Anti-melanogenic activity of salacinol by inhibition of tyrosinase oligosaccharide processing
Anti-melanogenic activity of salacinol by inhibition of tyrosinase oligosaccharide processing
复制标题
DOI：
10.1093/jb/mvz115
复制
发表时间：
2020-05-01
影响因子：
2.7
通讯作者：
Nagata, Kozo
中科院分区：
文献类型：
--
作者：
Homma, Toshiyuki;Kageyama, Shigeki;Nagata, Kozo
通过黄褐斑和日光性雀斑（老年斑）表现出来的色素沉着过度，虽然大多数对健康无害，但困扰着许多人。控制酪氨酸酶的限速活性对于抑制过量黑色素形成最有效，因此最近的研究重点是酪氨酸酶的成熟。五层龙是一种药用植物，在印度和斯里兰卡被用来治疗糖尿病。据报道，五层龙提取物含有抑制α-葡糖苷酶活性的组分。Salacinol是五层龙提取物中的活性成分，具有独特的硫代糖硫酸盐内盐结构。在这里，我们观察到五层龙提取物的水杨酸组分与各种现有的增白剂相比具有抗黑素生成活性。虽然水杨酸酚的抗黑素生成机制可能是通过抑制酪氨酸酶活性来治疗的，这在现有的增白剂中经常发现，但水杨酸酚在体外并不抑制酪氨酸酶活性。酪氨酸酶的细胞内状态的分析表明，由于抑制N-连接的寡糖加工，成熟酪氨酸酶形式减少。Salacinol抑制加工葡萄糖苷酶I/II，这是参与的N-连接的糖基化的初始阶段。水杨酚具有高活性、低细胞毒性和高亲水性，是一种很有前途的皮肤外用增白剂候选化合物。
Hyperpigmentation that manifests through melasma and solar lentigo (age spots), although mostly harmless for health, bothers many people. Controlling the rate-limiting activity of tyrosinase is most effective for suppressing excessive melanin formation and accordingly recent research has focused on the maturation of tyrosinase. Salacia, a medicinal plant, has been used to treat diabetes in India and Sri Lanka. Salacia extract reportedly contains components that inhibit the activity of alpha-glucosidase. Salacinol, the active ingredient in Salacia extract, has unique thiosugar sulphonium sulphate inner salt structure. Here, we observed that the salacinol component of Salacia extract possesses anti-melanogenic activity in comparison to various existing whitening agents. Although the anti-melanogenic mechanism of salacinol is presumably medicated by inhibition of tyrosinase activity, which is often found in existing whitening agents, salacinol did not inhibit tyrosinase activity in vitro. Analysis of the intracellular state of tyrosinase showed a decrease in the mature tyrosinase form due to inhibition of N-linked oligosaccharide processing. Salacinol inhibited the processing glucosidase I/II, which are involved in the initial stage of N-linked glycosylation. Owing to high activity, low cytotoxicity and high hydrophilicity, salacinol is a promising candidate compound in whitening agents aimed for external application on skin.