Dept. of Pharmacy, University of Iceland, 101 Reykjavik, Iceland.
Phytomedicine. 1994 Dec;1(3):187-91. doi: 10.1016/S0944-7113(11)80063-2.
The aliphatic α-methylene-γ-lactone (+)-protolichesterinic acid (1), isolated from Cetraria islandica, has been shown to exhibit inhibitory effects on the enzyme 5-lipoxygenase in an in vitro assay in which porcine leucocytes are used as a source of the enzyme system. The isomeric compounds (+)-lichesterinic acid (2) and (-)-lichesterinic acid (4), prepared from (+)-protolichesterinic- and (-)-allo-protolichesterinic acids, respectively, exhibited anti-5-lipoxygenase activity of the same order of magnitude. (+)-Methyl lichesterinate (3) was, however, inactive. It was shown that despite its lipophilic nature, protolichesterinic acid is extractable into an aqueous medium, the concentration being dependent on the length of extraction.
从冰岛衣属植物（Cetraria islandica）中分离得到的脂肪族 α-亚甲基-γ-内酯（+）-原贝壳杉烯酸（1），在以猪白细胞作为酶源的体外试验中，表现出对 5-脂氧合酶的抑制作用。从（+）-原贝壳杉烯酸和（-）-allo-原贝壳杉烯酸分别制备得到的立体异构体化合物（+）-贝壳杉烯酸（2）和（-）-贝壳杉烯酸（4），也表现出相同数量级的抗 5-脂氧合酶活性。（+）-甲基贝壳杉酯（3）则没有活性。研究表明，尽管原贝壳杉烯酸具有亲脂性，但仍可萃取到水介质中，其浓度取决于萃取时间的长短。
