Ye Sanghyun, Lee Seonju, Kang Seongsu, Jun Seung-Hyun, Kang Nae-Gyu
LG Household and Health Care R&D Center, Seoul 07795, Republic of Korea.
Biomolecules. 2025 Feb 17;15(2):296. doi: 10.3390/biom15020296.
Retinol is well-known anti-aging material in the cosmetics industry, owing to its proven superior efficacy both in vitro and in vivo. Despite its high efficacy, retinol is associated with limitations, such as skin irritation and its potential photodegradation. Retinol is converted into retinoid acid within cells, which then exerts a cellular response by activating both the retinoic acid receptor (RAR) and retinoid x receptor (RXR). Noting that RAR activity is associated with skin irritation and RXR activation alone can enhance skin-related indicators without inducing inflammation, we developed an alternative approach for skin anti-aging focusing solely on RXR activation. We found that combined treatment of andrographolide and extract successfully activated RXR alpha and enhanced gene expression. Moreover, we investigated their efficacy using dermal fibroblasts and keratinocytes and found that they enhanced the gene expression of extracellular matrix (ECM) proteins with anti-oxidant and anti-inflammation efficacies. Finally, in a human clinical trial, we confirmed that our materials successfully improved wrinkles in various areas, skin elasticity and hydration without causing irritating side effects. These findings highlight the potential of our RXR alpha-activating materials as an anti-wrinkle solution that avoids the typical side effects associated with retinol.
视黄醇是化妆品行业中著名的抗老化物质,因其在体外和体内均已证实具有卓越功效。尽管视黄醇功效显著,但它也存在一些局限性,如皮肤刺激性及其潜在的光降解性。视黄醇在细胞内会转化为维甲酸,然后通过激活维甲酸受体(RAR)和维甲酸X受体(RXR)来引发细胞反应。鉴于RAR活性与皮肤刺激有关,且仅激活RXR就能增强皮肤相关指标而不引发炎症,我们开发了一种仅专注于激活RXR的皮肤抗老化替代方法。我们发现穿心莲内酯和提取物联合处理成功激活了RXRα并增强了基因表达。此外,我们使用真皮成纤维细胞和角质形成细胞研究了它们的功效,发现它们增强了具有抗氧化和抗炎功效的细胞外基质(ECM)蛋白的基因表达。最后,在一项人体临床试验中,我们证实我们的材料成功改善了各个部位的皱纹、皮肤弹性和水合作用,且未产生刺激性副作用。这些发现凸显了我们的RXRα激活材料作为一种抗皱解决方案的潜力,该方案可避免与视黄醇相关的典型副作用。