The screening test system is also very important as keratinocytes play an active role in modulating melanogenesis within melanocytes. Mammalian skin or at least keratinocytes/melanocytes co-cultures should be preferred rather than pure melanocyte cultures or soluble tyrosinase.

KW - Antioxidants

KW - Depigmentation

KW - Flavonoids

KW - Hypopigmentation

KW - Melanocyte

KW - Tyrosinase inhibitors

UR - http://www.scopus.com/inward/record.url?scp=33750538670&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33750538670&partnerID=8YFLogxK

U2 - 10.1111/j.1600-0749.2006.00334.x

DO - 10.1111/j.1600-0749.2006.00334.x

M3 - Article

C2 - 17083484

AN - SCOPUS:33750538670

VL - 19

SP - 550

EP - 571

JO - Pigment Cell Research

JF - Pigment Cell Research

SN - 0893-5785

IS - 6

ER -