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贯叶连翘叶的抗溃疡活性及作用机制研究

Antiulcer Activity and Potential Mechanism of Action of the Leaves of L.

机构信息

Department of Pharmaceutical Sciences, Universidade Federal de Pernambuco, Recife, PE, Brazil.

Institute of Chemistry and Biotechnology, Universidade Federal de Alagoas, Maceió, AL, Brazil.

出版信息

Oxid Med Cell Longev. 2018 Apr 26;2018:1731459. doi: 10.1155/2018/1731459. eCollection 2018.

Abstract

L. is used in folk medicine for the treatment of inflammation and gastrointestinal diseases. Our study investigated the antiulcer activity of ethanolic extract (SmEE) and its majority compounds gallic acid (GA) and ellagic acid (EA). Phytochemical characterization was performed by HPLC. The SmEE was screened for in vitro antioxidant activities using phosphomolybdenum, ABTS, DPPH, and FRAP assays. The antiulcer activity of SmEE, GA, EA, or GA + EA was evaluated by gastric lesion models induced by absolute ethanol and indomethacin. Following this, it is capable of stimulating mucus production, antisecretory capacity, and the influence of -SH groups and NO in the effect of SmEE. Its healing activity was demonstrated by acetic acid-induced chronic ulcer model. Anti- activity was assessed by determining the MIC of the SmEE (64-1024 g/mL). The HPLC results identified the presence of gallic acid and ellagic acid in SmEE. The extract showed antioxidant activity in vitro. SmEE (50, 100, and 200 mg/kg) reduced the area of ulcerative lesions induced by ethanol in 23.8, 90.3, and 90.2%, respectively. In NSAID model, the SmEE induced protection of 36.8, 49.4, and 49.9%, respectively. GA (10 mg/kg) or EA (7 mg/kg) or the association of GA + EA (10 + 7 mg/kg) inhibited the ethanol-induced lesions in 71.8, 70.9, and 94.9%, respectively, indicating synergistic action. SmEE (100 mg/kg) decreased acid secretion and H concentration in the gastric contents, increased levels of mucus, and showed to be dependent of -SH groups and NO on the protection of the gastric mucosa. In chronic ulcer model, SmEE reduced the gastric area lesion. SmEE showed anti- activity. In conclusion, our study showed that SmEE has antiulcerogenic activity. GA and EA are isolated gastric protectors and, when associated, acted synergistically to protect the gastric mucosa.

摘要

L. 在民间医学中用于治疗炎症和胃肠道疾病。我们的研究调查了乙醇提取物(SmEE)及其主要化合物没食子酸(GA)和鞣花酸(EA)的抗溃疡活性。通过 HPLC 进行植物化学表征。使用磷钼酸盐、ABTS、DPPH 和 FRAP 测定法筛选 SmEE 的体外抗氧化活性。通过使用无水乙醇和吲哚美辛诱导的胃损伤模型评估 SmEE、GA、EA 或 GA+EA 的抗溃疡活性。在此之后,它能够刺激粘液产生、抗分泌能力以及 -SH 基团和 NO 在 SmEE 作用中的影响。通过乙酸诱导的慢性溃疡模型证明其愈合活性。通过测定 SmEE 的 MIC(64-1024μg/mL)评估抗活性。HPLC 结果表明 SmEE 中存在没食子酸和鞣花酸。提取物在体外具有抗氧化活性。SmEE(50、100 和 200mg/kg)分别减少了乙醇诱导的溃疡病变面积的 23.8%、90.3%和 90.2%。在 NSAID 模型中,SmEE 分别诱导了 36.8%、49.4%和 49.9%的保护作用。GA(10mg/kg)或 EA(7mg/kg)或 GA+EA 的联合(10+7mg/kg)分别抑制了乙醇诱导的病变,抑制率分别为 71.8%、70.9%和 94.9%,表明具有协同作用。SmEE(100mg/kg)降低了胃酸分泌和胃内容物中的 H 浓度,增加了粘液水平,并显示出对胃黏膜保护作用依赖于 -SH 基团和 NO。在慢性溃疡模型中,SmEE 减少了胃区病变。SmEE 具有抗活性。总之,我们的研究表明 SmEE 具有抗溃疡活性。GA 和 EA 是分离的胃保护剂,当联合使用时,可协同保护胃黏膜。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d7/5944294/ee05c7ae8c04/OMCL2018-1731459.001.jpg

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