4-Hydroxyderricin from Angelica keiskei: Analysis, Preparation, and Multiple Skin Care Effects

Introduction: The content of the bioactive component 4-hydroxyderricin (4-HD) in the roots, stems, and leaves of Angelica keiskei (Umbelliferae), a well-known medicinal and edible plant, was analyzed by HPLC. The dry root contained the highest level (2. 69 ± 0.09 mg/g) of 4-HD, which was then prepared and spectroscopically identified by column chromatography. Methods: The multiple skin care activities of 4-HD, including skin whitening, anti-allergy, and antiinflammation, were evaluated on enzymatic and cellular models. 4-HD showed a significant inhibitory effect on mushroom tyrosinase, and it could also strongly suppress the activity of tyrosinase in B16F10 cells. A molecular docking study revealed that 4-HD could closely bind to tyrosinase through hydrogen bonding and hydrophobic interactions. Results: In the anti-allergic assay, 4-HD could effectively reduce the degranulation rate in the neutral red staining test and largely down-regulate the release level of β-HEX in RBL-2H3 cells at the concentration of 5 μM. 4-HD decreased the production of NO in RAW264.7 cells induced by lipopolysaccharide (LPS), showing its anti-inflammatory effect. Conclusion: The skin whitening, anti-allergic, and anti-inflammatory effects of 4-HD have clearly demonstrated its potential usage in the pharmaceutical and cosmetic industries.