Iijima K, Kiyohara H, Tanaka M, Matsumoto T, Cyong J C, Yamada H
Oriental Medicine Research Center of the Kitasato Institute, Tokyo, Japan.
Planta Med. 1995 Feb;61(1):50-3. doi: 10.1055/s-2006-957998.
The survival rate for acute hepatic failure induced by Propionibacterium acnes and lipopolysaccharide (LPS) was increased when a hot water extract from the flowers of Inula britannica L. subsp. japonica Kitam. was injected into the experimental hepatitis mice, and anti-hepatitis substances could be extracted with CHCl3. The CHCl3 extract from I.britannica was fractionated and anti-hepatitis fractions IB-3-2 and IB-3-3 were obtained. IB-3-3 had the most potent anti-hepatitis activity among the fractions but further purification of the active compound was not achieved because of the low yield. IB-3-2 contained only one substance which was identified to be taraxasteryl acetate by 1H- and 13C-NMR and MS. Taraxasteryl acetate showed potent preventive activity against acute hepatic failure induced by P.acnes and LPS in a dose-dependent manner, however deacetylation and modification of the olefinic bonds significantly decreased the anti-hepatitis activity of taraxasteryl acetate. Taraxasteryl acetate also inhibited the increment of plasma transaminase on acute hepatic failure induced by carbon tetrachloride (CCl4) or D-galactosamine. From a histological study it appeared that degeneration and necrosis, which were observed in the liver from CCl4 mice, were not found in the liver cells from taraxasteryl acetate treated mice. These results indicates that taraxasteryl acetate shows preventive effects on experimental hepatitis caused by either immunologically induced injuries or hepatotoxic chemicals.
将旋覆花（Inula britannica L. subsp. japonica Kitam.）花的热水提取物注射到实验性肝炎小鼠体内时，痤疮丙酸杆菌和脂多糖（LPS）诱导的急性肝衰竭的存活率会提高，并且可以用CHCl₃提取抗肝炎物质。对旋覆花的CHCl₃提取物进行了分级分离，得到了抗肝炎级分IB - 3 - 2和IB - 3 - 3。在这些级分中，IB - 3 - 3具有最强的抗肝炎活性，但由于产率低，活性化合物的进一步纯化未成功。IB - 3 - 2仅含有一种物质，通过¹H - 和¹³C - NMR以及MS鉴定为蒲公英赛醇乙酸酯。蒲公英赛醇乙酸酯对痤疮丙酸杆菌和LPS诱导的急性肝衰竭具有剂量依赖性的显著预防活性，然而脱乙酰化和烯烃键的修饰显著降低了蒲公英赛醇乙酸酯的抗肝炎活性。蒲公英赛醇乙酸酯还抑制了四氯化碳（CCl₄）或D - 半乳糖胺诱导的急性肝衰竭时血浆转氨酶的升高。从组织学研究来看，在CCl₄处理小鼠的肝脏中观察到的变性和坏死，在蒲公英赛醇乙酸酯处理小鼠的肝细胞中未发现。这些结果表明，蒲公英赛醇乙酸酯对免疫诱导损伤或肝毒性化学物质引起的实验性肝炎具有预防作用。
