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巴西东北部红蜂胶提取物的胃保护作用及其分离化合物的作用。

The gastroprotective effect of red propolis extract from Northeastern Brazil and the role of its isolated compounds.

机构信息

School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil.

Postgraduate Program in Pharmaceutical Sciences (PPGCF), Nucleus for Chemical-Pharmaceutical Investigations (NIQFAR), University of Vale Do Itajaí (UNIVALI), Itajaí, SC, Brazil.

出版信息

J Ethnopharmacol. 2021 Mar 1;267:113623. doi: 10.1016/j.jep.2020.113623. Epub 2020 Nov 25.

DOI:10.1016/j.jep.2020.113623
PMID:33246124
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Propolis has been used in folk medicine to treat gastric disorders for centuries. However, although studies have been conducted to validate the gastroprotective and anti-ulcer activity of some types of propolis, red propolis activity remains unknown.

AIM OF THE STUDY

The present study aimed to evaluate the gastroprotective effect of the hydroalcoholic extract of red propolis (HERP), its mode of action, and the main compounds involved in its activity, therefore contributing to validate the chemical and pharmacological potential of this product.

MATERIAL AND METHODS

The effect of HERP (30, 100 and 300 mg/kg p.o. and 30 mg/kg i.p.), and the isolated compounds vestitol (VS), neovestitol (NV), methylvestitol (MV), medicarpin (MD), and oblongifolin AB (OB) (10 mg/kg p.o.) were evaluated on gastric ulcers induced by 60% ethanol/0.3 M HCl (5 mL/kg, p.o.) in mice. Histological changes and mucin levels were assessed by HE and PAS, respectively. Moreover, oxidative stress parameters and myeloperoxidase activity were analyzed on ulcerated tissue. The effect of HERP on gastric acid secretion was evaluated by pyloric ligature model and the mechanisms involved in its gastroprotective effect were investigated by pretreating mice with L-NAME (a non-selective nitric oxide synthase inhibitor, 70 mg/kg, i.p.), NEM (a sulfhydryl group chelator, 10 mg/kg, i.p.), yohimbine (an alpha-adrenergic receptor antagonist, 2 mg/kg, i.p.) and indomethacin (a non-selective cyclooxygenase inhibitor, 10 mg/kg, i.p.).

RESULTS

HERP (300 mg/kg p.o. or 30 mg/kg i.p.), MV, and MD (10 mg/kg p.o.) protected gastric mucosa against the damage induced by ethanol/HCl. Histological changes were attenuated by the HERP, MV, and MD. Moreover, HERP and MV increased mucin levels. Besides, oxidative stress and MPO activity were reduced by the three treatments. HERP did not display anti-secretory action, but its effect was abolished by indomethacin treatment.

CONCLUSIONS

HERP displays gastroprotective property against ethanol/HCl-induced damage. Its effect is dependent on prostaglandins and mucin production. The compounds MV and MD may have an essential role in the activity of HERP. Our data contribute to validate the traditional use of propolis for gastric disorders.

摘要

民族药理学相关性

蜂胶在民间医学中已被用于治疗胃部疾病数百年。然而,尽管已经进行了研究来验证某些类型蜂胶的胃保护和抗溃疡活性,但红色蜂胶的活性仍不清楚。

研究目的

本研究旨在评估红色蜂胶水醇提取物(HERP)的胃保护作用、作用方式以及其活性涉及的主要化合物,从而有助于验证该产品的化学和药理学潜力。

材料和方法

评估 HERP(30、100 和 300mg/kg 口服和 30mg/kg 腹腔注射)以及分离化合物 Vestitol(VS)、Neovestitol(NV)、Methylvestitol(MV)、Medicarpin(MD)和 Oblongifolin AB(OB)(10mg/kg 口服)对乙醇/0.3M HCl(5mL/kg,口服)诱导的小鼠胃溃疡的影响。通过 HE 和 PAS 分别评估组织学变化和粘蛋白水平。此外,还分析了溃疡组织中的氧化应激参数和髓过氧化物酶活性。通过幽门结扎模型评估 HERP 对胃酸分泌的影响,并通过预先用 L-NAME(一种非选择性一氧化氮合酶抑制剂,70mg/kg,腹腔注射)、NEM(一种巯基基团螯合剂,10mg/kg,腹腔注射)、育亨宾(一种α-肾上腺素能受体拮抗剂,2mg/kg,腹腔注射)和吲哚美辛(一种非选择性环氧化酶抑制剂,10mg/kg,腹腔注射)预处理小鼠来研究其胃保护作用的机制。

结果

HERP(300mg/kg 口服或 30mg/kg 腹腔注射)、MV 和 MD(10mg/kg 口服)可保护胃黏膜免受乙醇/HCl 引起的损伤。HERP、MV 和 MD 减轻了组织学变化。此外,HERP 和 MV 增加了粘蛋白水平。此外,三种处理均降低了氧化应激和 MPO 活性。HERP 没有显示出抗分泌作用,但它的作用被吲哚美辛处理所消除。

结论

HERP 对乙醇/HCl 诱导的损伤具有胃保护作用。其作用依赖于前列腺素和粘蛋白的产生。化合物 MV 和 MD 可能在 HERP 的活性中起重要作用。我们的数据有助于验证蜂胶在治疗胃部疾病方面的传统用途。

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