Safayhi H, Mack T, Sabieraj J, Anazodo M I, Subramanian L R, Ammon H P
Department of Pharmacology, University of Tuebingen, FRG.
J Pharmacol Exp Ther. 1992 Jun;261(3):1143-6.
Isomers (alpha- and beta-) of boswellic acids (BAs), 11-keto-beta-BA and their acetyl derivatives were isolated from the gum resin of Boswellia serrata. BA and derivatives concentration dependently decreased the formation of leukotriene B4 from endogenous arachidonic acid in rat peritoneal neutrophils. Among the BAs, acetyl-11-keto-beta-BA induced the most pronounced inhibition of 5-lipoxygenase (5-LO) product formation with an IC50 of 1.5 microM. In contrast to the redox type 5-LO inhibitor nordihydroguaiaretic acid, BA in concentrations up to 400 microM did not impair the cyclooxygenase and 12-lipoxygenase in isolated human platelets and the peroxidation of arachidonic acid by Fe-ascorbate. The data strongly suggest that BAs are specific, nonreducing-type inhibitors of the 5-LO product formation either interacting directly with the 5-LO or blocking its translocation.
从锯叶乳香的树胶树脂中分离出了乳香酸（BAs）的异构体（α-和β-）、11-酮-β-乳香酸及其乙酰化衍生物。BA及其衍生物能浓度依赖性地减少大鼠腹腔中性粒细胞内源性花生四烯酸生成白三烯B4。在这些BAs中，乙酰-11-酮-β-乳香酸对5-脂氧合酶（5-LO）产物生成的抑制作用最为显著，IC50为1.5微摩尔。与氧化还原型5-LO抑制剂去甲二氢愈创木酸不同，浓度高达400微摩尔的BA不会损害分离的人血小板中的环氧化酶和12-脂氧合酶，也不会影响抗坏血酸铁对花生四烯酸的过氧化作用。数据有力地表明，BAs是5-LO产物生成的特异性非还原型抑制剂，要么直接与5-LO相互作用，要么阻断其转位。
