马尾黄苷A(一种来自马尾黄的苯并呋喃苷)通过抑制p38MAPK、JNK和C/EBPβ磷酸化抑制脂多糖诱导的COX-2表达

IF 5.6 2区 医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2024-12-01 Epub Date: 2023-12-07 DOI:10.1080/14756366.2023.2287420
Shiu-Wen Huang, Ming Jen Hsu, Hsiu-Chen Chen, Rita Meleddu, Simona Distinto, Elias Maccioni, Filippo Cottiglia
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引用次数: 0

摘要

对pastinacea Magydaris种子的甲醇提取物进行植物化学研究,得到了两种未描述的苯并呋喃苷,furromagydarins A-B(1,2),以及三种已知的香豆素。新分离物的结构经过广泛的1D和2D NMR实验以及HR ms鉴定,化合物1能够抑制促炎刺激脂多糖刺激下RAW264.7巨噬细胞中COX-2的表达。RT-qPCR和荧光素酶报告基因检测表明,化合物1在转录水平上降低COX-2的表达。进一步的研究表明,化合物1能够抑制lps诱导的p38MAPK、JNK和C/EBPβ磷酸化,从而导致RAW264.7巨噬细胞中COX-2的下调。
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Suppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea.

The phytochemical investigation of the methanol extract of the seeds of Magydaris pastinacea afforded two undescribed benzofuran glycosides, furomagydarins A-B (1, 2), together with three known coumarins. The structures of the new isolates were elucidated after extensive 1D and 2D NMR experiments as well as HR MS. Compound 1 was able to inhibit the COX-2 expression in RAW264.7 macrophages exposed to lipopolysaccharide, a pro-inflammatory stimulus. RT-qPCR and luciferase reporter assays suggested that compound 1 reduces COX-2 expression at the transcriptional level. Further studies highlighted the capability of compound 1 to suppress the LPS-induced p38MAPK, JNK, and C/EBPβ phosphorylation, leading to COX-2 down-regulation in RAW264.7 macrophages.

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来源期刊
CiteScore
10.30
自引率
10.70%
发文量
195
审稿时长
4-8 weeks
期刊介绍: Journal of Enzyme Inhibition and Medicinal Chemistry publishes open access research on enzyme inhibitors, inhibitory processes, and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents. Journal of Enzyme Inhibition and Medicinal Chemistry aims to provide an international and interdisciplinary platform for the latest findings in enzyme inhibition research. The journal’s focus includes current developments in: Enzymology; Cell biology; Chemical biology; Microbiology; Physiology; Pharmacology leading to drug design; Molecular recognition processes; Distribution and metabolism of biologically active compounds.
期刊最新文献
Evaluation of N-alkyl isatins and indoles as acetylcholinesterase and butyrylcholinesterase inhibitors. Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation. Novel dual-targeting inhibitors of NSD2 and HDAC2 for the treatment of liver cancer: structure-based virtual screening, molecular dynamics simulation, and in vitro and in vivo biological activity evaluations. Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach. Suppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea.
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