Iijima Chie, Wong Chin Piow, Nugroho Alfarius Eko, Sotozono Yayoi, Someya Saki, Hirasawa Yusuke, Kaneda Toshio, Hadi A Hamid A, Morita Hiroshi
Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41 Shinagawa-ku, Tokyo, 142-8501, Japan.
Department of Chemistry, Faculty of Science, University Malaya, 50603, Kuala Lumpur, Malaysia.
J Nat Med. 2016 Oct;70(4):702-7. doi: 10.1007/s11418-016-1016-y. Epub 2016 Jun 29.
The ceramicines, a series of limonoids from Chisocheton ceramicus (Meliaceae), were evaluated for anti-melanin deposition activity on α-melanocyte stimulating hormone (α-MSH) and 3-isobutyl-1-methylxanthine (IBMX)-treated B16-F10 melanoma cell, and several ceramicines were found to be active. The structure-activity relationship of ceramicines as anti-melanin deposition inhibitors was deduced. Furthermore, the mechanism of anti-melanin deposition activity of ceramicine B, a major constituent of C. ceramicus that showed potent anti-melanin deposition activity, was investigated. Tyrosinase enzymatic activity and tyrosinase mRNA expression were not affected by ceramicine B. The anti-melanin deposition activity of ceramicine B was shown to be related to the downregulation of tyrosinase protein expression. These results suggest that ceramicines have potential to be used as depigmentation agents.
对从红果樫木（楝科）中提取的一系列柠檬苦素类化合物——ceramicines，进行了针对α-黑素细胞刺激激素（α-MSH）和3-异丁基-1-甲基黄嘌呤（IBMX）处理的B16-F10黑色素瘤细胞的抗黑色素沉着活性评估，发现几种ceramicines具有活性。推导了ceramicines作为抗黑色素沉着抑制剂的构效关系。此外，还研究了红果樫木的主要成分ceramicine B具有强效抗黑色素沉着活性的抗黑色素沉着活性机制。酪氨酸酶的酶活性和酪氨酸酶mRNA表达不受ceramicine B的影响。ceramicine B的抗黑色素沉着活性被证明与酪氨酸酶蛋白表达的下调有关。这些结果表明，ceramicines有潜力用作色素沉着抑制剂。
