Li Yong, Lee Sang-Hoon, Le Quang-To, Kim Moon-Moo, Kim Se-Kwon
Marine Bioprocess Research Center, Pukyong National University, Busan 608-737, Republic of Korea.
J Agric Food Chem. 2008 Dec 24;56(24):12073-80. doi: 10.1021/jf802732n.
Two bioactive phloroglucinol derivatives, fucodiphloroethol G (1) and phlorofucofuroeckol A (3) were first isolated from Eckolonia cava (EC) and characterized by nuclear magnetic resonance (NMR) spectroscopic methods, along with eckol (2). In this study, anti-allergic activities of phloroglucinol derivatives were assessed on human basophilic leukemia (KU812) and rat basophilic leukemia (RBL-2H3) cell lines using a histamine release assay. Both compounds 1 and 3 exhibited a significant inhibitory activity against histamine release. Meanwhile, the potential inhibitory mechanism was also suggested as the suppression of binding activity between IgE and Fc epsilonRI by the cytometric analysis. These results suggested that compounds 1 and 3 could be the key effectors in the crude methanol extract of EC against allergy disease and used as novel candidates for development in the cosmetic and drug industries potentially.
首次从海蕴（EC）中分离出两种具有生物活性的间苯三酚衍生物，岩藻双氯乙醇G（1）和间苯三酚岩藻呋喃醇A（3），并通过核磁共振（NMR）光谱法对其进行了表征，同时还鉴定出了eckol（2）。在本研究中，采用组胺释放试验评估了间苯三酚衍生物对人嗜碱性白血病（KU812）和大鼠嗜碱性白血病（RBL-2H3）细胞系的抗过敏活性。化合物1和3均表现出对组胺释放的显著抑制活性。同时，通过细胞分析还提示了潜在的抑制机制为抑制IgE与FcεRI之间的结合活性。这些结果表明，化合物1和3可能是海蕴粗甲醇提取物中抗过敏性疾病的关键效应物，有望作为化妆品和制药行业开发的新候选物。
