Dietary polyphenol oleuropein and its metabolite hydroxytyrosol are moderate skin permeable elastase and collagenase inhibitors with synergistic cellular antioxidant effects in human skin fibroblasts
Huifang Li, Hao He, Chang Liu, Toyosi Akanji, Justin Gutkowski, Ruilian Li, Huiqun Ma, Yinsheng Wan, Panpan Wu, Dongli Li, Navindra P. Seeram, Hang Ma
Abstract
Oleuropein (OLE) and hydroxytyrosol (HT) are dietary polyphenols with skin beneficial effects but their effects on skin-ageing-related enzymes are not clear. Herein, we evaluated their inhibitory effects on elastase and collagenase. OLE and HT (62.5–1 000 μM) showed moderate anti-elastase and anti-collagenase effects (5.1–26.3%, 5.8–12.2% and 12.6–31.0%, 11.6–31.9% inhibition, respectively). Combinations of OLE and HT (1:1 ratio) exerted synergistic inhibitory effects on elastase, which were supported by their combination index (CI), kinetic assay and computational docking. Moreover, HT (100 μM) reduced hydrogen peroxide (H2O2)-induced cytotoxicity and reactive oxygen species (ROS) in human dermal fibroblast cells by 21.8 and 15.2%, respectively. In addition, combinations of OLE and HT (6.25/6.25–100/100 μM) exerted synergistic cytoprotective effects by reducing ROS levels by 7.6–37.3% with CIs of 0.17–0.44, respectively. The findings from this study support the cosmeceutical activities of OLE and HT but further research is warranted to evaluate their anti-skin-ageing effects using in vivo models.