Results from in vitro and ex vivo skin aging models assessing the antiglycation and anti-elastase MMP-12 potential of glycylglycine oleamide

Abstract

BackgroundGlycation is an aging reaction of naturally occurring sugars with dermal proteins. Type I collagen and elastin are most affected by glycation during intrinsic chronological aging.AimTo study the in vitro and ex vivo assays in human skin cells and explants and the antiaging effects of glycylglycine oleamide (GGO).Materials and methodsThe antiglycation effect of GGO was assessed in a noncellular in vitro study on collagen and, ex vivo, by immunohistochemical staining on human skin explants (elastin network glycation). The ability of GGO to contract fibroblasts was assessed in a functional assay, and its anti-elastase (MMP-12) activity was compared to that of oleic acid alone, glycylglycine (GG) alone, and oleic acid associated with GG.ResultsIn vitro, GGO reduced the glycation of type I collagen. Ex vivo, GGO restored the expression of fibrillin-1 inhibited by glycation. Furthermore, GGO induced a tissue retraction of almost 30%. Moreover, the MMP-12 activity was inhibited by up to 60%.ConclusionUnder the present in vitro and ex vivo conditions, GGO prevents glycation of the major structural proteins of the dermis, helping to reduce the risk of rigidification. By maintaining the elastic function of the skin, GGO may be a promising sparring partner for other topical antiaging agents.

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

“…In a model of skin aging using UV irradiation on human skin explants, an antiaging cosmetic cream containing 0.05% RAL associated with Pre‐tocopheryl ® significantly reduced the UV‐generated free radicals, repaired laminin, elastic fiber and collagen network and stimulated collagen synthesis compared with a cream containing RAL alone . Another experimental study investigating the association of RAL, Pre‐tocopheryl ® and GGO (Relastide ® ) on fibroblasts and skin explants showed that these molecules exhibit antiaging properties by reversing the effects of oxidative damage, increasing proteasomal activity, stimulating the production of type I collagen, and decreasing metalloproteinase‐12 synthesis associated with skin aging . Those ex‐vivo studies support our observations that topical RAL in combination with Pre‐tocopheryl ® and GGO (Relastide ® ) is effective in improving skin appearance by acting on various cellular mechanisms involved in skin aging.…”

“…Glycylglycine Oleamide (GGO, Relastide ® ) is a lipopeptide with antioxidant and antiglycation properties. It was found to have a synergistic effect in association with RAL and protects skin elasticity . Pre‐tocopheryl ® , a vitamin E precursor, is a photostable antioxidant which was shown to increase collagen synthesis in vitro when associated with RAL .…”

A new dermocosmetic containing retinaldehyde, delta-tocopherol glucoside and glycylglycine oleamide for managing naturally aged skin: results from in vitro to clinical studies

“…Our ex vivo skin model confirmed that UVA induces alteration of the skin structure demonstrated by Boisnic et al 26 When adding, during the 48 hours following UVA irradiation, the tested combination, a restoration and improvement of the expression level of genes coding for the formation of elastin fibers, the cell–ECM interaction and the cytoskeleton, such as LOXL2 , FBLN1 , FBLN5 , FBN2 , ITGB1 , PXN and ACTA2 were observed paralleling findings made earlier when RAL, GGO and delta-TC were tested individually or after application of a combination of RAL and delta-TC in ex vivo skin samples. 18 , 24 , 26 , 27 The presently tested combination of 3 actives thus effectively protected skin tissues from UVA radiation and preserved the structure of both elastin and fibrillin-rich fibers preventing UVA-induced photoaging and preserving the elastic system organization. It is of note that a placebo preformulation was not efficient to protect the dermis against UVA, confirming the topical efficacy of the combined active ingredients.…”

“…Both are considered potential targets of antiaging products as demonstrated recently through in vitro and ex vivo studies on GGO. 24 …”

Novel Facial Cream Containing Carnosine Inhibits Formation of Advanced Glycation End-Products in Human Skin

“…Several published studies or in vitro studies have linked carnosine with a protection against glycation when taken orally [6,7]. To our knowledge the antiglycation efficacy of topical carnosine in skin has not been published.…”