New insights into the mechanism of action of the anti-inflammatory triterpene lupeol
New insights into the mechanism of action of the anti-inflammatory triterpene lupeol
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DOI：
10.1211/0022357011777909
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发表时间：
2001-11-01
影响因子：
3.3
通讯作者：
Villar, A
中科院分区：
文献类型：
--
作者：
Fernández, MA;de las Heras, B;Villar, A
体外研究了五环三萜芦皮醇对小鼠炎症模型和腹腔巨噬细胞功能的抑制作用。Lupeol（0.5和1mg /耳）对TPA诱导的小鼠耳部水肿有抑制作用，对花生四烯酸诱导的小鼠耳部水肿效果较差。中性粒细胞特异性标记物髓过氧化物酶的定量表明，其局部活性与炎症组织中细胞浸润的减少有关。在体外测试中，芦皮酮显著降低了a23187刺激的巨噬细胞产生的前列腺素E-2 (PGE(2))，但未能影响白三烯C-4的释放。它是亚硝酸盐释放的弱抑制剂，但剂量依赖性地抑制PGE(2)。脂多糖处理的巨噬细胞细胞因子（肿瘤坏死因子α和白细胞介素-1 β）的产生在10-100 μ m范围内被抑制。本研究表明，芦皮醇具有抗炎活性，这可能取决于其阻止某些介质产生的能力。
The pentacyclic triterpene lupeol has been studied for its inhibitory effects on murine models of inflammation and peritoneal macrophage functions in-vitro. Lupeol (0.5 and 1 mg/ear) administered topically suppressed the mouse ear oedema induced by 12-O-tetradecanoylphorbol acetate (TPA), being less effective on ear oedema induced by arachidonic acid. Quantitation of the neutrophil specific marker myeloperoxidase demonstrated that its topical activity was associated with reduction in cell infiltration into inflamed tissues. When tested invitro, lupeol significantly reduced prostaglandin E-2 (PGE(2)) production from A23187-stimulated macrophages, but failed to affect leukotriene C-4 release. It was a weak inhibitor of nitrite release, but dose-dependently suppressed PGE(2). Cytokine production (tumour necrosis factor alpha and interleukin-1 beta was inhibited in the range 10-100 mum in lipopolysaccharide-treated macrophages. This study demonstrated that lupeol possessed anti-inflammatory activity which was likely to depend on its ability to prevent the production of some mediators.