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源自……的化合物的抗炎活性

Anti-Inflammatory Activity of Compounds Derived from .

作者信息

Le DucDat, Han Sanghee, Min Kyung Hyun, Lee Mina

机构信息

College of Pharmacy and Research Institute of Life and Pharmaceutical Sciences, Sunchon National University, 255 Jungangno, Suncheon 57922, Republic of Korea.

School of Pharmacy and Institute of New Drug Development, Jeonbuk National University, Jeonju 54896, Republic of Korea.

出版信息

Metabolites. 2023 Feb 9;13(2):249. doi: 10.3390/metabo13020249.

DOI:10.3390/metabo13020249
PMID:36837867
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9962727/
Abstract

The objective of this study is to describe the separation and identification of one new phenolic and 19 known compounds from . Their structures were determined based on spectroscopic (NMR, CD, and MS) data analysis or Mosher's method, and were compared with those reported in the literature. These isolates were then evaluated for their anti-inflammatory and antioxidant activities based on the inhibition of nitric oxide (NO) and interleukin (IL)-8 production in lipopolysaccharide (LPS)-stimulated cells (RAW264.7 and HT-29) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging abilities, respectively. In the NO assay, compounds - showed strong inhibition with compounds and displaying significant inhibition. In the IL-8 assay, compounds , , , , , and exhibited potential to inhibit IL-8 production and other compounds displayed moderate inhibition. An in silico docking approach also revealed strong binding affinities for protein-ligand complexes of these active compounds against IL-8 production. The docking results were correlated with the experimental data of the IL-8 assay. Thus, these active compounds should be considered as candidates for further in vivo studies. This study implies the potential of new and active chemicals isolated from . and provides evidence to support the development of active fractions and constituents into functional products targeting inflammatory diseases the future.

摘要

本研究的目的是描述从……中分离和鉴定出一种新的酚类化合物和19种已知化合物。它们的结构是基于光谱(核磁共振、圆二色和质谱)数据分析或莫舍尔方法确定的,并与文献报道的结构进行了比较。然后,基于对脂多糖(LPS)刺激的细胞(RAW264.7和HT-29)中一氧化氮(NO)和白细胞介素(IL)-8产生的抑制作用以及2,2-二苯基-1-苦基肼(DPPH)自由基清除能力,分别对这些分离物的抗炎和抗氧化活性进行了评估。在NO测定中,化合物……表现出强烈的抑制作用,化合物……表现出显著的抑制作用。在IL-8测定中,化合物……、……、……、……、……和……表现出抑制IL-8产生的潜力,其他化合物表现出中等程度的抑制作用。一种计算机对接方法还揭示了这些活性化合物与蛋白质-配体复合物对IL-8产生的强结合亲和力。对接结果与IL-8测定的实验数据相关。因此,这些活性化合物应被视为进一步体内研究的候选物。本研究暗示了从……中分离出的新的活性化学物质的潜力,并为将活性成分和组分开发成针对未来炎症性疾病的功能性产品提供了证据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/29356ecc0e86/metabolites-13-00249-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/829a84cbd8a4/metabolites-13-00249-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/5db7e8a5d71a/metabolites-13-00249-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/163d0cee0a7d/metabolites-13-00249-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/7db1cade6c71/metabolites-13-00249-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/609955499815/metabolites-13-00249-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/b1353747f3fd/metabolites-13-00249-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/29356ecc0e86/metabolites-13-00249-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/829a84cbd8a4/metabolites-13-00249-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/5db7e8a5d71a/metabolites-13-00249-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/163d0cee0a7d/metabolites-13-00249-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/7db1cade6c71/metabolites-13-00249-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/609955499815/metabolites-13-00249-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/b1353747f3fd/metabolites-13-00249-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e35/9962727/29356ecc0e86/metabolites-13-00249-g007.jpg

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