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来自北美木兰属植物且具有环氧合酶2抑制活性的新木脂素。

Neolignans from North American Magnolia species with cyclooxygenase 2 inhibitory activity.

作者信息

Schühly W, Khan S I, Fischer N H

机构信息

Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Universitätsplatz 4, 8010 Graz, Austria.

出版信息

Inflammopharmacology. 2009 Apr;17(2):106-10. doi: 10.1007/s10787-009-7013-y.

DOI:10.1007/s10787-009-7013-y
PMID:19214385
Abstract

OBJECTIVES

Based upon reported ethnomedicinal use by Native Americans, extracts and pure isolates from leaves and seeds of Magnolia grandiflora, M. virginiana, M. acuminata and M. macrophylla, all native to the Southeastern United States, were investigated for their anti-inflammatory potential against cyclooxygenase 2 (COX-2).

MATERIAL AND METHODS

The extracts and pure compounds from Magnolia species were tested for their production of prostaglandin E(2) (PGE(2)) using a mouse macrophage (RAW 264.7) assay where cells were stimulated by lipopolysaccharide.

RESULTS

Leaf extracts were moderately active (44-58% inhibition at 50 microg/ml) whereas seed extracts showed significant activity of 54-88% inhibition, respectively. In the seed extract of M. grandiflora, honokiol, magnolol and 4'-O-methylhonokiol strongly inhibited COX-2 (IC(50): 1.2-2.0 microg/ml), 3-O-methylmagnolol was moderately active while a new compound was inactive towards COX-2. The neolignans were not cytotoxic to macrophages (RAW 264.7) and kidney fibroblast (VERO) cells in vitro.

CONCLUSIONS

The results indicate that the reported ethnomedicinal use of the investigated Magnolia species is in agreement with anti-inflammatory activity of their respective compounds.

摘要

目的

基于美国原住民报告的民族药用情况,对原产于美国东南部的北美木兰、弗吉尼亚木兰、渐尖木兰和大叶木兰的叶和种子提取物及纯分离物进行了抗环氧化酶2(COX-2)的抗炎潜力研究。

材料与方法

使用小鼠巨噬细胞(RAW 264.7)试验,通过脂多糖刺激细胞,检测木兰属植物的提取物和纯化合物产生前列腺素E2(PGE2)的情况。

结果

叶提取物活性中等(50微克/毫升时抑制率为44%-58%),而种子提取物的抑制率分别为54%-88%,显示出显著活性。在北美木兰的种子提取物中,厚朴酚、厚朴树皮酚和4'-O-甲基厚朴酚强烈抑制COX-2(半数抑制浓度:1.2-2.0微克/毫升),3-O-甲基厚朴酚活性中等,而一种新化合物对COX-2无活性。新木脂素在体外对巨噬细胞(RAW 264.7)和肾成纤维细胞(VERO)无细胞毒性。

结论

结果表明,所研究的木兰属植物的民族药用报告与其各自化合物的抗炎活性一致。

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