Inspired by vitamin A for anti‐ageing: Searching for plant‐derived functional retinoid analogues

Abstract

Background Cosmetic treatments that inspire one's appearance to resemble their younger portrait often utilize ingredients that confer acute effects, particularly hydration by creating hydrophobic barriers or transient elevation of barrier water content. But superior therapies successfully promote morphogenesis of the dermal‐epidermal junction, inspiring extracellular matrix (ECM) formation. This can be achieved by agonism of the very well‐known retinoid nuclear receptors using the endogenous ligand all‐trans retinoic acid (tRA), tRA precursors or plant‐based functional analogues, with reduced side effects. Aims, Materials and Methods While there are already many promising cosmetic ingredients available from the world's flora, higher potency is favoured, so increasing known candidates is a worth undertaking. Functional analogues of retinoic acid can be identified by culturing fibroblasts with lipophilic candidates from the plant kingdom and assessing gene‐arrays. Modern approaches to validating these findings include the coculturing of fibroblasts with keratinocytes as a measure to predict the potential effects of crosstalk. Results and Discussion In this regard, the most promising plant‐derived candidates are of terpene or meroterpene origin, including derivatives of squalene and phytol. Surprisingly pimaric or abietic acids and labdane diterpenes are also noteworthy agonists of the retinoic acid receptor, stimulating collagen expression in dermal fibroblasts. Conclusion There are numerous derivatives of these terpenes available from the world's flora and research conducted thus far encourages further screening of these chemical candidates.

A Harungana madagascariensis extract with retinol‐like properties: Gene upregulations and protein expressions in human fibroblasts and skin explants

“…Collectively, the results of this first study pinpoint at an induction of genes by HME that shows a similar pattern to that of retinols. Some plant compounds have been shown to induce gene upregulation partially overlapping that of retinol [35]. So far, only bakuchiol, a meroterpene phenol from the seeds of Psoralea corylifolia , was shown to have really a retinol‐like anti‐ageing gene induction profile [15].…”

Multidirectional activity of bakuchiol against cellular mechanisms of facial ageing ‐ Experimental evidence for a holistic treatment approach

“…Previous studies have implied that bakuchiol acts as a functional analogue of retinol [19–21]. Bakuchiol, thus, appears to be a promising alternative to retinol for facial antiageing treatments.…”

“…Bakuchiol was suggested to exhibit retinol-like functions, as in a skin substitute model, both substances show similar gene expression patterns in vitro [19] and an improvement of cutaneous photodamage in vivo [20]. Hence, it has also been referred to as a plantderived functional retinoid analogue [21]. Further studies demonstrated antioxidant [19,[22][23][24], anti-inflammatory [19,[25][26][27], antibacterial [28] as well as antiproliferative and antitumor effects [29,30] of bakuchiol.…”

Secondary Terpenes in Cannabis sativa L.: Synthesis and Synergy

“…In vitro, phytol has also been shown to increase the release of CA 2+ reserves via activation of GPR40, a G-protein-coupled receptor that normally binds to free fatty acids, with an EC 50 of 34.5 µM [ 170 ]. The activation of PPARs, RXRs, and GPR40 by phytol may also be of potential therapeutic benefit for the treatment of diabetes, and because of the ability to activate RXR receptors, phytol is also being pursued by the cosmeceutical industry as an anti-aging treatment in lieu of retinol (which is not well tolerated by all individuals due to its activation of TRPV1) [ 171 , 172 ].…”