Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dúbravská 9, 841 04 Bratislava, Slovak Republic.
Pharmacol Rep. 2011;63(3):790-8. doi: 10.1016/s1734-1140(11)70591-6.
N-feruloylserotonin (N-f-5HT) isomers, isolated from seeds of Leuzea carthamoides (Wild) DC, inhibited dose-dependent oxidative burst in human whole blood and isolated neutrophils in vitro, which were measured by luminol- and/or isoluminol-enhanced chemiluminescence in the following rank order of stimuli: PMA > OpZ > calcium ionophore A23187. In isolated neutrophils that were stimulated with PMA, N-f-5HT isomers were effective against extracellular and intracellular reactive oxygen species. Liberation of ATP, analysis of apoptosis, and recombinant caspase-3 activity revealed that N-f-5HT isomers, used in concentrations up to 100 μM, did not alter the viability and integrity of isolated neutrophils. Western blot analysis documented that in concentrations of 10 and 100 μM, N-f-5HT isomers significantly decreased PMA-induced phosphorylation of PKC α/β II. The results suggest that N-f-5HT isomers are an effective, naturally occurring substance with a potent pharmacological effect on the oxidative burst of human neutrophils. It should be further investigated for its pharmacological activity against oxidative stress in ischemia-reperfusion, inflammation and other pathological conditions.
N-阿魏酰血清素（N-f-5HT）异构体，从藜芦属（DC 野生）种子中分离出来，抑制体外人全血和分离的中性粒细胞中剂量依赖性的氧化爆发，这是通过在以下刺激物的以下顺序测量的发光和/或异鲁米诺增强化学发光来测量的：PMA>OpZ>钙离子载体 A23187。在 PMA 刺激的分离中性粒细胞中，N-f-5HT 异构体对细胞外和细胞内活性氧物质有效。释放的 ATP、细胞凋亡分析和重组 caspase-3 活性表明，N-f-5HT 异构体在高达 100 μM 的浓度下不改变分离中性粒细胞的活力和完整性。Western blot 分析记录，在 10 和 100 μM 的浓度下，N-f-5HT 异构体显著降低了 PMA 诱导的 PKCα/β II 的磷酸化。结果表明，N-f-5HT 异构体是一种有效的、天然存在的物质，对人中性粒细胞的氧化爆发具有很强的药理学作用。应进一步研究其对缺血再灌注、炎症和其他病理状况下氧化应激的药理学活性。
