酰基间苯三酚衍生物具有抗炎作用，可抑制 LPS 诱导的 RAW264.7 巨噬细胞。
Acylphloroglucinol Derivatives from with Anti-Inflammatory Effect in LPS-Induced RAW264.7 Macrophages.
机构信息
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Institute of Traditional Medicine, National Yang-Ming University, Taipei 112, Taiwan.
出版信息
Molecules. 2018 Oct 10;23(10):2587. doi: 10.3390/molecules23102587.
Two new acylphloroglucinol derivatives, 13,14-didehydroxygarcicowin C () and 13,14-didehydroxyisoxanthochymol (), have been isolated from the stems of , together with seven known compounds (⁻). The structures of new compounds and were elucidated by MS and extensive 1D/2D NMR spectroscopic analyses. Among the isolates, 13,14-didehydroxy-isoxanthochymol () and sampsonione B () exhibited inhibition against lipopolysaccharide (LPS)-induced NF-κB activation in macrophages at 30 μM with relative luciferase activity values (inhibitory %) of 0.75 ± 0.03 (24 ± 4%) and 0.12 ± 0.03 (88 ± 4%), respectively. Additionally, sampsonione B () reduced LPS-induced nitric oxide (NO) production in murine RAW264.7 macrophages and did not induce cytotoxicity against RAW 264.7 cells after 24 h treatment. Compound is worth further investigation and may be expectantly developed as an anti-inflammatory
从 茎中分离得到了两个新的酰基间苯三酚衍生物，13,14-二去氢高阿朴菲 C () 和 13,14-二去氢异黄腐醇 (), 以及 7 种已知化合物 (⁻)。新化合物 和 的结构通过 MS 和广泛的 1D/2D NMR 光谱分析阐明。在所分离的化合物中，13,14-二去氢异黄腐醇 () 和桑普森酮 B () 在 30 μM 时表现出对脂多糖 (LPS) 诱导的巨噬细胞 NF-κB 激活的抑制作用，相对荧光素酶活性值 (抑制%)分别为 0.75 ± 0.03 (24 ± 4%) 和 0.12 ± 0.03 (88 ± 4%)。此外，桑普森酮 B () 减少了 LPS 诱导的小鼠 RAW264.7 巨噬细胞中一氧化氮 (NO) 的产生，并且在 24 小时处理后对 RAW 264.7 细胞没有诱导细胞毒性。化合物 值得进一步研究，可能有望开发为一种抗炎药。
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