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蓬莪术(L.)Mansf。的甲醇提取物及其主要化合物 pinostrobin 在体内诱导抗溃疡作用:可能涉及间接抗氧化作用。

The methanolic extract of Boesenbergia rotunda (L.) Mansf. and its major compound pinostrobin induces anti-ulcerogenic property in vivo: possible involvement of indirect antioxidant action.

机构信息

Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.

出版信息

J Ethnopharmacol. 2011 Sep 2;137(2):963-70. doi: 10.1016/j.jep.2011.07.010. Epub 2011 Jul 8.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Boesenbergia rotunda (L) Mansf. has been used for the treatment of gastrointestinal disorders including peptic ulcer. In the current study we aimed to investiagte the anti-ulcer activities of methanolic extract of B. rotunda (MEBR) and its main active compound, pinostrobin on ethanol-induced ulcer in rats. The possible involevement of lipid peroxidation, nitric oxide, cyclooxygenases and free radical scavenging mechanisms also has been investigated.

MATERIALS AND METHODS

Pinostrobin was isolated form the rhizomes of B. rotunda. Ulcer index, gastric juice acidity, mucus content, gross and histological gastric lesions and thiobarbituric acid reactive substances (TBARS) were evaluated in ethanol-induced ulcer in vivo. The effect of pinostrobin into lipopolysaccharide/interferon-γ stimulated rodent cells, COX-1 and COX-2 activities were done in vitro.

RESULTS

Pre-treatment with MEBR, pinostrobin or omeprazole protected the gastric mucosa as seen by reduction in ulcer area and mucosal content, reduced or absence of submucosal edema and leucocytes infiltration. Pinostrobin significantly (p<0.05) lowered the elevated TBARS level into gasteric homogenate. Pinostrobin did not produced significant in vitro inhibition of NO from LPS/IFN-γ activated rodent cells without affecting the viability of these cells. Further, the compound did bot revleaed inhibitory effects on both COX- 1& 2 enzymes. The antioxidant assays also exhibited non significance in vitro.

CONCLUSION

Thus it can be concluded that MEBR possesses anti-ulcer activity, which could be attributed to indirect anti-oxidant mechanism of pinostrobin but not to the intervention with nitric oxide and COX inflammation pathways.

摘要

民族药理学相关性

蓬莪术(L)曼斯菲尔德已被用于治疗胃肠道疾病,包括消化性溃疡。在本研究中,我们旨在研究蓬莪术甲醇提取物(MEBR)及其主要活性化合物 pinostrobin 对乙醇诱导的大鼠溃疡的抗溃疡活性。还研究了脂质过氧化、一氧化氮、环氧化酶和自由基清除机制的可能参与。

材料和方法

pinostrobin 从蓬莪术的根茎中分离出来。在体内乙醇诱导的溃疡中,评估溃疡指数、胃液酸度、粘液含量、大体和组织学胃损伤以及硫代巴比妥酸反应物质(TBARS)。在体外,研究了 pinostrobin 对脂多糖/干扰素-γ刺激的啮齿动物细胞、COX-1 和 COX-2 活性的影响。

结果

MEBR、pinostrobin 或奥美拉唑预处理可通过减少溃疡面积和粘膜含量、减少或消除粘膜下水肿和白细胞浸润来保护胃粘膜。pinostrobin 可显著(p<0.05)降低胃匀浆中升高的 TBARS 水平。pinostrobin 对 LPS/IFN-γ 激活的啮齿动物细胞中的 NO 没有产生显著的体外抑制作用,也不影响这些细胞的活力。此外,该化合物对 COX-1 和 COX-2 酶均未表现出抑制作用。抗氧化剂测定也显示体外无意义。

结论

因此,可以得出结论,MEBR 具有抗溃疡活性,这可能归因于 pinostrobin 的间接抗氧化机制,而不是干预一氧化氮和 COX 炎症途径。

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