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62 LIFESTYLE COSMETICS


in our lungs, where bitter substances induce bronchial relaxation. Yet bitter taste receptors also exist in heart, or in adipose tissue where they modulate adipogenesis, or activate the immune system.12 Interesting from a cosmetic perspective is


the fact that bitter taste receptors also exist in skin. Recent research identified bitter taste receptors in keratinocytes. Here, they trigger the synthesis of skin barrier lipids and proteins or induce anti-inflammatory processes.13


This


makes bitter taste receptors novel cosmetic targets to treat sensitive skin.


Andrographis paniculata - an activator of bitter taste receptors in skin Andrographolide is an extremely bitter-tasting substance isolated from the stems and leaves of Andrographis paniculata – also known as ‘King of Bitters’. It is a diterpene that selectively binds and activates human bitter taste receptors of the TAS2R family in skin keratinocytes.13 Receptor activation induces a signal cascade that leads to enhanced production of skin barrier lipids and reduces inflammatory markers, linking bitter andrographolide to skin physiology and making it a potential active substance to target sensitive skin (Figure 1).


Sweet tasting licorice root – a source of natural anti-inflammatory compounds To date, the most effective and widely prescribed compounds to combat inflammation are glucocorticoid derivatives, for example cortisol. They exhibit anti-inflammatory effects by suppressing the expression of pro-inflammatory genes and by inhibiting the production of inflammatory cytokines. Therefore, topical corticosteroid creams and ointments are the main form of therapy to control acute flares of atopic dermatitis. The growing trend of natural cosmetics


demands for plant-derived solutions as attractive alternatives for the treatment of sensitive skin or atopic dermatitis. One good example is licorice, the root of Glycyrrhiza glabra, which contains the active compound


A Restoration of Bitter Taste Receptor (TAS2R50) Normal Skin Atopic Skin


Atopic Skin + 'Bittersweet complex'


Bitter Component Bitter Receptor Activation Benefits for Sensitive Skin


Figure 1: Bitter compound andrographolide is a natural activator of bitter taste receptors. Bitter receptors are integral membrane proteins that are used by cells to convert extracellular chemical signals into intracellular responses. The signaling cascade starts by docking a bitter molecule to the receptor. The activated receptor activates a G-protein, which finally triggers the influx of Ca++ ions. In keratinocytes, the influx of Ca++ induces the production of skin barrier lipids


glycyrrhizin – one of the sweetest substances found in nature. It has 30–50 times the sweetness of sucrose. Glycyrrhizin is a triterpene glycoside and


its hydrolysate, glycyrrhetinic acid (GA), has a structure close to mineral-corticoids and glucocorticoids. For its anti-inflammatory action, GA and licorice root extract have been successfully tested in the treatment of atopic dermatitis and pruritus.7-8


The rise


of natural cosmetics makes plant-derived glycyrrhetinic acid from Glycyrrhiza glabra, as well as andrographolide from Andrographis paniculata, very attractive alternatives for the treatment of sensitive skin.


The novel approach: first system of bitter and sweet for sensitive skin The bittersweet complex, for the first time, combines bitter and sweet actives for the treatment of sensitive skin: Firstly, andrographolide, as activator of bitter taste receptors, triggers the production of skin barrier lipids. Secondly, glycyrrhetinic acid from sweet tasting licorice root, suppresses inflammation and stress reactions. This


complementary action makes the bittersweet complex unique.


The bittersweet complex restores bitter taste receptor levels in atopic skin


The study’s objective was to show that skin keratinocytes contain bitter taste receptors and to demonstrate that bittersweet complex restores a deregulated expression of bitter taste receptors in atopic skin. In the experiment, a 3D model of reconstituted human epidermis with atopic skin alterations was treated with bittersweet complex and compared to normal skin.14


The expression


of bitter taste receptors was monitored by immunofluorescence microscopy using specific antibodies. The study revealed that bitter taste


receptor TAS2R50 is expressed in human epidermis confirming earlier results.3 Furthermore, the expression level of TAS2R50 (intensity of fluorescence signal) is significantly reduced in the atopic skin model but could be restored by the bittersweet complex (Figure 2).


B 150 * 100 50 0


Normal Skin


Atopic Skin


'Bittersweet complex'


Atopic Skin +


Figure 2: The expression of bitter receptors in a human skin model is restored by bittersweet complex. (A) Immunofluorescence images of reconstituted human epidermis ‘Normal Skin Model’, ‘Atopic Skin Model’ or upon addition of the bittersweet complex. The green staining refers to labelling of TAS2R50 with specific antibodies. The signal is proportional to the amount of expressed bitter taste receptors. The blue signal highlights the cell nuclei. (B) TAS2R50 fluorescence intensity expressed in percent relative to normal skin. N = 3; Mean + SEM. Student’s t-test. * = p < 0.05, *** = p< 0.001


PERSONAL CARE April 2023 www.personalcaremagazine.com -23% *** +37%


TAS2R50 Intensity


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