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基于液相色谱-串联质谱引导从……中分离具有抗炎活性的愈创木烷型倍半萜类化合物。

LC-MS/MS-guided separation of guaiacolane-type sesquiterpenes with anti-inflammatory activities from .

作者信息

Li Xinyue, Cai Yanfen, Hu Yunshuang, Miu Limei, Zhang Yanyu, Huang Shiyun, Wei Min, Ma Qing, Liu Zhongqiu, Zhou Hua, Wu Peng

机构信息

Guangdong Provincial Key Laboratory of Translational Cancer Research of Chinese Medicines, Joint International Research Laboratory of Translational Cancer Research of Chinese Medicines, International Institute for Translational Chinese Medicine, School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine Guangzhou 510006 P. R. China

Henan Key Laboratory of Traditional Chinese Medicine Prescription and Syndrome Signaling & Henan International Joint Laboratory of Traditional Chinese Medicine Prescription and Syndrome Signaling, Henan University of Chinese Medicine Zhengzhou 450046 P. R. China.

出版信息

RSC Adv. 2025 Jul 22;15(32):26173-26183. doi: 10.1039/d5ra03586d. eCollection 2025 Jul 21.

Abstract

Four previously undescribed compounds, including three guaiacane-type sesquiterpenoids (1-3) and one oleanane-type triterpenoid (4), along with seven known sesquiterpenoids, were isolated from the aerial parts of using LC-MS/MS-guided fractionation. Structures were elucidated by IR, UV, HR-ESI-MS, and 1D/2D NMR analyses, and their absolute configurations were determined by ECD calculations. The anti-inflammatory activity was evaluated in LPS-stimulated RAW264.7 cells with NF-κB translocation by high-content imaging (HCI). Compound 2 reduced NF-κB translocation (IC = 9.70 μM) without cytotoxicity at 20 μM. Compounds 8 and 9 showed potent activity (IC = 2.04 and 1.21 μM, respectively) and no cytotoxicity at 6.25 μM.

摘要

通过液相色谱-串联质谱(LC-MS/MS)引导的分级分离,从[植物名称未给出]的地上部分分离出四种先前未描述的化合物,包括三种愈创木烷型倍半萜(1 - 3)和一种齐墩果烷型三萜(4),以及七种已知的倍半萜。通过红外光谱(IR)、紫外光谱(UV)、高分辨电喷雾电离质谱(HR-ESI-MS)和一维/二维核磁共振(1D/2D NMR)分析阐明了其结构,并通过电子圆二色光谱(ECD)计算确定了它们的绝对构型。通过高内涵成像(HCI)在脂多糖(LPS)刺激的RAW264.7细胞中评估了其抗炎活性,其中核因子κB(NF-κB)发生易位。化合物2在20 μM时无细胞毒性,可减少NF-κB易位(半数抑制浓度[IC] = 9.70 μM)。化合物8和9显示出强效活性(IC分别为2.04和1.21 μM),在6.25 μM时无细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b74a/12282369/76efa93da05c/d5ra03586d-f1.jpg

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