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枇杷叶的抗炎和镇痛特性。

Anti-inflammatory and antinociceptive properties of the leaves of Eriobotrya japonica.

机构信息

College of Pharmacy, Woosuk University, Chonbuk 565-701, Republic of Korea.

出版信息

J Ethnopharmacol. 2011 Mar 24;134(2):305-12. doi: 10.1016/j.jep.2010.12.017. Epub 2010 Dec 21.

Abstract

AIM OF THE STUDY

The leaves of Eriobotrya japonica Lindl. have been widely used as a traditional medicine for the treatment of many diseases including coughs and asthma. The present study was designed to validate the anti-inflammatory and antinociceptive properties of the n-BuOH fraction of E. japonica (LEJ) leaves.

MATERIALS AND METHODS

The anti-inflammatory properties of LEJ were studied using IFN-γ/LPS activated murine peritoneal macrophage model. The antinociceptive effects of LEJ were assessed using experimental models of pain, including thermal nociception methods, such as the tail immersion test and the hotplate test, and chemical nociception induced by intraperitoneal acetic acid and subplantar formalin in mice. To examine the possible connection of the opioid receptor to the antinociceptive activity of LEJ, we performed a combination test with naloxone, a nonselective opioid receptor antagonist.

RESULTS

In the IFN-γ and LPS-activated murine peritoneal macrophage model, LEJ suppressed NO production and iNOS expression via down-regulation of NF-κB activation. It also attenuated the expression of COX-2 and the secretion of pro-inflammatory cytokines like TNF-α and IL-6. Moreover, LEJ also demonstrated strong and dose-dependent antinociceptive activity compared to tramadol and indomethacin in various experimental pain models. In a combination test using naloxone, diminished analgesic activities of LEJ were observed, indicating that the antinociceptive activity of LEJ is connected with the opioid receptor.

CONCLUSIONS

The results indicate that LEJ had potent inhibitory effects on the inflammatory mediators including nitric oxide, iNOS, COX-2, TNF-α and IL-6 via the attenuation of NF-κB translocation to the nucleus. LEJ also showed excellent antinociceptive activity in both central and peripheral mechanism as a weak opioid agonist. Based on these results, LEJ may possibly be used as an anti-inflammatory and an analgesic agent for the treatment of pains and inflammatory diseases.

摘要

目的

橘叶已被广泛用于治疗咳嗽和哮喘等多种疾病的传统药物。本研究旨在验证橘叶正丁醇(LEJ)提取物的抗炎和镇痛特性。

材料和方法

采用 IFN-γ/LPS 激活的小鼠腹腔巨噬细胞模型研究 LEJ 的抗炎特性。采用热痛觉法(如尾浸试验和热板试验)和腹腔注射醋酸和足底福尔马林诱导的化学性疼痛模型评估 LEJ 的镇痛作用。为了研究 LEJ 的镇痛活性与阿片受体的可能联系,我们用纳洛酮(一种非选择性阿片受体拮抗剂)进行了联合试验。

结果

在 IFN-γ 和 LPS 激活的小鼠腹腔巨噬细胞模型中,LEJ 通过抑制 NF-κB 激活来抑制 NO 产生和 iNOS 表达。它还能减弱 COX-2 的表达和促炎细胞因子如 TNF-α 和 IL-6 的分泌。此外,LEJ 在各种实验性疼痛模型中也表现出比曲马多和吲哚美辛更强和剂量依赖性的镇痛活性。在纳洛酮联合试验中,LEJ 的镇痛活性减弱,表明 LEJ 的镇痛活性与阿片受体有关。

结论

结果表明,LEJ 通过抑制 NF-κB 向核内易位,对包括一氧化氮、iNOS、COX-2、TNF-α 和 IL-6 在内的炎症介质具有强大的抑制作用。LEJ 作为一种弱阿片类激动剂,在外周和中枢机制中均表现出优异的镇痛活性。基于这些结果,LEJ 可能可用于治疗疼痛和炎症性疾病的抗炎和镇痛药物。

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