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金合欢荚果多糖组分:潜在的抗炎用途。

Polysaccharide fractions of Caesalpinia ferrea pods: potential anti-inflammatory usage.

机构信息

Instituto Superior de Ciências Biomédicas, Universidade Estadual do Ceará, Fortaleza, CE, Brazil.

出版信息

J Ethnopharmacol. 2012 Jan 31;139(2):642-8. doi: 10.1016/j.jep.2011.12.012. Epub 2011 Dec 13.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Caesalpinia ferrea (Caesalpinioideae), known as pau-ferro or juca, has been used in the traditional medicine in North and Northeast of Brazil in inflammatory disorder, among others. Thus, experimental evaluation of the anti-inflammatory activity of extracts and fraction polysaccharides of Caesalpinia ferrea pods, and correlation with its anti-inflammatory activity and popular use is important.

MATERIALS AND METHODS

Total polysaccharides (TPL) were applied to ion exchange chromatography and eluted stepwise. Paw edema was induced s.c. by λ-carrageenan, dextran, histamine, serotonin, compound 48/80, bradykinin, prostaglandin E(2) (PGE(2)) or L-arginine and analyzed by plethysmometry and protein leakage by spectrophotometry. Peritonitis was induced i.p. by carrageenan or N-formyl-methionyl-leucyl-phenylalanine (fMLP) and analyzed 4 h later for leukocyte migration and protein leakage. Animals were treated i.v. with TPL or polysaccharide fractions (0.01, 0.1, 1 mg/kg) 30 min before stimuli in both models. Toxicity (variation of body/organ mass and hematological/biochemical parameters) was evaluated after the seven-day treatment with the most active polysaccharide fraction (1 mg/kg; i.v.).

RESULTS

Chromatography of TPL (2.8% yield) provided three major polysaccharide fractions (FI, FII, FIII). At 1 mg/kg, TPL inhibited the paw edema induced by carrageenan (60%) and FIII (fraction presenting high carbohydrate and low protein content) inhibited the inflammatory parameters in the paw edema induced by the following stimuli: carrageenan (70%), dextran (53%), histamine (65%), serotonin (62%), bradykinin (60%), PGE(2) (63%), nitric oxide (61%) and compound 48/80 (36%). Additionally, FIII at 1 mg/kg inhibited the carrageenan-induced edema in animals with intact mast cells, but only the late phase of those with degranulated mast cells elicited by compound 48/80. Moreover, FIII inhibited cell migration and protein leakage in the model of peritonitis elicited by carrageenan (88%) and fMLP (64%), being well tolerated by animals.

CONCLUSIONS

Extracts and polysaccharide fractions of Caesalpinia ferrea pods exhibit potent anti-inflammatory activity via negative modulation of histamine, serotonin, bradykinin, PGE(2) and NO released in the carrageenan-induced edema, showing involvement of mast cells. FIII could be interfering not only in the vascular, but also in cellular inflammatory events, revealing to be an important active component of traditionally prepared remedies used to treat inflammatory states.

摘要

民族药理学相关性

铁线莲(云实科),俗称 pau-ferro 或 juca,在巴西北部和东北部的传统医学中被用于治疗炎症等疾病。因此,评估铁线莲豆荚的提取物和多糖部分的抗炎活性及其与抗炎活性和民间用途的相关性非常重要。

材料和方法

总多糖(TPL)应用于离子交换层析并逐步洗脱。爪肿胀通过 λ-角叉菜胶、葡聚糖、组胺、血清素、化合物 48/80、缓激肽、前列腺素 E2 (PGE2) 或 L-精氨酸皮下诱导,通过体积描记法分析,并通过分光光度法分析蛋白质渗漏。腹膜炎通过腹腔内注射角叉菜胶或 N-甲酰基-甲硫氨酸-亮氨酸-苯丙氨酸(fMLP)诱导,并在 4 小时后分析白细胞迁移和蛋白质渗漏。在两种模型中,动物在刺激前 30 分钟静脉内给予 TPL 或多糖部分(0.01、0.1、1mg/kg)进行治疗。在七天的治疗后,用最有效的多糖部分(1mg/kg;静脉内)评估毒性(体重/器官质量和血液学/生化参数的变化)。

结果

TPL(2.8%产率)的色谱分析提供了三种主要的多糖部分(FI、FII、FIII)。TPL (1mg/kg)抑制角叉菜胶诱导的爪肿胀(60%),FIII(具有高碳水化合物和低蛋白质含量的部分)抑制以下刺激物诱导的爪肿胀中的炎症参数:角叉菜胶(70%)、葡聚糖(53%)、组胺(65%)、血清素(62%)、缓激肽(60%)、PGE2(63%)、一氧化氮(61%)和化合物 48/80(36%)。此外,FIII(1mg/kg)抑制了完整肥大细胞诱导的角叉菜胶诱导的水肿,但仅抑制了化合物 48/80 诱导的脱颗粒肥大细胞的后期阶段。此外,FIII 抑制了由角叉菜胶(88%)和 fMLP(64%)诱导的腹膜炎模型中的细胞迁移和蛋白渗漏,对动物具有良好的耐受性。

结论

铁线莲豆荚的提取物和多糖部分通过负调节角叉菜胶诱导的水肿中释放的组胺、血清素、缓激肽、PGE2 和 NO,表现出有效的抗炎活性,表明涉及肥大细胞。FIII 不仅可能干扰血管炎症,还可能干扰细胞炎症事件,表明它是传统制备的用于治疗炎症状态的药物的重要活性成分。

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