CHEN, JIH JUNG,陈日荣,陳日榮,SHIEH, PO CHUEN,谢博铨,謝博銓,CHEN, CHIN YEN,陈晋彦,陳晉彥,HWANG, TSONG LONG,黄聪龙,黃聰龍
申请号：
TW101125077
公开号：
TW201402112A
申请日:
2012.07.12
申请国别(地区):
TW
年份:
2014
代理人:
摘要：
Fraxinus chinensis are widely used in traditional Chinese medicine for reducing inflammation, stopping cough, improving gastrointestinal disease, and as a diuretic. The phytochemical investigation of stem bark of F. chinensis has led to the isolation of three new secoiridoid derivatives, (8E)-4"-O-methylligstroside (1), (8E)-4"-O-methyldemethylligstroside (2), and 3",4"-di-O-methyl- demethyloleuropein (3), along with 12 known compounds. The structures of all isolates were determined through spectral analyses (including 2D-NMR: NOESY, COSY, HMBC, HSQC...etc) and comparison of their physical and spectral data with literatures. The anti-inflammatory effects of compounds from F. chinensis were evaluated by suppressing formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B (fMLP/ CB)-induced superoxide radical anion (O2.-) generation and elastase release by human neutrophils. The result of anti-inflammatory test showed that (8E)-4"-O-methylligstroside (1), (8E)-4"-O-methyl-demethylligstroside (2), 3",4"-di-O-methyldemethyloleuropein (3), oleuropein (5), aesculetin (7), isoscopoletin (9), aesculetin dimethyl ester (10), fraxetin (12), tyrosol (13), 4-hydroxyphenethyl acetate (14), and (+)-pinoresinol (15) exhibited inhibition (IC50 values 7.65 g/mL) of superoxide anion generation by human neutrophils in response to formyl-L-methionyl-L-leuckyl-L-phenylalanine/cytochalasin B (fMLP/ CB).In addition, (8E)-4"-O-methylligstroside (1), aesculetin (7), isoscopoletin (9), fraxetin (12), tyrosol (13), and 4-hydroxyphenethyl acetate (14) inhibited fMLP/CB-induced elastase release with IC50 values 3.23 g/mL.白蠟樹為常用中藥材,臨床用於消炎、咳嗽、利尿及改善胃腸疾病等。本發明係研究由白蠟樹樹皮分離出3種新secoiridoid化合物:(8E)-4"-O-methylligstroside(1),(8E)-4"-O-methyldimethylligstroside(2)及3",4"-di-O-methyldemethyloleuropein(3),以及12個已知化合物(4-15)。這些化合物經各種實驗數據分析(包括2D-NMR:NOESY,COSY, HMBC,HSQC...等)以及比對相關文獻上之數據,而確認其結構。上述分離之化合物,藉由抑制formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B(fMLP/CB)所誘導人類嗜中性白血球產生超氧陰離子(O2.-)及彈性蛋白酶(elast
