The Combination of a Retinoid, a Phenolic Agent and an Antioxidant Improves Tolerance while Retaining an Optimal Depigmenting Action in Reconstructed Epidermis

Sorg, Olivier; Kasraee, Behrooz; Salomon, Denis; Saurat, Jean‐Hilaire

doi:10.1159/000353578

Cited by 12 publications

(17 citation statements)

References 31 publications

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“…Such a combination of three agents, a retinoid (RAL), a new phenolic agent (4-(1-phenylethyl)-resorcinol) and a reducing agent (δ-tocopheryl-β- D -glucopyranoside) was shown to enable in reconstructed epidermis an optimal depigmenting action while being less toxic than each compound alone at the concentrations that would be required to reach the same depigmenting action as in combination [9]. …”

Section: Discussionmentioning

confidence: 99%

“…A novel lightening combination containing a retinoid (retinaldehyde, RAL), a new phenolic agent (4-(1-phenylethyl)-resorcinol) and a reducing agent (δ-tocopheryl-β- D -glucopyranoside) has been recently reported to have effective and safe depigmenting activity in reconstructed epidermis [9]. In this study we clinically and instrumentally evaluated the efficacy and tolerability of such a depigmenting combination for the treatment of solar lentigines in vivo.…”

Section: Introductionmentioning

confidence: 99%

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Clinical and Instrumental Evaluation of the Efficacy of a New Depigmenting Agent Containing a Combination of a Retinoid, a Phenolic Agent and an Antioxidant for the Treatment of Solar Lentigines

Cameli¹,

Abril²,

Agozzino³

et al. 2015

Dermatology

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Background: Solar lentigines are common benign macular hyperpigmented lesions localized on sun-exposed areas. Objective: To evaluate the efficacy and safety of a new depigmenting agent containing a retinoid (retinaldehyde), a new phenolic agent (4-(1-phenylethyl)-resorcinol) and a reducing agent (δ-tocopheryl-β-D-glucopyranoside) in the topical treatment of solar lentigines. Patients and Methods: Twenty patients with solar lentigines of the face and hands applied the depigmenting agent on each lentigo once daily for 12 weeks. The outcome was evaluated at 45 days (T1) and 3 months (T2) after the end of treatment compared to baseline (T0) by means of clinical evaluation, Mexameter® and Visioface devices for digital and ultraviolet computerized image analysis of skin color as well as in vivo reflectance confocal microscopy. Results: Image analysis and confocal laser reflectance microscopy showed that hyperpigmentation was significantly reduced at T2 compared to baseline and to controls. Conclusion: The study treatment was well tolerated and showed significant improvement in the depigmentation of solar lentigines.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Clinical and Instrumental Evaluation of the Efficacy of a New Depigmenting Agent Containing a Combination of a Retinoid, a Phenolic Agent and an Antioxidant for the Treatment of Solar Lentigines

Cameli¹,

Abril²,

Agozzino³

et al. 2015

Dermatology

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“…If our results are confirmed in clinical trials, this means that RAL might have a place among the other depigmenting agents and, due to its particular mechanisms of action, could be combined with phenolic active ingredients. A similar in vitro study assessing the association of RAL, a phenolic agent and an antioxidant precursor showed promising data regarding such a combination of agents acting via different mechanisms [32]. …”

Section: Discussionmentioning

confidence: 99%

The Potential Depigmenting Activity of Retinaldehyde

Sorg

Kasraee²,

Salomon³

et al. 2013

Dermatology

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Background: Retinoids have been reported to exert depigmenting activity. Unlike most depigmenting agents that target tyrosinase, they are not phenolic agents and may act via different mechanisms. Objectives: We analysed the properties of retinaldehyde (RAL), a precursor of retinoic acid (RA), as a skin-lightening agent in various models. Methods: The viability and the depigmenting properties of RAL were assessed in murine melanocytes, in human reconstructed epidermis, and in mice and guinea pigs. The melanin content and cytotoxicity were assessed in melanocytes; in 3-dimensional models, the melanin concentration and the number of active melanocytes were determined. Results: RAL was taken up by melanocytes and mostly metabolised to retinol and retinyl esters, and to a lesser extent to RA. RAL decreased the melanin concentration of guinea pig ears and mouse tails by 54 and 74%, respectively, and decreased the number of active melanocytes by 42 and 77%, respectively. In reconstructed epidermis the melanin concentration was increased by 52%, whereas the number of active melanocytes decreased by 44%. Conclusion: RAL exerts a significant depigmenting activity with a mode of action that looks different from that of RA. Our data suggest a skin-lightening effect related to a melanolytic action (i.e. a decrease in melanin concentration, whatever the mechanism) rather than to melanocytotoxicity, besides other still unknown actions of RAL on melanocytes.

