Inhibitory effects of brown algal phlorotannins on secretory phospholipase A2s, lipoxygenases and cyclooxygenases
Inhibitory effects of brown algal phlorotannins on secretory phospholipase A2s, lipoxygenases and cyclooxygenases
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DOI：
10.1023/a:1022972221002
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发表时间：
2003-01-01
影响因子：
3.3
通讯作者：
Nakamura, T
中科院分区：
文献类型：
--
作者：
Shibata, T;Nagayama, K;Nakamura, T
采用体外实验方法研究褐藻根皮单宁对分泌型磷脂酶A（2）s（sPLA（2）s）、脂氧合酶（LOX s）和环氧合酶（COX s）的抑制作用。间苯三酚的低聚物;从棕色双环拟青霉中分离的ECKOL（三聚体）、间苯二甲酸呋喃酮ECKOL A（五聚体）、DIECKOL（六聚体）和8，8 '-BIECKOL（六聚体）对来自猪胰和蜂毒的sPLA（2）具有显著的抑制作用（IC 50 100-200 μ M）。的根皮单宁抑制LOX活性更有效地比著名的LOX抑制剂，白藜芦醇和表没食子儿茶素没食子酸酯。本研究中最强的LOX抑制剂8，8 '-Bieckol抑制大豆LOX和5-LOX，IC 50值分别为38和24 μ M。除了100 μ M时dieckol对考克斯-1（74.7%）和eckol对考克斯-2（43.2%）的抑制作用外，发现根皮单宁对考克斯-1和考克斯-2的影响可以忽略不计或非常弱。
The inhibitory effects of brown algal phlorotannins on secretory phospholipase A(2)s (sPLA(2)s), lipoxygenases (LOXs) and cyclooxygenases (COXs) were determined with an in vitro assay. Oligomers of phloroglucinol; eckol (a trimer), phlorofucofuroeckol A (a pentamer), dieckol (a hexamer) and 8,8'-bieckol (a hexamer) isolated from the brown alga Eisenia bicyclis had pronounced inhibitory effects on sPLA(2) from porcine pancreas and bee venom (IC50 100-200 muM). The phlorotannins inhibited LOX activity more effectively than the well-known LOX inhibitors; resveratrol and epigallocatechin gallate. 8,8'-Bieckol, the strongest LOX inhibitor in this study, inhibited soybean LOX and 5-LOX with IC50 values of 38 and 24 muM, respectively. Negligible or very weak effects of the phlorotannins on COX-1 and COX-2 were found, except for an inhibitory effect of dieckol on COX-1 (74.7%) and of eckol on COX-2 (43.2%) at 100 muM.