中草藥活性分子抑制酪胺酸酶之美白成份探討

Investigation of Tyrosinase Inhibition by Chinese Herbal Medicine Active Compounds as Skin-whitening Ingredients

本研究從衛生福利部國家中醫藥研究所中草藥化合物庫篩選出針對抑制酪胺酸酶功效之研究，我們發現8種中草藥活性分子分別來自於牛至、青藤、倒地鈴、黃藤、茜草、山埔姜、赤芍、金銀花。利用酪胺酸酶的酵素活性抑制實驗，分對照組（市售的麴酸（IC50=40.69μM）和熊果素（IC50=368.93μM））和實驗組（8種中草藥活性分子）進行，實驗結果發現，來自於牛至、青藤、倒地鈴、黃藤的中草藥活性分子和麴酸抑制酪胺酸酶的活性IC50約100μM以下；同樣的來自於茜草、山埔姜、赤芍、金銀花的中草藥活性分子抑制酪胺酸酶的活性介於麴酸和熊果素之間。除此之外，透過分子模擬方法闡明中草藥活性分子如何和酪胺酸酶進行交互作用機制，這些結果證實來自於中草藥活性分子具有潛力當作功能性化妝品抑制黑色素生成的活性添加劑。

This study investigates the tyrosinase inhibitory effect of 8 active compounds of TCM database from National Research Institute of Chinese Medicine, Ministry of Health and Welfare. We further discover eight Chinese herbal medicine small molecules derived from Origanum vulgare L., Sinomenium acutum, Cardiospermum halicabum, Calamus quiquesetinervius, Rubia akane Nakai, Radix paeoniae rubra, Messerschmidia argentea (L.) Johnston and Lonicera japonica. Enzyme activity inhibition experiments for tyrosinase were conducted for control groups, which contain commercially available kojic acid (IC50 = 40.69 μM) and arbutin (IC50 = 368.93 μM), and experimental groups, which use the eight different small molecules. The results reveal that small molecules from Origanum vulgare L., Sinomenium acutum, Cardiospermum halicabum, Calamus quiquesetinervius and kojic acid have IC50 about less than 100 μM in tyrosinase inhibitory activity. Similarly, small molecules from Rubia akane Nakai, Radix paeoniae rubra, Messerschmidia argentea (L.) Johnston and Lonicera japonica demonstrate activity between kojic acid and arbutin. In addition, molecular simulation was performed to study the interaction mechanism of these small molecules with tyrosinase. These results confirm the potential use of small molecules from Chinese herbal medicines as active additives in cosmetic products to inhibit melanin formation.