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Inhibitory effects of brown algal phlorotannins on secretory phospholipase A2s, lipoxygenases and cyclooxygenases
Authors:Toshiyuki Shibata  Kohki Nagayama  Ryusuke Tanaka  Kuniko Yamaguchi  Takashi Nakamura
Affiliation:(1) Laboratory of Marine Resource Chemistry, Department of Bioscience and Biotechnology, Graduate School of Agriculture, Kyushu University, 6-10-1 Hakozaki, Higashi-ku, Fukuoka, 812-8581, Japan;(2) Department of Food Science, National University of Fisheries, Yoshimi, Shimonoseki, 759-65, Japan
Abstract:The inhibitory effects of brown algal phlorotannins on secretory phospholipase A2s (sPLA2s), 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 8,8prime-bieckol (a hexamer) isolated from the brown alga Eisenia bicyclis had pronounced inhibitory effects on sPLA2 from porcine pancreas and bee venom (IC50 100–200 mgrM). The phlorotannins inhibited LOX activity more effectively than the well-known LOX inhibitors; resveratrol and epigallocatechin gallate. 8,8prime-Bieckol, the strongest LOX inhibitor in this study, inhibited soybean LOX and 5-LOX with IC50 values of 38 and 24 mgrM, 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 mgrM.
Keywords:Brown alga  Cyclooxygenase  Eisenia bicyclis  Enzyme inhibition  HPLC  Lipoxygenase  Phlorotannin  Polyphenol  Secretory phospholipase A2
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