Anti-inflammatory activity of abietic acid, a diterpene isolated from Pimenta racemosa var. grissea
Anti-inflammatory activity of abietic acid, a diterpene isolated from Pimenta racemosa var. grissea
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DOI：
10.1211/0022357011776027
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发表时间：
2001-06-01
影响因子：
3.3
通讯作者：
Sáenz, MT
中科院分区：
文献类型：
--
作者：
Fernández, MA;Tornos, MP;Sáenz, MT
松香酸（一种从 Pimenta racemosa var. var. 中分离出来的二萜）的抗炎活性。 grissea（桃金娘科），进行了体内和体外评估。口服或局部给药后，该化合物以时间和剂量依赖性方式显着抑制角叉菜胶诱导的大鼠爪水肿，以及12-O-十四烷酰佛波醇乙酸酯诱导的小鼠耳水肿。髓过氧化物酶的抑制表明其局部活性受到中性粒细胞浸润到发炎组织（耳朵）的影响。此外，还对松香酸对某些巨噬细胞功能的影响进行了体外分析。无毒浓度的松香酸可抑制脂多糖处理的巨噬细胞中前列腺素 E-2 (PGE(2)) 的产生，而亚硝酸盐、肿瘤坏死因子 α 和白细胞介素 1 β 的产生仅受此二萜的微弱影响。 A23187 刺激的巨噬细胞产生的 PGE(2) 仅在高剂量 (100 muM) 时受到抑制，并且无法改变白三烯 C-4 的产生。这些结果表明，松香酸在口服或局部给药后发挥体内抗炎活性，并且具有部分阻止某些炎症介质产生的能力。
The anti-inflammatory activity of abietic acid, a diterpene isolated from Pimenta racemosa var. grissea (Myrtaceae), was evaluated in-vivo and in-vitro. This compound significantly inhibited rat paw oedema induced by carrageenan in a time- and dose-dependent manner, and mouse ear oedema induced by 12-O-tetradecanoylphorbol acetate, after oral or topical administration. The inhibition of myeloperoxidase enzyme showed that its topical activity was influenced by neutrophil infiltration into the inflamed tissues (ears). In addition, the effect of abietic acid on some macrophage functions was analysed in-vitro. Non-toxic concentrations of abietic acid inhibited prostaglandin E-2 (PGE(2)) production in lipopolysaccharide-treated macrophages, whereas nitrite, tumour necrosis factor alpha and interleukin-1 beta production were only weakly affected by this diterpene. PGE(2) production from A23187-stimulated macrophages was only inhibited at high doses (100 muM) and it failed to modify leukotriene C-4 production. These results indicate that abietic acid exerts in-vivo anti-inflammatory activity after oral or topical administration and has partial ability to prevent the production of some inflammatory mediators.