School of Pharmacy, Guangdong Medical University, 523808 Dongguan, China.
School of Chemistry, Sun Yat-Sen University, 510275 Guangzhou, China.
Molecules. 2020 Jan 29;25(3):576. doi: 10.3390/molecules25030576.
Twelve 1, 4-naphthoquinone derivatives, including two new ( and ) and 10 known (-), were obtained from endophytic fungus sp. SK-S009 isolated from the fruit of . All structures were identified through extensive analysis of the nuclear magnetic resonance (NMR), mass spectrometry (MS) and circular dichroism (CD), as well as by comparison with literature data. These compounds significantly inhibited the lipopolysaccharide (LPS)-induced nitric oxide (NO) production in the murine macrophage cell line (RAW 264.7 cells). The half maximal inhibitory concentration (IC) values, except for compound 2, were lower than that of indomethacin (26.3 μM). Compound inhibited the LPS-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) mRNA expressions in RAW 264.7 macrophages. Additionally, compound reduced the mRNA levels of pro-inflammatory factors interleukin (IL)1β, IL-6, and tumor necrosis factor (TNF)-α. The results of this study demonstrated that these 1, 4-naphthoquinone derivatives can inhibit LPS-induced inflammation.
从内生真菌 sp. SK-S009 中分离得到的果实中,获得了 12 种 1,4-萘醌衍生物,包括两种新化合物( 和 )和 10 种已知化合物(-)。通过核磁共振(NMR)、质谱(MS)和圆二色性(CD)的广泛分析以及与文献数据的比较,确定了所有结构。这些化合物显著抑制脂多糖(LPS)诱导的小鼠巨噬细胞系(RAW 264.7 细胞)中一氧化氮(NO)的产生。除化合物 2 外,半数最大抑制浓度(IC)值均低于吲哚美辛(26.3 μM)。化合物 抑制 LPS 诱导的 RAW 264.7 巨噬细胞中诱导型一氧化氮合酶(iNOS)和环氧化酶-2(COX-2)mRNA 的表达。此外,化合物 降低了促炎因子白细胞介素(IL)1β、IL-6 和肿瘤坏死因子(TNF)-α 的 mRNA 水平。本研究结果表明,这些 1,4-萘醌衍生物可抑制 LPS 诱导的炎症。