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欧洲接骨木叶的抗溃疡活性及活性成分的分离

Anti-ulcerogenic activity and isolation of the active principles from Sambucus ebulus L. leaves.

作者信息

Yesilada Erdem, Gürbüz Ilhan, Toker Gülnur

机构信息

Yeditepe University, Faculty of Pharmacy, 34755 Atasehir, Istanbul, Turkey.

Gazi University, Faculty of Pharmacy, Etiler, 06330 Ankara, Turkey.

出版信息

J Ethnopharmacol. 2014 Apr 28;153(2):478-83. doi: 10.1016/j.jep.2014.03.004. Epub 2014 Mar 12.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Sambucus ebulus L. has a very prominent place in Turkish folk medicine. Leaves of the plant are practiced externally to relieve rheumatic pain, to treat abscess, for wound healing and internally against hemorrhoids and stomachache. In a previous work, aqueous extract of the leaves was shown to possess potent antiulcerogenic activity on water immersion and immobilization-induced stress ulcer model in rats. This study aims to investigate the antiulcerogenic activity profile of the plant on various in vivo peptic ulcer models and gastric biochemical parameters and through bioassay-guided processing to isolate the active constituent (s) and to elucidate its structure.

MATERIALS AND METHODS

Among the subextracts obtained by successive solvent extractions from the MeOH extract of the leaves, the butanol subextract exerted significant antiulcerogenic activity against water-immersion and immobilization-induced stress ulcer model in rats as the bioassay model. This subextract was then subjected to successive chemical separation techniques (precipitation, column chromatography based on ion-exchange, silica gel and sephadex) and the activity of each fraction/subfraction was tested using the same bioassay model. After determination of active principles, further studies were performed on the active subextract by using various in vivo test models (ethanol-, serotonin-, pyloric ligation-induced ulcerogenesis) in rats as well as biochemical methods for the evaluation of antiulcerogenic potential.

RESULTS

Bioassay-guided fractionation procedures yielded two flavonol glycosides as the active antiulcerogenic principles. The structures of these compounds were elucidated as isorhamnetin-3-O-monoglycoside and quercetin-3-O-monoglycoside by using (1)H, (13)C-NMR, and FAB-MS techniques.

CONCLUSION

This study has proven the folkloric use of Sambucus ebulus leaves for the treatment of gastric ailments in Turkish folk medicine. The antiulcerogenic activity of the two flavonol glycosides isolated in the present study was not previously reported elsewhere.

摘要

民族药理学相关性

接骨木在土耳其民间医学中占有非常突出的地位。该植物的叶子外用可缓解风湿疼痛、治疗脓肿、促进伤口愈合,内服可治疗痔疮和胃痛。在先前的一项研究中,叶子的水提取物在大鼠水浸和束缚应激性溃疡模型中显示出强大的抗溃疡活性。本研究旨在研究该植物在各种体内消化性溃疡模型和胃生化参数上的抗溃疡活性谱,并通过生物测定指导的方法分离活性成分并阐明其结构。

材料与方法

在通过连续溶剂萃取从叶子的甲醇提取物中获得的亚提取物中,丁醇亚提取物作为生物测定模型,对大鼠水浸和束缚应激性溃疡模型具有显著的抗溃疡活性。然后对该亚提取物进行连续化学分离技术(沉淀、基于离子交换、硅胶和葡聚糖凝胶的柱色谱),并使用相同的生物测定模型测试每个级分/亚级分的活性。在确定活性成分后,使用大鼠体内各种测试模型(乙醇、血清素、幽门结扎诱导的溃疡形成)以及评估抗溃疡潜力的生化方法,对活性亚提取物进行了进一步研究。

结果

生物测定指导的分级分离程序产生了两种黄酮醇苷作为活性抗溃疡成分。通过使用(1)H、(13)C-NMR和FAB-MS技术,将这些化合物的结构阐明为异鼠李素-3-O-单糖苷和槲皮素-3-O-单糖苷。

结论

本研究证实了接骨木叶在土耳其民间医学中用于治疗胃部疾病的民间用途。本研究中分离出的两种黄酮醇苷的抗溃疡活性此前在其他地方尚未见报道。

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