Antiaging efficacy of a retinaldehyde‐based cream compared with glycolic acid peel sessions: A randomized controlled study

Rouvrais, C.; Baspeyras, Martine; Mengeaud, V.; Rossi, Ana B.

doi:10.1111/jocd.12511

Cited by 7 publications

(7 citation statements)

References 18 publications

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“… − Research on melatonin has attracted considerable attention through its applications to the cosmetics industry that uses it as an antioxidant and skin immune strengthener. It is believed that to some extent, melatonin is more suitable than vitamin C, vitamin E, and phenolic acid for these purposes as it does not appear to generate highly toxic hydroxyl radicals. − Melatonin also protects the body against UV-induced oxidative stress-mediated damaging through the melatoninergic anti-oxidative system. , This process eliminates the reactive oxygen species in the skin by the biotransformation of melatonin to 2-hydroxymelatonin, 4-hydroxymelatonin, and consecutively to N 1 -acetyl- N 2 -formyl-5-methoxykynuramine. Recently, suggestions have been made that melatonin may have therapeutic properties against the Covid-19 virus. , Melatonin and its metabolites are strongly lipophilic and are metabolized in the body by the cytochrome P450 CYP1A subfamily. , …”

Section: Introductionmentioning

confidence: 99%

Mechanism of Melatonin Metabolism by CYP1A1: What Determines the Bifurcation Pathways of Hydroxylation versus Deformylation?

2022

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Melatonin, a widely applied cosmetic active ingredient, has a variety of uses as a skin protector through antioxidant and anti-inflammatory functions as well as giving the body UV-induced defenses and immune system support. In the body, melatonin is synthesized from a tryptophan amino acid in a cascade of reactions, but as melatonin is toxic at high concentrations, it is metabolized in the human skin by the cytochrome P450 enzymes. The P450s are diverse heme-based mono-oxygenases that catalyze oxygen atom-transfer processes that trigger metabolism and detoxification reactions in the body. In the catalytic cycle of the P450s, a short-lived high-valent iron(IV)–oxo heme cation radical is formed that has been proposed to be the active oxidant. How and why it activates melatonin in the human body and what the origin of the product distributions is, are unknown. This encouraged us to do a detailed computational study on a typical human P450 isozyme, namely CYP1A1. We initially did a series of molecular dynamics simulations with substrate docked into several orientations. These simulations reveal a number of stable substrate-bound positions in the active site, which may lead to differences in substrate activation channels. Using tunneling analysis on the full protein structures, we show that two of the four binding conformations lead to open substrate-binding pockets. As a result, in these open pockets, the substrate is not tightly bound and can escape back into the solution. In the closed conformations, in contrast, the substrate is mainly oriented with the methoxy group pointing toward the heme, although under a different angle. We then created large quantum cluster models of the enzyme and focused on the chemical reaction mechanisms for melatonin activation, leading to competitive O-demethylation and C6-aromatic hydroxylation pathways. The calculations show that active site positioning determines the product distributions, but the bond that is activated is not necessarily closest to the heme in the enzyme–substrate complex. As such, the docking and molecular dynamics positioning of the substrate versus oxidant can give misleading predictions on product distributions. In particular, in quantum mechanics cluster model I, we observe that through a tight hydrogen bonding network, a preferential 6-hydroxylation of melatonin is obtained. However, O-demethylation becomes possible in alternative substrate-binding orientations that have the C6-aromatic ring position shielded. Finally, we investigated enzymatic and non-enzymatic O-demethylation processes and show that the hydrogen bonding network in the substrate-binding pocket can assist and perform this step prior to product release from the enzyme.

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Section: Introductionmentioning

confidence: 99%

Mechanism of Melatonin Metabolism by CYP1A1: What Determines the Bifurcation Pathways of Hydroxylation versus Deformylation?

