Koshihara Y, Neichi T, Murota S, Lao A, Fujimoto Y, Tatsuno T
FEBS Lett. 1983 Jul 11;158(1):41-4. doi: 10.1016/0014-5793(83)80672-3.
Three of four natural compounds, which are caffeic acid, eupatilin and 4'-demethyleupatilin, isolated from Chinese plant, Artemisia rubripes Nakai selectively inhibited 5-lipoxygenase of cultured mastocytoma cells. Half-inhibition doses (ID50) for caffeic acid, eupatilin and 4'-demethyleupatilin were 3.7, 14 and 18 X 10(-6) M, respectively. The inhibition by caffeic acid was non-competitive types. Prostaglandin synthase activities were little inhibited by eupatilin and 4'-demethyleupatilin, but rather stimulated by caffeic acid. The formation of leukotriene C4 and D4 by mast tumor cells was almost completely suppressed by these compounds at 10(-4) M.
从中国植物红足蒿(Artemisia rubripes Nakai)中分离出的四种天然化合物中的三种,即咖啡酸、紫花牡荆素和4'-去甲基紫花牡荆素,可选择性抑制培养的肥大细胞瘤细胞的5-脂氧合酶。咖啡酸、紫花牡荆素和4'-去甲基紫花牡荆素的半数抑制剂量(ID50)分别为3.7、14和18×10⁻⁶ M。咖啡酸的抑制作用为非竞争性类型。紫花牡荆素和4'-去甲基紫花牡荆素对前列腺素合酶活性的抑制作用较小,但咖啡酸反而会刺激其活性。在10⁻⁴ M浓度下,这些化合物几乎完全抑制了肥大细胞瘤细胞白三烯C4和D4的形成。