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Myrtinols A-F:来自澳大利亚本土植物叶子的新型抗炎 Peltogynoid 类黄酮衍生物。

Myrtinols A-F: New Anti-Inflammatory Peltogynoid Flavonoid Derivatives from the Leaves of Australian Indigenous Plant .

机构信息

NICM Health Research Institute, Western Sydney University, Penrith, NSW 2750, Australia.

Department of Pharmacology, Western Sydney University, Campbelltown Campus, Sydney, NSW 2560, Australia.

出版信息

Molecules. 2023 Feb 25;28(5):2160. doi: 10.3390/molecules28052160.

Abstract

Our in-house ethnopharmacological knowledge directed our anti-inflammatory investigation into the leaves of . Bioassay guided isolation of the Australian indigenous plant led to the isolation of six new rare peltogynoid derivatives named myrtinols A-F (-) along with three known compounds 4--methylcedrusin (), 7--methylcedrusin () and 8-demethylsideroxylin (). The chemical structures of all the compounds were elucidated by detailed spectroscopic data analysis, and absolute configuration was established using X-ray crystallography analysis. All compounds were evaluated for their anti-inflammatory activity by assessing the inhibition of nitric oxide (NO) production and tumor necrosis factor- α (TNF-α) in lipopolysaccharide (LPS) and interferon (IFN)-γ activated RAW 264.7 macrophages. A structure activity relationship was also established between compounds (-), noting promising anti-inflammatory potential by compounds and with an IC value of 8.51 ± 0.47 and 8.30 ± 0.96 µg/mL for NO inhibition and 17.21 ± 0.22 and 46.79 ± 5.87 µg/mL for TNF-α inhibition, respectively.

摘要

我们内部的民族药理学知识指导了我们对. 的叶子的抗炎研究。对澳大利亚本土植物的生物测定导向分离导致了六种新的罕见的 peltogynoid 衍生物的分离,命名为 myrtinols A-F (-),以及三种已知化合物 4--methylcedrusin ()、7--methylcedrusin () 和 8-demethylsideroxylin ()。所有化合物的化学结构都是通过详细的光谱数据分析阐明的,并通过 X 射线晶体学分析确定了绝对构型。所有化合物都通过评估其对脂多糖 (LPS) 和干扰素 (IFN)-γ 激活的 RAW 264.7 巨噬细胞中一氧化氮 (NO) 产生和肿瘤坏死因子-α (TNF-α) 的抑制作用来评估其抗炎活性。还建立了化合物 (-) 之间的构效关系,注意到化合物 和 具有有希望的抗炎潜力,其对 NO 抑制的 IC 值分别为 8.51 ± 0.47 和 8.30 ± 0.96 µg/mL,对 TNF-α 抑制的 IC 值分别为 17.21 ± 0.22 和 46.79 ± 5.87 µg/mL。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e47f/10004088/8bda114c2c29/molecules-28-02160-g001.jpg

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