Department of Molecular Medicine, Cell and Matrix Research Institute, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University, 680, Gukchaebosang-ro, Jung-gu, Daegu, 41944, Korea.
Gyeongbuk Natural Color Industry Institute, 181, Cheonmun-ro, Yeongcheon-si, Gyeongsangbuk-do, 38896, Korea.
Br J Dermatol. 2016 Sep;175(3):501-11. doi: 10.1111/bjd.14496. Epub 2016 Jun 28.
Abnormal deposition of melanin may cause an aesthetic skin problem; therefore, the control of unwanted excessive melanin synthesis is the major goal of cosmetic research.
To identify novel tyrosinase (TYR) inhibitors from marine plants and examine their cellular antimelanogenic effects.
The extracts of 50 marine plants endemic to Korea were screened against human TYR. Active constituents were then isolated from the selected plant extracts that showed potential and their chemical structures elucidated. Furthermore, their antimelanogenic effects were examined using murine melanoma B16/F10 cells and human epidermal melanocytes (HEM).
Among the tested extracts, that of Phyllospadix iwatensis Makino exhibited the strongest human TYR inhibitory activity. The active constituents were purified from the butanol fraction of the P. iwatensis extract and identified as hispidulin 7-sulfate and luteolin 7-sulfate. Luteolin 7-sulfate inhibited human TYR more strongly than hispidulin 7-sulfate, luteolin, hispidulin and arbutin. Furthermore, luteolin 7-sulfate showed lower cytotoxicity than luteolin in both B16/F10 cells and HEM. Luteolin 7-sulfate attenuated cellular melanin synthesis more effectively in B16/F10 cells and HEM stimulated by α-melanocyte-stimulating hormone and l-tyrosine than arbutin.
This study demonstrates that luteolin 7-sulfate isolated from P. iwatensis is a human TYR inhibitor with advantageous antimelanogenic properties, and would be useful for development as a therapeutic agent for the control of unwanted skin pigmentation.
黑色素的异常沉积可能导致美容方面的皮肤问题，因此，控制过量黑色素的合成是化妆品研究的主要目标。
从海洋植物中鉴定新型的酪氨酸酶（TYR）抑制剂，并研究其细胞抗黑色素生成作用。
对 50 种韩国特有海洋植物提取物进行筛选，以检测其对人 TYR 的抑制活性。然后从显示出潜力的选定植物提取物中分离活性成分，并阐明其化学结构。此外，使用鼠黑素瘤 B16/F10 细胞和人表皮黑素细胞（HEM）检测其抗黑色素生成作用。
在所测试的提取物中，岩藻 Phyllospadix iwatensis Makino 的提取物对人 TYR 具有最强的抑制活性。从 P. iwatensis 提取物的正丁醇部分中纯化出活性成分，并鉴定为毛蕊花糖苷 7-硫酸盐和木樨草素 7-硫酸盐。木樨草素 7-硫酸盐比毛蕊花糖苷 7-硫酸盐、木樨草素、毛蕊花糖苷和熊果苷对人 TYR 的抑制作用更强。此外，木樨草素 7-硫酸盐在 B16/F10 细胞和 HEM 中的细胞毒性均低于木樨草素。与熊果苷相比，木樨草素 7-硫酸盐在 α-促黑素细胞激素和 l-酪氨酸刺激的 B16/F10 细胞和 HEM 中更有效地减弱细胞黑色素合成。
本研究表明，从 Phyllospadix iwatensis 中分离出的木樨草素 7-硫酸盐是一种具有优势抗黑色素生成特性的人 TYR 抑制剂，可作为控制非期望性皮肤色素沉着的治疗剂。