2022

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“…While the evidence for efficacy is less voluminous and compelling than for tretinoin that probably reflects the fact that tretinoin is the active form, the precursors appear to be well tolerated. 38 , 39 The evidence for the clinical efficacy of the ester derivatives such as retinyl acetate and retinyl palmitate is equivocal. 40 , 41 …”

Section: Resultsmentioning

confidence: 99%

Cosmeceuticals: The Principles and Practice of Skin Rejuvenation by Nonprescription Topical Therapy

Glass

2020

Aesthetic Surgery Journal Open Forum

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Background Aesthetic practice relies on a harmonious relationship between medicine and commerce. Bridging the gap are a large number of skincare products that make therapeutic claims while avoiding the regulatory framework of pharmaceuticals. In this grey area we find ourselves poorly disposed to counsel our patients wisely as the industry is expanding faster than empirical evidence of efficacy and safety can be acquired. To serve our patients and engage with industry we must understand the theoretical principles and evaluate the clinical evidence in practice. Objectives The purpose of this paper is to classify cosmeceuticals by method of action, explain how they work in principle with reference to skin aging and evaluate the clinical evidence for them. Methods A literature and cosmetic clinic website search was conducted to establish a list of the most commonly advertised cosmeceuticals and a peer-reviewed literature search was then conducted to establish the clinical evidence for them. Results A huge number of cosmeceuticals are marketed for skin rejuvenation but almost invariably they fall into one of four categories. These include the induction of tissue repair mechanisms, inflammatory modulation, scavenging of reactive oxygen species or a combination of the three. With the exception of retinol derivatives and hydroxyl acids the clinical evidence is limited, despite promising preclinical evidence for several cosmeceuticals. Conclusions Cosmeceuticals reside within a highly competitive ecosystem and are often brought to market based on preclinical, not clinical evidence. Success and failure will largely be governed by the establishment of clinical evidence in retrospect.

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“…Several in vitro and in vivo studies demonstrate the ability of retinol and its derivatives to penetrate across the epithelium exerting a biological effect in keratinocyte cells differentiation, corneocyte exfoliation, and regulating fibroblast proliferation in the dermis by angiogenesis, collagen and elastin synthesis stimulation [14,15]. The retinoids receptor signaling mediated by the interaction with specific nuclear receptors, such as retinoid X receptors (RXRs) and retinoic acid receptors (RARs), increases the production of procollagen, thus leading to the synthesis of new collagen and, at the same time, inhibits Matrix Metalloproteinases (MMPs) [16][17][18][19][20][21][22]. In addition, many articles show the potential effect of a new dermocosmetic containing retinaldehyde (RAL), delta-tocopherol glucoside, and glycylglycine oleamide with in vitro and clinical studies as well as the restoration and the improvement of the ECM complex in UV-irradiated fibroblast models [23][24][25][26][27].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Anti-Photoaging Effects of a Novel Cosmeceutical Containing a Retinoids Mixture Using In Vitro Cell Models

et al. 2021

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Physiological ageing due to the passing of time and prolonged exposure to harmful sun rays generate wrinkles and reduce skin elasticity. These visible and clinical signs can be prevented or reversed by known strategies, such as the daily use of cosmetic products with antioxidant combinations or retinoids. A new dermocosmetic formulation enriched with a complex of retinoids, called RETINOIDS SERUM, was investigated through in vitro assays using human skin cells. The experiments were carried out to assess the anti-ageing activity in normal human dermal fibroblasts (NHDF) and epidermal keratinocytes (HaCaT). After the preliminary MTT assay, the proliferation together with the synthesis of collagen and elastin fibers was performed on NHDF cells after 24 h treatment with the two non-cytotoxic concentrations. Using UVB-irradiated HaCaT cells, the measurement of matrix metalloproteinase-1 (MMP-1) levels was also investigated. In vitro studies show that the dermocosmetic product improves collagen and elastin synthesis and the renewal of dermal fibroblasts. Moreover, a reduction in the MMP-1 secretion was also highlighted in UVB-irradiated HaCaT cells. These results suggest that the cosmetic formulation containing functional compounds such as retinoids can be useful to prevent the natural sign of ageing.

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Antiaging efficacy of a retinaldehyde‐based cream compared with glycolic acid peel sessions: A randomized controlled study

Abstract: A dermocosmetic cream containing 0.1% RAL, GGO (Relastide ) and Pre-tocopheryl is as effective as 3 sequential GA peels, better tolerated, and is an alternative in the management of photoaged skin.

Cited by 7 publications

References 18 publications

Mechanism of Melatonin Metabolism by CYP1A1: What Determines the Bifurcation Pathways of Hydroxylation versus Deformylation?

Mechanism of Melatonin Metabolism by CYP1A1: What Determines the Bifurcation Pathways of Hydroxylation versus Deformylation?

Cosmeceuticals: The Principles and Practice of Skin Rejuvenation by Nonprescription Topical Therapy

Evaluation of Anti-Photoaging Effects of a Novel Cosmeceutical Containing a Retinoids Mixture Using In Vitro Cell Models

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