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天然二芳基庚烷类化合物对完整人中性粒细胞中5-羟基二十碳四烯酸（5-HETE）生成的抑制作用：姜黄素类和氧化姜黄酮类的抑制活性

Inhibition of 5-hydroxy-eicosatetraenoic acid (5-HETE) formation in intact human neutrophils by naturally-occurring diarylheptanoids: inhibitory activities of curcuminoids and yakuchinones.

作者信息

Flynn D L, Rafferty M F, Boctor A M

出版信息

Prostaglandins Leukot Med. 1986 Jun;22(3):357-60. doi: 10.1016/0262-1746(86)90146-0.

DOI:10.1016/0262-1746(86)90146-0
PMID:3460103
Abstract

Various diarylheptanoids including curcumin, bis (3,4-dihydroxy-cinnamoyl) methane, and yakuchinones A & B were screened and found to be potent inhibitors of 5-HETE production by intact human neutrophils, with respective IC50 values of 8.0, 4.4, 5.4, and 4.0 microM. These diarylheptanoids were found to be more potent than BW-755C, Phenidone, and AA-861. We have confirmed a previous report that several of these diarylheptanoids inhibit cyclooxygenase. Thus, curcuminoids and yakuchinones are more accurately characterized as dual inhibitors of arachidonic acid metabolism.

摘要

对包括姜黄素、双（3,4-二羟基肉桂酰）甲烷以及氧化白当归素A和B在内的多种二芳基庚烷类化合物进行了筛选，发现它们是完整人中性粒细胞产生5-羟二十碳四烯酸（5-HETE）的有效抑制剂，其半数抑制浓度（IC50）值分别为8.0、4.4、5.4和4.0微摩尔。发现这些二芳基庚烷类化合物比BW-755C、非那吡啶和AA-861更有效。我们证实了之前的一份报告，即这些二芳基庚烷类化合物中的几种会抑制环氧化酶。因此，姜黄素类化合物和氧化白当归素更准确地被描述为花生四烯酸代谢的双重抑制剂。

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