Skin Moisturizing Effect through the Stimulation of the Cornified Cell Envelope Formation by Bis-Glyceryl Ascorbate

Misaki Doi, Sayaka Nakamura, N. Taira, Y. Katsuyama, H. Masaki, M. Yoshioka
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Abstract

Ascorbic acid ( AsA ) is well-known as a multifunctional water soluble vitamin that shows anti-pigmentation effects in epidermal melanocytes and stimulates collagen synthesis in dermal fibro-blasts. However, AsA has some disadvantages in cosmetic formulations since it is quite unstable in aqueous solutions and emulsions. To improve the stability of AsA in cosmetic formulations, we developed a novel AsA derivative, bis-glyceryl ascorbate ( VC-DG ) , which introduces 2 glycerol groups into AsA, and confirmed that VC-DG has a higher stability than AsA and maintains its bioactivities as well as AsA. In this study, we evaluated the skin moisturizing effects of VC-DG focusing on the cornified cell envelope ( CE ) to develop its unique biological activities. As the re-sults, VC-DG up-regulated the mRNA and protein expression levels of CE-related substances, such as involucrin, loricrin and transglutaminase-1, which in turn significantly increased CE formation in normal human epidermal keratinocytes. Additionally, topical application of VC-DG increased the protein expression levels of involucrin, loricrin and transglutaminase-1 in the spi-nous and / or granular cell layers of reconstructed human epidermal equivalents. In a human vol-unteer test, the application of VC-DG increased the skin surface water content. Therefore, we consider VC-DG to be an effective ingredient that improves skin hydration through enhancing CE formation.
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双甘油抗坏血酸通过刺激角质细胞包膜形成的皮肤保湿效果
抗坏血酸(AsA)是一种众所周知的多功能水溶性维生素,在表皮黑色素细胞中具有抗色素沉着作用,并刺激真皮成纤维细胞中的胶原合成。然而,AsA在化妆品配方中有一些缺点,因为它在水溶液和乳液中非常不稳定。为了提高AsA在化妆品配方中的稳定性,我们开发了一种新的AsA衍生物,双甘油酰抗坏血酸酯(VC-DG),它在AsA中引入了2个甘油基团,并证实VC-DG具有比AsA更高的稳定性,并且保持了AsA的生物活性。本研究以VC-DG为研究对象,对VC-DG的皮肤保湿作用进行了研究,以揭示VC-DG独特的生物活性。VC-DG上调CE相关物质如天花素、氯仿素和谷氨酰胺转胺酶-1的mRNA和蛋白表达水平,从而显著增加正常人表皮角化细胞CE的形成。此外,局部应用VC-DG增加了重建的人表皮等效物的刺状和/或颗粒状细胞层中天青苷、氯丙苷和转谷氨酰胺酶-1的蛋白表达水平。在人体志愿者试验中,VC-DG的应用增加了皮肤表面含水量。因此,我们认为VC-DG是一种通过促进CE形成来改善皮肤水合作用的有效成分。
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