2-Mercaptonicotinoyl glycine prevents UV-induced skin darkening and delayed tanning in healthy subjects: A randomized controlled clinical study.

BACKGROUND: Chronic nonextreme sun exposure induces two mechanisms of skin pigmentation, causing immediate darkening and delayed tanning. A new molecule, 2-mercaptonicotinoyl glycine (2-MNG), has been shown in vitro to inhibit both immediate darkening and new melanin synthesis via covalent conjugation of the thiol group of 2-MNG to melanin precursors. OBJECTIVE: To evaluate 2-MNG in preventing both mechanisms in vivo. METHODS: In a randomized, intra-individual and controlled study, 33 subjects with melanin-rich skin were exposed to UV daylight on designated areas on the back and treated with a cosmetic formula containing 0.5% or 1% 2-MNG alone or 0.5% 2-MNG in association with lipohydroxy acid (LHA, 0.3%) plus Mexoryl-SX (MSX, 1.5%). The respective vehicles were used as controls and 4-n-butyl-resorcinol (4-n-BR, 2.5%) as a positive reference. RESULTS: 2-MNG alone significantly reduced immediate darkening and inhibited new melanin production when compared with vehicle, with higher performance at 1% than at 0.5%. 2-MNG at 0.5% in association with LHA and MSX showed significantly higher performance than 2-MNG 0.5% alone. 2-MNG at 0.5% and 1% showed significantly better performance than 4-n-BR. CONCLUSIONS: 2-MNG inhibited both UV-induced skin pigmentation mechanisms in vivo. The association of 2-MNG with LHA plus MSX showed the highest efficacy on melanin-rich skin with pigmentation induced by UV exposure.

Polygonum multiflorum Radix extract protects human foreskin melanocytes from oxidative stress in vitro and potentiates hair follicle pigmentation ex vivo.

OBJECTIVE: To examine the ability of an extract from traditional Chinese medicine, Polygonum multiflorum Radix, to protect melanocyte viability from oxidative stress, a key mechanism in the initiation and progression of hair greying. METHODS: To assess the antioxidant capacity of Polygonum multiflorum Radix extract, primary human foreskin melanocytes were treated with a commercially available Polygonum multiflorum Radix extract added to culture medium and exposed to hydrogen peroxide (H2 O2 ), using intracellular reactive oxygen species concentrations and glutathione/protein ratios as endpoints. To improve solubility for cosmetic uses, a new Polygonum multiflorum Radix extract was derived. As hair greying is the consequence of melanocyte disappearance in an oxidative stress environment, we checked whether the antioxidant capacity of the new Polygonum multiflorum Radix extract could preserve melanocyte viability in response to H2 O2 -induced oxidative stress, and preserve pigmentation within ex vivo human hair follicles. RESULTS: In vitro treatment of primary human foreskin melanocytes with traditional available Polygonum multiflorum Radix extract resulted in decreased intracellular ROS accumulation in response to H2 O2 exposure with a concomitant preservation of glutathione-to-protein ratio, consistent with a protective response against H2 O2 exposure and demonstrating the promise of this extract for protecting melanocytes against oxidative stress. Melanocytes treated with the improved Polygonum multiflorum Radix extract exhibited attenuated H2 O2 -induced cell death, demonstrating a clear cytoprotective effect. Treatment of ex vivo human hair follicles with the improved Polygonum multiflorum Radix extract resulted in a higher level of melanin compared to vehicle-treated controls, demonstrating an ex vivo protective effect on hair pigmentation. CONCLUSION: Polygonum multiflorum Radix extract protects in vitro primary human foreskin melanocytes from the deleterious effects of H2 O2 exposure and improves pigmentation within ex vivo human hair follicles, demonstrating the utility of Polygonum multiflorum Radix extract as a potential active ingredient for the protection of melanocytes against premature death. This data provides in vitro mechanistic evidence consistent with existing in vivo studies for the use of Polygonum multiflorum Radix extract as a strategy for the prevention of oxidative stress-induced hair greying, in line with traditional Polygonum multiflorum Radix uses.

The skin-depigmenting potential of Paeonia lactiflora root extract and paeoniflorin: in vitro evaluation using reconstructed pigmented human epidermis.

OBJECTIVE: The roots of the herb Paeonia lactiflora ('White Peony') are used in association with other herbs in traditional clinical cosmetic practice in China as oral treatment for skin pigmentary disorders, such as brown or dark pigmentary spots. However, the skin-depigmenting potential of Paeonia lactiflora root extract and its main ingredient paeoniflorin has been scarcely investigated by topical application. The purpose of this study was to evaluate the efficacy of Paeonia lactiflora root extract and paeoniflorin as skin whitening agent in cosmetic application. METHODS: Paeonia lactiflora root extract (containing 53.25% of paeoniflorin) and paeoniflorin (97% purity) were applied topically on reconstructed pigmented human epidermis model, a three-dimensional (3D) human skin equivalent, showing morphological and functional characteristics similar to those of in vivo human skin. Two specific methods were used for quantifying melanin inside the reconstructed pigmented epidermis: Fontana-Masson staining (2D quantification) and multiphoton microscopy (3D quantification). RESULTS: Compared to vehicle (dimethyl sulfoxide DMSO), a significant decrease in 2D and 3D melanin content was observed after topical application on reconstructed pigmented epidermis of Paeonia lactiflora extract at 300 µg mL(-1) (-28% and -27%, respectively) and paeoniflorin at 120 µg mL(-1) /250 µM (-30% and -23%, respectively), which is in the same order of magnitude as the positive reference 4-n-butylresorcinol at 83 µg mL(-1) /500 µM (-26% and -40%, respectively). CONCLUSION: These results demonstrate, for the first time, the depigmenting potential of paeoniflorin and thus the potential interest of using Paeonia lactiflora root extracts containing paeoniflorin in cosmetic or dermatological applications for reducing the severity of some hyperpigmented skin disorders.