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在[具体亚种名称未给出]中鉴定出白皮杉醇：一种天然存在的芪类化合物，可抑制脂多糖诱导的促炎细胞因子和介质的表达，并抑制JAK/STAT信号通路。

Identification of Pinosylvin in subsp. : A Naturally Occurring Stilbenoid Suppressing LPS-Induced Expression of Pro-Inflammatory Cytokines and Mediators and Inhibiting the JAK/STAT Signaling Pathway.

作者信息

Perri Maria Rosaria, Pellegrino Michele, Marrelli Mariangela, Aquaro Stefano, Cavaliere Fabiola, Grande Fedora, Occhiuzzi Maria Antonietta, Lupia Carmine, Toma Claudia-Crina, Conforti Filomena, Statti Giancarlo

机构信息

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.

Mediterranean Ethnobotanical Conservatory, 88054 Sersale, Italy.

出版信息

Pharmaceuticals (Basel). 2023 May 9;16(5):718. doi: 10.3390/ph16050718.

DOI:10.3390/ph16050718
PMID:37242501
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10221723/
Abstract

Stilbenoids, a group of phytoalexin polyphenols produced by plants as a defence mechanism in response to stress conditions, are known for their anti-inflammatory potential. Pinosylvin, a naturally occurring molecule traditionally found in pinus trees, was here identified in subsp. var. from Southern Italy through HPLC analysis. Both this molecule and its well-known analogue resveratrol, the most famous wine polyphenol, were compared for their in vitro potential anti-inflammatory activity. Pinosylvin significantly inhibited the release of pro-inflammatory cytokines (TNF-α and IL-6) and NO mediator in LPS-stimulated RAW 264.7 cells. Moreover, its ability to inhibit the JAK/STAT signaling pathway was assessed: Western blot analyses showed a downregulation of both phosphorylated JAK2 and STAT3 proteins. Finally, in order to verify whether this biological activity could be attributed to a direct interaction of pinosylvin with JAK2, a molecular docking study was performed, confirming the capability of pinosylvin to bind the active site of the protein.

摘要

芪类化合物是植物在应激条件下作为防御机制产生的一类植保素多酚，以其抗炎潜力而闻名。松二氢愈创木脂是一种传统上在松树中发现的天然分子，通过高效液相色谱分析在来自意大利南部的亚种变种中鉴定出来。将该分子与其著名的类似物白藜芦醇（最著名的葡萄酒多酚）的体外潜在抗炎活性进行了比较。松二氢愈创木脂显著抑制脂多糖刺激的RAW 264.7细胞中促炎细胞因子（TNF-α和IL-6）和NO介质的释放。此外，评估了其抑制JAK/STAT信号通路的能力：蛋白质印迹分析显示磷酸化JAK2和STAT3蛋白均下调。最后，为了验证这种生物活性是否可归因于松二氢愈创木脂与JAK2的直接相互作用，进行了分子对接研究，证实了松二氢愈创木脂与该蛋白质活性位点结合的能力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/5b7db02a6f2b/pharmaceuticals-16-00718-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/2f5f28f593e1/pharmaceuticals-16-00718-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/14fdb24009de/pharmaceuticals-16-00718-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/298a3b184eab/pharmaceuticals-16-00718-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/d92d32c95ebd/pharmaceuticals-16-00718-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/5b7db02a6f2b/pharmaceuticals-16-00718-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/2f5f28f593e1/pharmaceuticals-16-00718-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/14fdb24009de/pharmaceuticals-16-00718-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/298a3b184eab/pharmaceuticals-16-00718-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/d92d32c95ebd/pharmaceuticals-16-00718-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d697/10221723/5b7db02a6f2b/pharmaceuticals-16-00718-g005.jpg

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Signal Transduct Target Ther. 2021 Nov 26;6(1):402. doi: 10.1038/s41392-021-00791-1.
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松二氢黄酮作为一种有前景的天然抗癌剂：作用机制及癌症治疗的未来方向
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