Choi Jongwon, Shin Kyoung-Min, Park Hee-Juhn, Jung Hyun-Ju, Kim Hyoung Ja, Lee Yong Sup, Rew Jae-Hwan, Lee Kyung-Tae
College of Pharmacy, Kyungsung University, Pusan, Korea.
Planta Med. 2004 Nov;70(11):1027-32. doi: 10.1055/s-2004-832642.
In the present study, syringin, isolated by activity-guided fractionation of the ethyl acetate (EtOAc) extracts of the stem bark of Magnolia sieboldii, and sinapyl alcohol, the hydrolysate of syringin, were evaluated for anti-inflammatory and antinociceptive activities. Sinapyl alcohol (20, 30 mg/kg/day, p. o.) inhibited increased vascular permeability by acetic acid in mice and reduced acute paw edema by carrageenan in rats more so than syringin. When analgesic activity was measured using the acetic acid-induced writhing test and the hot plate test, sinapyl alcohol was much more potent than syringin in a mouse model. In addition, sinapyl alcohol more potently inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E2 (PGE2), and tumor necrosis factor (TNF)-alpha production by macrophages than syringin. Consistent with these observations, the expression levels of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 was reduced by sinapyl alcohol in a concentration-dependent manner. These results suggest that the anti-inflammatory and antinociceptive effects of syringin after oral administration may be attributed to its in vivo transformation to sinapyl alcohol.
在本研究中，通过活性导向分离日本厚朴茎皮的乙酸乙酯（EtOAc）提取物得到紫丁香苷，以及紫丁香苷的水解产物芥子醇，对它们的抗炎和镇痛活性进行了评估。芥子醇（20、30mg/kg/天，口服）比紫丁香苷更能抑制小鼠因乙酸引起的血管通透性增加，并减轻大鼠因角叉菜胶引起的急性爪肿胀。当使用乙酸诱导的扭体试验和热板试验测量镇痛活性时，在小鼠模型中，芥子醇的效力比紫丁香苷强得多。此外，芥子醇比紫丁香苷更有效地抑制巨噬细胞中脂多糖（LPS）诱导的一氧化氮（NO）、前列腺素E2（PGE2）和肿瘤坏死因子（TNF）-α的产生。与这些观察结果一致，芥子醇以浓度依赖性方式降低诱导型一氧化氮合酶（iNOS）和环氧化酶（COX）-2的表达水平。这些结果表明，口服给药后紫丁香苷的抗炎和镇痛作用可能归因于其在体内转化为芥子醇。
