Isolation of Resveratrol from Vitis Viniferae Caulis and Its Potent Inhibition of Human Tyrosinase

Abstract

Tyrosinase (TYR) catalyzes rate-limiting reactions of cellular melanin synthesis, and its inhibitors are of commercial interest as potential skin whitening agents. However, the limited availability of human TYR makes the screening of TYR inhibitors difficult. To overcome this hurdle, we transformed nonmelanocytic human embryonic kidney (HEK) 293 cells to express human TYR constitutively. Using these cells as a source of human TYR, the ethanolic extracts of 52 medicinal plants grown in Korea were tested for human TYR activity, and the extract of Vitis Viniferae Caulis (dried stems of the grape tree, Vitis vinifera L.) was found to inhibit human TYR activity potently. An active compound was isolated from this extract by solvent fractionation followed by liquid column chromatography and identified as resveratrol by spectroscopic and chromatographic analyses. Resveratrol was determined to be a highly potent inhibitor of human TYR (IC50 = 0.39 μg mL−1) as compared with p-coumaric acid (IC50 = 0.66 μg mL−1) and arbutin (IC50 > 100 μg mL−1) and inhibited melanin synthesis by human epidermal melanocytes at subtoxic concentrations. This study suggests that resveratrol and resveratrol-containing extracts of Vitis Viniferae Caulis have a potential use as skin whitening agents.

Resveratrol-Enriched Rice Down-Regulates Melanin Synthesis in UVB-Induced Guinea Pigs Epidermal Skin Tissue

“…Recent reports have shown that resveratrol produced therapeutic effects against hyperplastic skin disorders by inhibiting keratinocyte proliferation , inhibited skin photoaging by acting as a Sirt-1 agonist (Lee et al, 2010), and showed anti-cancer effects in human melanoma cell lines (Niles et al, 2003). The anti-melanogenic effects of resveratrol and resveratrol analogs have already been reported by many other groups (Ohguchi et al, 2003;Song et al, 2012;Bae et al, 2013;Park and Boo, 2013;Park et al, 2014). We previously demonstrated the depigmentation effects of resveratrol in UVB-treated guinea pigs , too.…”

“…Interestingly, RR shows synergistic effects in comparison that of each resveratrol or rice alone (Baek et al, 2013;Baek et al, 2014). Several reports show that resveratrol decreases the expression of tyrosinase (Franco et al, 2012;Zheng et al, 2012;Bae et al, 2013;Park and Boo, 2013;Park et al, 2014), and Jun et al reported that gamma-oryzanol from rice extract dually inhibited cellular melanogenesis, too (Jun et al, 2012). Because each of resveratrol and rice had anti-melanogenic effects, we expected that RR would produce synergistic antimelanogenic effects and thus have some advantages over treatment with rice or resveratrol alone.…”

Kinetics of Tyrosinase Inhibitory Activity Using Vitis vinifera Leaf Extracts

“…As in Figure 3, the inhibition of tyrosinase activity increased with the added amount of kojic acid, and its IC 50 was 0.014 mg/mL. The tyrosinase inhibitory activity of Vitis vinifera L. was reported in the previous study using the extract of dried stems of the grape tree [28]. Although RVLE solution does not outperform kojic acid as an inhibitor, it was still generally recognized as a safe natural ingredient and could be safely used in cosmetic products [29].…”

Cosmetic Potential of a Liotropic Liquid Crystal Emulsion Containing Resveratrol

“…Liquid crystal systems are more stable when compared with other emulsions because they promote higher cutaneous hydration by retaining water in the corneal layer and delivering the sustained release of active ingredients to target areas. When the chemical structure is compared with the composition and disposition of both lipids and water present in the epidermis, an emulsion is the best option to address cutaneous issues in the cosmetic field, in particular, as an antiaging treatment [9][10][11][12][13][14].…”

“…In this context, several advantages of using the liquid crystal formulation in cosmetics include: (i) visual features, some crystals possess properties such as thermochromism (some substances change their colors at different temperatures); (ii) protective properties, substances incorporated in the liquid crystal matrix, or the formulation made with it, have protection against photo-or thermo-degradation because of its microstructure; (iii) hydrating properties, promote an increase in water retention in the stratum corneum layer resulting in a higher cutaneous hydration and an extended release of substances because its chemical structure is similar to the composition arrangement of lipids and water in the human epidermis; and (iv) stability, have a higher physicochemical stability when compared with traditional emulsions [12][13][14].…”