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白花前胡根提取物中的具有多药耐药逆转及抗炎活性的吡喃香豆素类成分。

Pyranocoumarins from Root Extracts of Peucedanum praeruptorum Dunn with Multidrug Resistance Reversal and Anti-Inflammatory Activities.

作者信息

Lee Jun, Lee You Jin, Kim Jinhee, Bang Ok-Sun

机构信息

KM Convergence Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, Korea.

Korean Medicine Life Science, University of Science & Technology, Daejeon 34054, Korea.

出版信息

Molecules. 2015 Nov 25;20(12):20967-78. doi: 10.3390/molecules201219738.

Abstract

In the search for novel herbal-based anticancer agents, we isolated a new angular-type pyranocoumarin, (+)-cis-(3'S,4'S)-3'-angeloyl-4'-tigloylkhellactone (1) along with 12 pyranocoumarins (2-13), two furanocoumarins (14, 15), and a polyacetylene (16) were isolated from the roots of Peucedanum praeruptorum using chromatographic separation methods. The structures of the compounds were determined using spectroscopic analysis with nuclear magnetic resonance (NMR) and high-resolution-electrospray ionization-mass spectrometry (HR-ESI-MS). The multidrug-resistance (MDR) reversal and anti-inflammatory effects of all the isolated compounds were evaluated in human sarcoma MES-SA/Dx5 and lipopolysaccharide (LPS)-induced RAW 264.7 cells. Among the 16 tested compounds, two (2 and 16) downregulated nitric oxide (NO) production and five (1, 7, 8, 11, and 13) inhibited the efflux of drugs by MDR protein, indicating the reversal of MDR. Therefore, these compounds may be potential candidates for the development of effective agents against MDR forms of cancer.

摘要

在寻找新型基于草药的抗癌药物的过程中,我们使用色谱分离方法从白花前胡的根中分离出一种新的角型吡喃香豆素,(+)-顺式-(3'S,4'S)-3'-当归酰基-4'-惕各酰基凯刺内酯(1),同时还分离出12种吡喃香豆素(2 - 13)、两种呋喃香豆素(14,15)和一种聚乙炔(16)。使用核磁共振(NMR)光谱分析和高分辨率电喷雾电离质谱(HR - ESI - MS)确定了这些化合物的结构。在人肉瘤MES - SA/Dx5细胞和脂多糖(LPS)诱导的RAW 264.7细胞中评估了所有分离化合物的多药耐药(MDR)逆转和抗炎作用。在16种测试化合物中,两种(2和16)下调了一氧化氮(NO)的产生,五种(1、7、8、11和13)抑制了MDR蛋白介导的药物外排,表明具有MDR逆转作用。因此,这些化合物可能是开发针对MDR型癌症的有效药物的潜在候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8aa2/6332054/2fcad868a944/molecules-20-19738-g001.jpg

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