Benrezzouk R, Terencio M C, Ferrándiz M L, San Feliciano A, Gordaliza M, Miguel del Corral J M, de la Puente M L, Alcaraz M J
Department of Pharmacology, University of Valencia, Spain.
Life Sci. 1999;64(19):PL205-11. doi: 10.1016/s0024-3205(99)00119-8.
The inhibitory effect of two neo-clerodane diterpenoids, E-isolinaridial (EI) and its methylketone derivative (EIM), isolated from Linaria saxatilis var. glutinosa, on PLA2 and other enzyme activities involved in the inflammatory process was studied. Both compounds inhibited human synovial sPLA2 in a concentration-dependent manner with IC50 values of 0.20 and 0.49 microM, respectively, similar to scalaradial. Besides, these compounds decreased the cell-free 5-lipoxygenase activity and A23187-induced neutrophil LTB4 biosynthesis. Another function of human neutrophils, such as receptor-mediated degranulation, was also significantly reduced. In contrast, none of the compounds affected superoxide generation in leukocytes, or cyclooxygenase-1, cyclooxygenase-2 and inducible nitric oxide synthase activities in cell-free assays.
研究了从粘毛柳穿鱼（Linaria saxatilis var. glutinosa）中分离得到的两种新克罗烷二萜类化合物，即E-异薰衣草醛（EI）及其甲基酮衍生物（EIM），对参与炎症过程的磷脂酶A2（PLA2）和其他酶活性的抑制作用。这两种化合物均以浓度依赖的方式抑制人滑膜分泌型PLA2（sPLA2），IC50值分别为0.20和0.49微摩尔，与刺芒柄花素相似。此外，这些化合物降低了无细胞体系中5-脂氧合酶的活性以及A23187诱导的中性粒细胞白三烯B4（LTB4）的生物合成。人中性粒细胞的另一项功能，如受体介导的脱颗粒作用，也显著降低。相比之下，这些化合物在无细胞实验中均不影响白细胞中超氧化物的产生，也不影响环氧合酶-1（COX-1）、环氧合酶-2（COX-2）和诱导型一氧化氮合酶（iNOS）的活性。
