Boosting of retinol activity using novel lecithin : Retinol acyltransferase inhibitors / Dominik Imfeld in INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Vol. 46, N° 4 (08/2024)  

[article]  inINTERNATIONAL JOURNAL OF COSMETIC SCIENCE > Vol. 46, N° 4 (08/2024) . - p. 544-552 Titre : Boosting of retinol activity using novel lecithin : Retinol acyltransferase inhibitors Type de document : texte imprimé Auteurs : Dominik Imfeld, Auteur ; André Fischer, Auteur ; Leithe Budel, Auteur ; Clarissa Stoll, Auteur ; Rolf Schütz, Auteur ; Anthony Vincent Rawlings, Auteur Année de publication : 2024 Article en page(s) : p. 544-552 Note générale : Bibliogr. Langues : Anglais (eng) Catégories : Antiâge Antienzymes Collagène Collagène III Cosmétiques Etude ex vivo Lécithine La phosphatidylcholine est plus connue sous le nom lécithine. Au sens le plus strict, la lécithine désigne uniquement les phosphatidylcholines c'est-à-dire un lipide formé à partir d'une choline, d'un phosphate, d'un glycérol et de deux acides gras (figure). Dans ce contexte, il serait plus juste de parler des lécithines, car il ne s'agit pas d'une seule molécule mais d'un groupe dont la composition en acide gras varie d'une molécule à l'autre. Ainsi, les lécithines vont adopter diverses couleurs selon leur composition : du jaune, pour la lécithine végétale, au brun, pour la lécithine de poisson. Le terme de lécithine est aussi utilisé par extension pour désigner l'ensemble des phospholipides extraits du vivant (par exemple le soja), dans la mesure où ils sont majoritairement constitués de phosphatidylcholine. Peau -- Soins et hygiène Relations structure-activité Vitamine A Index. décimale : 668.5 Parfums et cosmétiques Résumé : Lecithin:retinol acyltransferase (LRAT) is the main enzyme catalysing the esterification of retinol to retinyl esters and, hence, is of central importance for retinol homeostasis. As retinol, by its metabolite retinoic acid, stimulates fibroblasts to synthesize collagen fibres and inhibits collagen-degrading enzymes, the inhibition of LRAT presents an intriguing strategy for anti-ageing ingredients by increasing the available retinol in the skin. Here, we synthesized several derivatives mimicking natural lecithin substrates as potential LRAT inhibitors. By exploring various chemical modifications of the core scaffold consisting of a central amino acid and an N-terminal acylsulfone, we explored 10 different compounds in a biochemical assay, resulting in two compounds with IC50 values of 21.1 and 32.7 μM (compounds 1 and 2), along with a simpler arginine derivative with comparative inhibitory potency. Supported by computational methods, we investigated their structure–activity relationship, resulting in the identification of several structural features associated with high inhibition of LRAT. Ultimately, we conducted an ex vivo study with human skin, demonstrating an increase of collagen III associated with a reduction of the skin ageing process. In conclusion, the reported compounds offer a promising approach to boost retinol abundance in human skin and might present a new generation of anti-ageing ingredients for cosmetic application. Note de contenu : - LRAT enzyme inhibition assay - In vitro assay - Ex vivo assay - Molecular modelling DOI : https://doi.org/10.1111/ics.12968 En ligne : https://drive.google.com/file/d/1nudejcOZvSlVima-18M-h2lWS8P6sSZ0/view?usp=drive [...] Format de la ressource électronique : Pdf Permalink : https://e-campus.itech.fr/pmb/opac_css/index.php?lvl=notice_display&id=41353 [article]

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Topically applied, fatty acid-containing formulations provide superior barrier benefits in an ex vivo tape-stripped skin model / John Nip in INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Vol. 46, N° 4 (08/2024)  

[article]  inINTERNATIONAL JOURNAL OF COSMETIC SCIENCE > Vol. 46, N° 4 (08/2024) . - p. 506-515 Titre : Topically applied, fatty acid-containing formulations provide superior barrier benefits in an ex vivo tape-stripped skin model Type de document : texte imprimé Auteurs : John Nip, Auteur ; Hilal Ilarslan, Auteur ; Ana Villa, Auteur ; Dawn Mihalov, Auteur ; Manoj Misra, Auteur ; Samantha D. Samaras, Auteur ; Lin Feng, Auteur ; Stella Arcella, Auteur ; John Bajor, Auteur ; Andrew E. Mayes, Auteur Année de publication : 2024 Article en page(s) : p. 506-515 Note générale : Bibliogr. Langues : Anglais (eng) Catégories : Acides gras Barrière cutanée Couche cornée Dermo-cosmétologie Dermo-pharmacie Etude ex vivo Formulation (Génie chimique) Lamelles lipidiques Lipides Index. décimale : 668.5 Parfums et cosmétiques Résumé : - OBJECTIVE : Ex vivo skin has been used to study various skin conditions from atopic dermatitis to burn injury. The aim of this research is to identify a more effective barrier improvement strategy and to evaluate topical formulations in replenishing the skin. The skin can create new longer chain fatty acids and ceramides (CERs) from topically applied skin natural fatty acid to help renew the skin's barrier. - METHODS : An ex vivo skin model damaged by sequential tape stripping of the stratum corneum (SC) was used to investigate the repair of the SC. Confocal laser scanning microscopy was used to assess the SC layers recovered. Ultrastructural analysis was performed using transmission electron microscopy to visualize the lamellar bodies and intercellular lipid lamellae. - RESULTS : The data in this study provide the first direct ex vivo evidence comparing different marketed formulations containing three CERs with those containing fatty acids. Free fatty acid (FFA)-containing formulations, but not CER-containing formulations, directly applied to the damaged skin, showed an increased number of repaired SC layers and this was reflected at the ultrastructural level by an increased intercellular lipid lamellae length and an increased number of lamellar bodies. - CONCLUSION : These findings demonstrate that FFA-containing formulations can repair damaged ex vivo skin and point to a repair mechanism in which topically applied palmitic and stearic acids, (which boost lipid levels and elongation) can increase the production and transport of lipids into a repaired SC and thus rebuild an effective skin barrier. Note de contenu : - MATERIALS AND METHODS : Formulations - Ex vivo skin, tape-stripping and treatment - Biopsies of treated areas - Biopsy collection and processing for histology and cornified layer analysis - H&E staining of sections - Immunohistochemistry for Ki67 - Imaging and quantitation of epidermal area and Ki67 staining - Corneocyte layer quantification - Sample preparation for transmission electron microscopy (TEM) - Quantitative analysis of lamellar bodies (LB) and intercellular lipid lamellae (ICLL) - Statistical analyses - RESULTS : Ex vivo skin response to tape stripping - Removal of SC and its recovery in ex vivo skin - Topical free fatty acid-containing formulations (FFA) increased SC layer recovery - Topical free fatty acid-containing formulations (FFA) increased intercellular lipid lamella (ICLL) formation and length - Topical FFA treatment stimulates lamellar body production and secretion DOI : https://doi.org/10.1111/ics.12961 En ligne : https://drive.google.com/file/d/1dBCIelfqOUS_L1KmdXWBuOYVPw4fintT/view?usp=drive [...] Format de la ressource électronique : Pdf Permalink : https://e-campus.itech.fr/pmb/opac_css/index.php?lvl=notice_display&id=41350 [article]

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