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从尼日利亚东部槲寄生(Loranthus micranthus(Linn))中分离得到的一种羽扇豆烷三萜酯的免疫调节活性。

Immunomodulatory activity of a lupane triterpenoid ester isolated from the eastern Nigeria mistletoe, Loranthus micranthus (Linn).

机构信息

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria, 410001, Nsukka, Nigeria.

出版信息

Asian Pac J Trop Med. 2011 Jul;4(7):514-22. doi: 10.1016/S1995-7645(11)60137-5.

Abstract

OBJECTIVE

To provide further evidence for the ethnomedicinal use of the Eastern Nigeria mistletoe, Loranthus micranthus (L. micranthus), as an immunostimulant.

METHODS

Solvent fractions from the crude extract of the mistletoe plant was obtained and screened by the cell mediated delayed type hypersensitivity reaction (DTHR) model in mice. Then the immunomodulatory potentials of a major lupane triterpenoid ester isolated from an active hexane fraction of the Eastern Nigeria mistletoe was investigated. Three lupeol-based triterpenoid esters: 7β 15α-dihydroxyl-lup-20(29)-ene-3β-palmitate (I), 7β, 15α-dihydroxyl-lup-20(29)-ene-3β-stearate (II) and 7β, 15α-dihydroxyl-lup-20(29)-ene-3β-decadecanoate (III) were isolated from the plant leaves epiphyting on a local kola nut tree and were characterized. Compound 1 was subjected to cell proliferation studies using C57Bl/6 splenocytes at three dose levels (5, 25 and 100 μg/mL) in presence of controls. Furthermore, the effect of this compound on IL-8 receptor expression was evaluated at three doses (1, 5 and 10 μg/mL) using the real time polymerase chain reaction assay.

RESULTS

This triterpenoid ester produced some enhancement of the splenocytes at the tested doses but at doses higher than 5 μg/mL caused inhibition of the IL-8 receptor expression.

CONCLUSIONS

The present findings support the ethnomedicinal use of the Eastern Nigeria Mistletoe in the management of diseases affecting the immune system. The triterpenoid(s) have some immunomodulatory abilities on splenocytes and IL-8 receptors and may partly account for the overall immunomodulatory activity of this plant.

摘要

目的

为尼日利亚东部槲寄生作为免疫刺激剂的民间药用提供进一步的证据。

方法

从槲寄生植物的粗提取物中获得溶剂馏分,并通过细胞介导的迟发型超敏反应(DTHR)模型在小鼠中进行筛选。然后研究了从尼日利亚东部槲寄生活性正己烷馏分中分离得到的主要羽扇豆烷三萜酯的免疫调节潜力。从寄生在当地可乐果树上的植物叶子中分离出三种羽扇豆烷三萜酯:7β15α-二羟基-羊毛甾-20(29)-烯-3β-棕榈酸酯(I)、7β、15α-二羟基-羊毛甾-20(29)-烯-3β-硬脂酸酯(II)和 7β、15α-二羟基-羊毛甾-20(29)-烯-3β-癸酸酯(III),并对其进行了表征。在存在对照的情况下,将化合物 1 在三个剂量水平(5、25 和 100 μg/mL)下用于 C57Bl/6 脾细胞的细胞增殖研究。此外,使用实时聚合酶链反应测定法在三个剂量(1、5 和 10 μg/mL)下评估了该化合物对 IL-8 受体表达的影响。

结果

该三萜酯在测试剂量下对脾细胞有一定的增强作用,但在剂量高于 5 μg/mL 时会抑制 IL-8 受体的表达。

结论

本研究结果支持尼日利亚东部槲寄生在治疗影响免疫系统疾病中的民间药用。三萜类化合物对脾细胞和 IL-8 受体具有一定的免疫调节作用,可能部分解释了该植物的整体免疫调节活性。

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