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桐花树提取物可抑制大鼠爪部炎症的初期和后期阶段,并减弱大鼠中性粒细胞和人血小板中类花生酸的生成。

Aegiceras corniculatum extract suppresses initial and late phases of inflammation in rat paw and attenuates the production of eicosanoids in rat neutrophils and human platelets.

作者信息

Roome Talat, Dar Ahsana, Naqvi Sabira, Ali Shamsher, Choudhary Muhammad Iqbal

机构信息

International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

出版信息

J Ethnopharmacol. 2008 Nov 20;120(2):248-54. doi: 10.1016/j.jep.2008.08.025. Epub 2008 Sep 2.

Abstract

AIM OF THE STUDY

The present study is designed to explore the anti-inflammatory potential of Aegiceras corniculatum Linn. Blanco stems extracts and their mechanism of action against various pro-inflammatory mediators and to validate its traditional use against inflammatory diseases.

MATERIALS AND METHODS

Rat paw edema and peritonitis models were employed for in vivo studies. For in vitro studies human platelets and rat neutrophils were stimulated with Ca(2+)-ionophore A23187 leading to the production of various pro-inflammatory metabolites, i.e., 12-HTT, 12-HETE and LTB(4) and 5-HETE which were quantified by HPLC.

RESULTS

The highly polar methanol extract (100mg/kg) caused approximately 90% reduction in the carrageenan- and prostaglandin E2-induced paw edema in rats. It also caused the inhibition of cycloxygenase-1 metabolite, 12-HHT (IC(50) 41.1+/-1.5microg/ml) with a concomitant rise in 12-lipoxygenase metabolite, 12-HETE in A23187 stimulated human platelets. Conversely, the non-polar hexane extract attenuated (IC(50) 0.36+/-0.12microg/ml) 12-HETE formation with a parallel rise in 12-HHT, thereby displaying a selectivity towards 12-lipoxygenase. Non-polar hexane extract also antagonized the production of 5-lipoxygenase metabolites, i.e., leukotriene B(4) and 5-HETE in the rat neutrophils. Furthermore, ethyl acetate extract inhibited both COX and 5-LOX with a marked decline in the production of 12-HHT (IC(50) 0.08+/-0.002microg/ml) and LTB(4) (IC(50) 0.86+/-0.03microg/ml), respectively. The anti-inflammatory effect of hexane and ethyl acetate extracts was also reflected by the diminution of carrageenan-induced cell infiltration in rat peritoneum. Additionally, plant extracts caused approximately 60% suppression in dextran-induced paw edema implying that they also ameliorate histamine and serotonin release.

CONCLUSION

Hexane, ethyl acetate and methanol extracts derived from Aegiceras corniculatum possess significant anti-inflammatory activity via multiple mechanisms and validate their traditional use against inflammation-related diseases.

摘要

研究目的

本研究旨在探究桐花树(Aegiceras corniculatum Linn. Blanco)茎提取物的抗炎潜力及其对多种促炎介质的作用机制,并验证其在治疗炎症性疾病方面的传统用途。

材料与方法

采用大鼠足爪水肿和腹膜炎模型进行体内研究。体外研究中,用钙离子载体A23187刺激人血小板和大鼠中性粒细胞,导致产生多种促炎代谢产物,即12-羟基二十碳四烯酸(12-HTT)、12-羟基二十碳五烯酸(12-HETE)、白三烯B4(LTB4)和5-羟基二十碳四烯酸(5-HETE),通过高效液相色谱法对其进行定量分析。

结果

高极性甲醇提取物(100mg/kg)可使角叉菜胶和前列腺素E2诱导的大鼠足爪水肿减轻约90%。它还能抑制环氧合酶-1代谢产物12-HHT(半数抑制浓度(IC50)为41.1±1.5μg/ml),同时使A23187刺激的人血小板中12-脂氧合酶代谢产物12-HETE升高。相反,非极性己烷提取物可减弱12-HETE的生成(IC50为0.36±0.12μg/ml),同时使12-HHT平行升高,从而显示出对12-脂氧合酶的选择性。非极性己烷提取物还可拮抗大鼠中性粒细胞中5-脂氧合酶代谢产物白三烯B4和5-HETE的产生。此外,乙酸乙酯提取物可同时抑制环氧合酶(COX)和5-脂氧合酶(5-LOX),使12-HHT(IC50为0.08±0.002μg/ml)和白三烯B4(IC50为0.86±0.03μg/ml)的生成显著下降。己烷和乙酸乙酯提取物的抗炎作用还体现在角叉菜胶诱导的大鼠腹膜细胞浸润减少。此外,植物提取物可使右旋糖酐诱导的足爪水肿减轻约60%,这表明它们还能改善组胺和5-羟色胺的释放。

结论

桐花树的己烷、乙酸乙酯和甲醇提取物通过多种机制具有显著的抗炎活性,证实了其在治疗炎症相关疾病方面的传统用途。

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