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从醉鱼草属植物的叶子中分离和合成新的抗炎性酚酰胺 melodamide A。

Isolation and synthesis of melodamide A, a new anti-inflammatory phenolic amide from the leaves of Melodorum fruticosum.

机构信息

Department of Pharmacy, China Medical University, Taichung, Taiwan.

出版信息

Planta Med. 2013 Mar;79(3-4):288-94. doi: 10.1055/s-0032-1328131. Epub 2013 Jan 23.

Abstract

Together with twelve known compounds (2-13), melodamide A (1), a new phenolic amide possessing p-quinol moiety, was purified and characterized from the methanolic extracts of the leaves of Melodorum fruticosum. The structure of melodamide A (1) was established with a combination of 2D NMR experiments, HR-ESI-MS and X-ray analyses. The other known compounds were identified by comparison of their spectroscopic and physical data with those reported in the literature. Moreover, some isolated compounds were examined for their inhibitory activity towards superoxide anion generation and elastase release in human neutrophils. Among the tested compounds, 1, 3, and 5 exhibited strong inhibition of superoxide anion generation with IC50 values ranging from 5.25 to 8.65 µM. Furthermore, synthesis and biological evaluation of melodamide A (1) and its analogs (14a-p) were described.

摘要

与十二种已知化合物(2-13)一起,从醉鱼草(Melodorum fruticosum)叶的甲醇提取物中分离得到并鉴定了一种新的酚酰胺化合物 melodamide A(1),它具有 p-醌部分。通过二维 NMR 实验、高分辨电喷雾质谱(HR-ESI-MS)和 X 射线分析相结合,确定了 melodamide A(1)的结构。其他已知化合物通过与文献报道的光谱和物理数据进行比较来鉴定。此外,还对一些分离得到的化合物进行了超氧阴离子生成和人中性粒细胞弹性蛋白酶释放抑制活性的测试。在所测试的化合物中,化合物 1、3 和 5 对超氧阴离子生成具有很强的抑制作用,IC50 值范围为 5.25-8.65µM。此外,还描述了 melodamide A(1)及其类似物(14a-p)的合成和生物评价。

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