Chen Hongwei, Lin Jun, Zhu Sisi, Zeng Kewu, Tu Pengfei, Jiang Yong
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
Phytochemistry. 2022 Nov;203:113369. doi: 10.1016/j.phytochem.2022.113369. Epub 2022 Aug 13.
Seven undescribed compounds, including four acridones, two coumarins, and a phenylpropanoid, together with 13 known acridone analogues were isolated from the ethanolic extract of the stems and leaves of Glycosmis ovoidea Pierre. Their structures were elucidated on the basis of comprehensive analysis of 1D and 2D NMR and HRESIMS spectroscopic data, and the absolute configurations were assigned by comparison of the experimental and calculated ECD data. Five compounds showed moderate inhibitory effects on nitric oxide production stimulated by lipopolysaccharide in BV-2 microglial cells with IC values in the range of 18.30-30.84 μM, and three compounds showed potent inhibition on 5-lipoxygenase (5-LOX) with IC values in the range of 2.08-10.26 μM. The possible binding sites of the active compounds with 5-LOX were further performed by molecular docking.
从卵叶山小橘（Glycosmis ovoidea Pierre）的茎叶乙醇提取物中分离得到7个未描述的化合物，包括4个吖啶酮、2个香豆素和1个苯丙素，以及13个已知的吖啶酮类似物。通过对一维和二维核磁共振以及高分辨电喷雾电离质谱光谱数据的综合分析阐明了它们的结构，并通过比较实验和计算的电子圆二色光谱数据确定了绝对构型。5个化合物对脂多糖刺激BV-2小胶质细胞产生一氧化氮具有中等抑制作用，半数抑制浓度（IC）值在18.30至30.84 μM范围内，3个化合物对5-脂氧合酶（5-LOX）具有强效抑制作用，IC值在2.08至10.26 μM范围内。通过分子对接进一步研究了活性化合物与5-LOX的可能结合位点。
