Jung Hyun-Ju, Park Hee-Juhn, Kim Ryung-Gue, Shin Kyoung-Min, Ha Joohun, Choi Jong-Won, Kim Hyoung Ja, Lee Yong Sup, Lee Kyung-Tae
Division of Applied Plant Sciences, Sangji University, Woosan-Dong, Wonju, Korea.
Planta Med. 2003 Jul;69(7):610-6. doi: 10.1055/s-2003-41127.
In the present study, liriodendrin isolated by activity-guided fractionation from the ethyl acetate (EtOAc) extracts of the stem bark of Acanthopanax senticosus, was evaluated for anti-inflammatory and antinociceptive activities. Liriodendrin (5, 10 mg/kg/day, p. o.) significantly inhibited the increase of vascular permeability induced by acetic acid in mice and reduced an acute paw edema induced by carrageenan in rats. When the analgesic activity was measured by the acetic acid-induced writhing test and hot plate test, liriodendrin showed a dose-dependent inhibition in animal models. In addition, syringaresinol, the hydrolysate of liriodendrin, more potently inhibited the LPS-induced production of NO, PGE 2 and TNF-alpha production of macrophages than liriodendrin. Consistent with these observations, the expression level of iNOS and COX-2 enzyme was decreased by syringaresinol in a concentration-dependent manner. These results suggest that the anti-inflammatory and antinociceptive effects of liriodendrin after oral administration were attributable to the in vivo transformation to syringaresinol, which may function as the active constituent.
在本研究中，通过活性导向分馏从刺五加茎皮乙酸乙酯提取物中分离得到的鹅掌楸苷，对其抗炎和镇痛活性进行了评估。鹅掌楸苷（5、10毫克/千克/天，口服）显著抑制了乙酸诱导的小鼠血管通透性增加，并减轻了角叉菜胶诱导的大鼠急性足爪水肿。当通过乙酸诱导的扭体试验和热板试验测量镇痛活性时，鹅掌楸苷在动物模型中表现出剂量依赖性抑制作用。此外，鹅掌楸苷的水解产物丁香树脂醇比鹅掌楸苷更有效地抑制脂多糖诱导的巨噬细胞一氧化氮（NO）、前列腺素E2（PGE2）和肿瘤坏死因子-α（TNF-α）的产生。与这些观察结果一致，丁香树脂醇以浓度依赖性方式降低了诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）的表达水平。这些结果表明，鹅掌楸苷口服后的抗炎和镇痛作用归因于其在体内转化为丁香树脂醇，丁香树脂醇可能是其活性成分。
