Beiersdorf AG, Hamburg, Germany.
Skin Pharmacol Physiol. 2012;25(4):192-9. doi: 10.1159/000338190. Epub 2012 May 15.
BACKGROUND/AIM: Aquaporins (AQPs) present in the epidermis are essential hydration-regulating elements controlling cellular water and glycerol transport. In this study, the potential of glyceryl glucoside [GG; alpha-D-glucopyranosyl-alpha-(1->2)-glycerol], an enhanced glycerol derivative, to increase the expression of AQP3 in vitro and ex vivo was evaluated.
In vitro studies with real-time RT-PCR and FACS measurements were performed to test the induction by GG (3% w/v) of AQP3 mRNA and protein in cultured human keratinocytes. GG-containing formulations were applied topically to volunteer subjects and suction blister biopsies were analyzed to assess whether GG (5%) could penetrate the epidermis of intact skin, and subsequently upregulate AQP3 mRNA expression and improve barrier function.
AQP3 mRNA and protein levels were significantly increased in cultured human keratinocytes. In the studies on volunteer subjects, GG significantly increased AQP3 mRNA levels in the skin and reduced transepidermal water loss compared with vehicle-controlled areas.
GG promotes AQP3 mRNA and protein upregulation and improves skin barrier function, and may thus offer an effective treatment option for dehydrated skin.
背景/目的:表皮中存在的水通道蛋白(AQP)是调节细胞水和甘油转运的重要水合调节因子。本研究评估了甘油葡糖苷(GG;α-D-吡喃葡萄糖基-α-(1->2)-甘油)作为增强型甘油衍生物增加体外和离体 AQP3 表达的潜力。
采用实时 RT-PCR 和 FACS 测量进行体外研究,以测试 GG(3%w/v)对培养的人角质形成细胞中 AQP3 mRNA 和蛋白的诱导作用。将含有 GG 的制剂局部应用于志愿者受试者,并分析抽吸性水疱活检,以评估 GG(5%)是否可以穿透完整皮肤的表皮,随后上调 AQP3 mRNA 表达并改善屏障功能。
在培养的人角质形成细胞中,AQP3 mRNA 和蛋白水平显著增加。在对志愿者受试者的研究中,与载体对照区域相比,GG 显著增加了皮肤中的 AQP3 mRNA 水平,并降低了经表皮水分流失。
GG 促进 AQP3 mRNA 和蛋白的上调,并改善皮肤屏障功能,因此可能为脱水皮肤提供有效的治疗选择。