Department of Food Science and Technology, Pukyong National University, Busan 608-737, Korea.
Phytother Res. 2013 Jan;27(1):148-51. doi: 10.1002/ptr.4694. Epub 2012 Apr 4.
Pancreatic lipase is a potential therapeutic target for the treatment of diet-induced obesity in humans. In an ongoing search for new pancreatic lipase inhibitors from natural sources, a methanolic extract of marine brown algae, Eisenia bicyclis, showed a significant inhibitory effect against pancreatic lipase. Bioassay-guided isolation of this methanolic extract using a pancreatic lipase inhibitory assay led to the isolation and identification of six known phlorotannins: eckol (1), fucofuroeckol A (2), 7-phloroeckol (3), dioxindehydroeckol (4), phlorofucofuroeckol A (5), and dieckol (6). The structures were established on the basis of nuclear magnetic resonance and mass spectrometry spectroscopic data interpretation. Among the isolated phloroglucinol polymers, compounds 2 and 3 showed potent inhibitory effects on pancreatic lipase with IC₅₀ values ranging from 37.2 ± 2.3 to 12.7 ± 1.0 μM, respectively.
胰脂肪酶是治疗人类饮食诱导性肥胖的潜在治疗靶点。在不断从天然来源寻找新的胰脂肪酶抑制剂的过程中，海洋褐藻(Eisenia bicyclis)的甲醇提取物对胰脂肪酶表现出显著的抑制作用。使用胰脂肪酶抑制测定法对这种甲醇提取物进行生物测定指导分离，导致分离和鉴定出六种已知的岩藻多酚：艾杜醇(1)、岩藻呋喃基 fucofuroeckol A(2)、7-岩藻基-艾杜醇(3)、二氧代去氢艾杜醇(4)、岩藻基 fucofuroeckol A(5)和 dieckol(6)。根据核磁共振和质谱光谱数据解释确定了这些结构。在分离出的间苯三酚聚合物中，化合物 2 和 3 对胰脂肪酶表现出很强的抑制作用，IC₅₀ 值分别为 37.2 ± 2.3 和 12.7 ± 1.0 μM。
