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    • 1. 发明申请
    • Anti-inflammatory and cure for ageing, Alzheimer's disease on phloroglucinol derivatives
    • 消炎和治愈老化,阿尔茨海默病对间苯三酚衍生物
    • US20060205808A1
    • 2006-09-14
    • US11078194
    • 2005-03-10
    • Chun-Nan LinJih-Pyang WangJing-Ru Weng
    • Chun-Nan LinJih-Pyang WangJing-Ru Weng
    • A61K31/343C07C49/105C07D307/92A61K31/12
    • C07D307/92C07C49/743C07D307/80
    • The fresh seeds obtained from the fresh fruits of Garcinia subelliptica, were extracted with chloroform at room temperature. The CHCl3 extract was concentrated under reduced pressure to afford a brown residue. This residue was subjected to column chromatography (silica gel) and eluted with appropriate solvent system to give two phloroglucinol derivatives (Compounds 1 and 4). Compound 1 exhibited potent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils stimulated with formyl-Met-Leu-Phe(fMLP)/cyto-chalasin B (CB). Compound 1 also exhibited potent inhibitory effect on the superoxide anion generation in rat neutrophils stimulated with fMLP/CB. Compound 4 exhibited potent inhibitory effect on NO production in lipopolysaccharide (LPS)/interferon-γ (IFN-γ)-activation in N9 cells. These Compounds may be developed as anti-inflammatory, anti-cancer agent, cure for ageing, and Alzheimer's disease treatment drugs.
    • 从藤黄新鲜果实中获得的新鲜种子在室温下用氯仿萃取。 将CHCl 3萃取物在减压下浓缩,得到棕色残余物。 将该残余物进行柱色谱法(硅胶),并用合适的溶剂系统洗脱,得到两种间苯三酚衍生物(化合物1和4)。 化合物1对用甲酰-Mly-Leu-Phe(fMLP)/细胞色素B(CB)刺激的大鼠嗜中性粒细胞释放β-葡糖苷酸酶和溶菌酶具有有效的抑制作用。 化合物1还对用fMLP / CB刺激的大鼠嗜中性粒细胞中的超氧阴离子产生表现出有效的抑制作用。 化合物4对N9细胞中脂多糖(LPS)/干扰素-γ(IFN-γ)活化的NO产生表现出有效的抑制作用。 这些化合物可以被开发为抗炎,抗癌剂,治愈老化和阿尔茨海默病治疗药物。