Lee Se-Eun, Kim Min-Ju, Hillman Prima F, Oh Dong-Chan, Fenical William, Nam Sang-Jip, Lim Kyung-Min
The Graduate School of Industrial Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea.
Department of Chemistry and Nanoscience, Ewha Womans University, Seoul 03760, Korea.
Mar Drugs. 2022 Feb 21;20(2):155. doi: 10.3390/md20020155.
The tricyclic quinazoline alkaloid deoxyvasicinone (, ) was isolated from a marine-derived sp. CNQ-617, and its anti-melanogenic effects were investigated. Deoxyvasicinone was shown to decrease the melanin content of B16F10 and MNT-1 cells that have been stimulated by α-melanocyte-stimulating hormone (α-MSH). In addition, microscopic images of the cells showed that deoxyvasicinone attenuated melanocyte activation. Although, deoxyvasicinone did not directly inhibit tyrosinase (TYR) enzymatic activity, real-time PCR showed that it inhibited the mRNA expression of TYR, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2). In the artificial 3D pigmented skin model Melanoderm, deoxyvasicinone brightened the skin significantly, as confirmed by histological examination. In conclusion, this study demonstrated that the marine microbial natural product deoxyvascinone has an anti-melanogenic effect through downregulation of melanogenic enzymes.
从海洋来源的 种 CNQ - 617 中分离出三环喹唑啉生物碱脱氧瓦西酮( , ),并对其抗黑色素生成作用进行了研究。结果表明,脱氧瓦西酮可降低经α - 黑素细胞刺激激素(α - MSH)刺激的 B16F10 和 MNT - 1 细胞中的黑色素含量。此外,细胞显微镜图像显示脱氧瓦西酮可减弱黑素细胞的活化。虽然脱氧瓦西酮并未直接抑制酪氨酸酶(TYR)的酶活性,但实时定量聚合酶链反应显示它可抑制 TYR、酪氨酸酶相关蛋白 1(TRP - 1)和酪氨酸酶相关蛋白 2(TRP - 2)的 mRNA 表达。在人工三维色素沉着皮肤模型 Melanoderm 中,组织学检查证实脱氧瓦西酮可显著提亮皮肤。总之,本研究表明海洋微生物天然产物脱氧瓦西酮通过下调黑色素生成酶具有抗黑色素生成作用。