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评价拉弗恩西亚·帕卡里甲醇茎皮提取物(紫葳科)在实验动物中的抗溃疡活性及作用机制。

Evaluation of antiulcer activity and mechanism of action of methanol stem bark extract of Lafoensia pacari A. St.-Hil. (Lytraceae) in experimental animals.

机构信息

Department of Basic Sciences in Health, Faculty of Medicine, Federal University of Mato Grosso, Av. Fernando Correa da Costa, n. 2367, Cuiabá 78060-900, Mato Grosso, Brazil.

出版信息

J Ethnopharmacol. 2012 Dec 18;144(3):497-505. doi: 10.1016/j.jep.2012.09.019. Epub 2012 Oct 13.


DOI:10.1016/j.jep.2012.09.019
PMID:23069941
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE: Lafoensia pacari St.-Hil. is a tree native to the Brazilian Cerrado. Its bark macerate is popularly used in Brazilian folk medicine for the treatment of peptic ulcer, wound healing and inflammation. AIM OF THE STUDY: To evaluate the antiulcer activities of the methanol extract of Lafoensia pacari (MELP) and possible mechanisms of actions involved. MATERIALS AND METHODS: The stem bark of Lafoensia pacari was macerated in methanol to obtain the crude methanol extract of Lafoensia pacari (MELP). The gastroprotective and ulcer healing of MELP were evaluated using ethanol, indomethacin, cold-restraint stress-induced (acute) and acetic acid (chronic) ulcer models. The probable mode of action of MELP was also evaluated by determining intestinal transit, involvement of non-protein sulfhyhydryls (NP-SH), gastric mucus secretion, gastric secretory parameters and pro-inflammatory cytokines, tumor necrosis factor-α (TNF-α) and interleukin-17 (IL-17). Phytochemical analysis was carried out using classical methods and ellagic acid, one of the most important pharmacological active compounds was confirmed by HPLC. RESULTS: The results of the pharmacological studies on MELP demonstrated potent and effective gastroprotection against ethanol, indomethacin and cold stress-induced acute ulcers and ulcer healing in acetic acid induced chronic ulcer. MELP had no significant effect on the intestinal motility and it is also independent of mucus production but rather have a mucolytic effect. In pylorus-ligated rats the extract showed anti-secretory activity by decreasing total gastric juice volume and gastric acidity while increasing the gastric pH. The gastroprotection against ethanol is partially attributed to effective attenuation in the decrease in NP-SH levels, inhibition of the increases in the pro-inflammatory cytokines, TNF-α and IL-17. Phytochemical analysis of MELP revealed the presence of pyrrogalic tannins, saponins, steroids, triterpenoids and simple phenols, with ellagic acid being the major components. CONCLUSION: The results of this study showed that MELP possesses preventive and curative effects against gastric ulcer in experimental animals. These effects are partly dependent on its anti-oxidant, anti-secretory properties and inhibition of pro-inflammatory cytokines and independent of gastric/intestinal motility and mucus secretion. Ellagic acid, a compound of proven antiulcer activity, was found in MELP as the major component. These results confirmed the traditional use of MELP in Brazilian popular medicine for the treatment of gastric ulcers and shed some light on some of its mechanisms of action.

摘要

民族药理学相关性:Lafoensia pacari St.-Hil. 是一种原产于巴西塞拉多的树。其树皮浸膏在巴西民间医学中被广泛用于治疗消化性溃疡、伤口愈合和炎症。

研究目的:评估 Lafoensia pacari(MELP)甲醇提取物的抗溃疡活性及其可能涉及的作用机制。

材料和方法:用甲醇浸渍 Lafoensia pacari 的茎皮以获得 Lafoensia pacari(MELP)的粗甲醇提取物。使用乙醇、吲哚美辛、冷束缚应激(急性)和乙酸(慢性)溃疡模型评估 MELP 的胃保护和溃疡愈合作用。还通过测定肠转运、非蛋白巯基(NP-SH)的参与、胃粘液分泌、胃分泌参数和促炎细胞因子、肿瘤坏死因子-α(TNF-α)和白介素-17(IL-17)来评估 MELP 的可能作用模式。使用经典方法进行植物化学分析,并通过 HPLC 确认鞣花酸是最重要的药理活性化合物之一。

结果:MELP 的药理学研究结果表明,它对乙醇、吲哚美辛和冷应激引起的急性溃疡以及乙酸诱导的慢性溃疡具有强大而有效的胃保护作用,并能促进溃疡愈合。MELP 对肠道蠕动没有明显影响,也不依赖于粘液产生,而是具有粘液溶解作用。在幽门结扎大鼠中,提取物通过减少总胃液量和胃酸来显示抗分泌活性,同时增加胃 pH 值。乙醇的胃保护作用部分归因于有效抑制 NP-SH 水平降低、抑制促炎细胞因子 TNF-α和 IL-17 的增加。MELP 的植物化学分析显示存在吡咯烷单宁、皂苷、类固醇、三萜和简单酚类,其中鞣花酸是主要成分。

结论:本研究结果表明,MELP 对实验动物的胃溃疡具有预防和治疗作用。这些作用部分依赖于其抗氧化、抗分泌特性以及抑制促炎细胞因子,并且与胃/肠道蠕动和粘液分泌无关。鞣花酸是一种具有抗溃疡活性的化合物,在 MELP 中被发现是主要成分。这些结果证实了 MELP 在巴西民间医学中用于治疗胃溃疡的传统用途,并阐明了其一些作用机制。

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