Topical Retinaldehyde on Human Skin: Biologic Effects and Tolerance

Saurat, J.‐H.; Didierjean, Liliane; Masgrau, E.; Piletta, Pierre; Jaconi, Stefano; Chatellard-Gruaz, Dominique; Gumowski, Dagmar; Masouyé, Isabelle; Salomon, Denis; Siegenthaler, Georges

doi:10.1111/1523-1747.ep12412861

Cited by 131 publications

(121 citation statements)

References 22 publications

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“…Topical application of retinol to human skin stimulates the same biological effects as topical RA treatment, probably by local metabolism to RA . Similarly, treatment of human skin with retinal leads to RA biological activity, further suggesting local conversion to RA (Saurat et al, 1994). Measurement of retinoids in cultured human keratinocytes has shown that RA can be detected in these cells (Siegenthaler et al, 1990;Randolph and Simon, 1993).…”

Section: Introductionmentioning

confidence: 97%

Class IV alcohol/retinol dehydrogenase localization in epidermal basal layer: Potential site of retinoic acid synthesis during skin development

1997

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Section: Introductionmentioning

confidence: 97%

Class IV alcohol/retinol dehydrogenase localization in epidermal basal layer: Potential site of retinoic acid synthesis during skin development

1997

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“…Topical RA induces a skin irritation that may lead to cessation of treatment. Topical RAL is quite less irritant and may be used for longer periods of time [30][31][32][33]. In this context it is interesting to have at one's disposal a new family of branched retinoids with a potential depigmenting effect, which could be added, alone or in combination, in skin lightening formulations.…”

Section: Discussionmentioning

confidence: 99%

In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives

Sorg¹,

Kasraee²,

Saurat³

2014

TODDISJ

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Abstract:Background: In spite of the numerous depigmenting agents available, there is an inverse relationship between safety and efficiency. Natural retinoids exert depigmenting activities in vivo, but have a narrow therapeutic window. There is thus a need for a new class of depigmenting agents that would be both safe and useful.Objective: The aim of the study was to analyse the potential interest of new retinoid derivatives as topical depigmenting agents. Methods:The tolerance profile of the new retinoids was analysed in murine BDVII keratinocytes and murine B16 melanocytes using the MTT assay. The uptake and the metabolism of the retinoids were analysed in keratinocytes and melanocytes by HPLC/UV. The cellular content of melanin was determined in melanocytes using a photometric assay.Results: Methyl-and t-butyl-4-oxoretinoate, arbutin retinoate and retinoic acid were shown to have the best depigmenting potential according to the ratio between the IC 50 for MTT assay and that for melanin content. Retinaldehyde, 4-hydroxyretinaldehyde and methyl-4-hydroxyretinoate have a good depigmenting potential too, although the therapeutic window is narrower due to a higher toxicity.Conclusion: 4-Oxoesters of retinoic acid, arbutin retinoate and 4-hydroxyretinaldehyde derivatives offer a new family of depigmenting agents acting via a different pathway than tyrosinase inhibitors.

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“…Over the last years, however, there has also been a renewed interest in the effects of natural retinoids, primarily as topical agents. Thus, vitamin A – either in the form of retinol or retinyl esters – is commonly added to cosmetics (although it is a poor prodrug of RA when applied locally on the skin), and retinaldehyde (which is a much more efficient prodrug) attracts increasing interest as a topical treatment for skin aging and other skin disorders [84]. An advantage of using retinaldehyde instead of RA is its more versatile metabolism – a surplus of the drug will be rapidly reduced to retinol and hence inactivated as retinyl esters.…”

Section: Clinical Effectsmentioning

confidence: 99%

What Are Natural Retinoids?

Vahlquist

1999

Dermatology

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Vitamin A (retinol) is the prototype of all other natural retinoids. It is composed of a nonaromatic ring structure, a polyprenoid side chain and a carbonyl end group. These features make it liable to metabolic interconversion and protein interactions but also cause detergent-like properties and a sensitivity to UV irradiation and oxidation. Natural retinoids are present in all living organisms, either as preformed vitamin A or as carotenoids, and are required for a vast number of biological processes, e.g. vision, cellular growth and differentiation and reproduction. Although retinol is the most omnipotent compound, natural retinoids like all-trans-, 9-cis- and didehydroretinoic acid (RA) are clearly more potent outside the retina and trigger gene expression via binding to nucelar retinoid receptors. Retinaldehyde takes an intermediate position in this respect, with ability to convert to both retinol and RA. Over the years, many natural retinoids have been tried therapeutically against skin disorders with the best effects achieved with retinol, retinaldehyde, 13-cis-RA and all-trans-RA. The latter compound was the prototype when new, synthetic derivatives of vitamin A were sought, hoping for a better therapeutic index and a higher functional specificity. Inevitably, treatment with such drugs will influence the effects of coexisting natural retinoids. An understanding of the basic principles of these interactions may have major impact on patient outcome.

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Topical Retinaldehyde on Human Skin: Biologic Effects and Tolerance

Cited by 131 publications

References 22 publications

Class IV alcohol/retinol dehydrogenase localization in epidermal basal layer: Potential site of retinoic acid synthesis during skin development

Class IV alcohol/retinol dehydrogenase localization in epidermal basal layer: Potential site of retinoic acid synthesis during skin development

In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives

What Are Natural Retinoids?

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