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“…Retinoic acid increases keratinocyte‐melanocyte proliferation and acceleration of epidermal turnover, while retinoic acid with combination of other depigmenting compounds strongly suppresses melanogenesis . The combination of δ‐tocopheryl glucoside (C 30 H 49 O 6 ), retinoid, and 4‐(1‐phenylethyl‐resorcinol (C 14 H 14 O 2 ) effectively reduces melanin production due to antioxidant property and various depigmenting modes of action on several melanogenic pathways . The mentioned formulation also had less toxic effect than each compound alone at the same concentrations to its combination .…”

Section: Development Of Potent Depigmenting Formulationmentioning

confidence: 99%

“…On the other hand, improved skin lightening effect was seen in combination of several bioactive compounds and antioxidants like arbutin (50%, w/v), α‐lipoic acid (5%, w/v), KA (1%, w/v), and azelaic acid (10%, w/v) in one formulation . The combination of 4‐n‐butylresorcinol (C 10 H 14 O 2 ) and a natural monoterpenoid, hinokitiol (C 10 H 12 O 2 ), reduces MITF expression and gave better depigmenting activity compared to the action of only a single compound . The presence of gallic acid (C 7 H 6 O 5 ), chebulinic acid (C 41 H 32 O 27 ), and ellagic acid (C 14 H 6 O 8 ) in a formulated Indian medicine, Triphala, remarkably reduce TYR mRNA expression levels in B16F10 cells .…”

Section: Development Of Potent Depigmenting Formulationmentioning

confidence: 99%

Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

Lajis

Ariff

2019

J of Cosmetic Dermatology

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Summary Human skin pigmentation is a result of constitutive and facultative pigmentation. Facultative pigmentation is frequently stimulated by UV radiation, pharmacologic drugs, and hormones whereby leads to the development of abnormal skin hyperpigmentation. To date, many state‐of‐art depigmenting compounds have been studied using in vitro model to treat hyperpigmentation problems for cosmetic dermatological applications; little attention has been made to compare the effectiveness of these depigmenting compounds and their mode of actions. In this present article, new and recent depigmenting compounds, their melanogenic pathway targets, and modes of action are reviewed. This article compares the effectiveness of these new depigmenting compounds to modulate several melanogenesis‐regulatory enzymes and proteins such as tyrosinase (TYR), TYR‐related protein‐1 (TRP1), TYR‐related protein‐2 (TRP2), microphthalmia‐associated transcription factor (MITF), extracellular signal—regulated kinase (ERK) and N‐terminal kinases (JNK) and mitogen‐activated protein kinase p38 (p38 MAPK). Other evidences from in vitro assays such as inhibition on melanosomal transfer, proteasomes, nitric oxide, and inflammation‐induced melanogenesis are also highlighted. This article also reviews analytical techniques in different assays performed using in vitro model as well as their advantages and limitations. This article also provides an insight on recent finding and re‐examination of some protocols as well as their effectiveness and reliability in the evaluation of depigmenting compounds. Evidence and support from related patents are also incorporated in this present article to give an overview on current patented technology, latest trends, and intellectual values of some depigmenting compounds and protocols, which are rarely highlighted in the literatures.

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The Combination of a Retinoid, a Phenolic Agent and an Antioxidant Improves Tolerance while Retaining an Optimal Depigmenting Action in Reconstructed Epidermis

Cited by 12 publications

References 31 publications

Clinical and Instrumental Evaluation of the Efficacy of a New Depigmenting Agent Containing a Combination of a Retinoid, a Phenolic Agent and an Antioxidant for the Treatment of Solar Lentigines

Clinical and Instrumental Evaluation of the Efficacy of a New Depigmenting Agent Containing a Combination of a Retinoid, a Phenolic Agent and an Antioxidant for the Treatment of Solar Lentigines

The Potential Depigmenting Activity of Retinaldehyde

Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

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