Anti-hepatitis B virus activities of Geranium carolinianum L. extracts and identification of the active components
Anti-hepatitis B virus activities of Geranium carolinianum L. extracts and identification of the active components
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DOI：
10.1248/bpb.31.743
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发表时间：
2008-04-01
影响因子：
2
通讯作者：
Zhou, Pei
中科院分区：
文献类型：
--
作者：
Li, Jiyang;Huang, Hai;Zhou, Pei
采用不同的有机溶剂对国产天竺葵（Geranium carolinianum L.）乙醇提取物进行了顺序提取。测定其抗乙型肝炎病毒（HBV）活性。发现乙酸乙酯部分含有最高水平的抗hbv活性。为了鉴定其有效成分，采用柱层析法对乙酸乙酯部分进行进一步分离。鉴定出鞣花酸、天竺葵苷、槲皮苷、金丝桃苷、毛素、槲皮素、山奈酚等7个化合物，并通过NMR对其结构进行了表征。卡罗来纳草中含有抗HBV化合物天竺葵苷、鞣花酸和金丝桃苷，可能是这种民间药物治疗HBV感染有效的原因。在无细胞毒浓度为200 μ g/ml时，天竺葵素对乙型肝炎表面抗原（HBsAg）和乙型肝炎e抗原（HBeAg）的抑制作用分别大于85.8%和63.7%。在相同浓度下，天竺香蛋白对HBsAg和HBeAg分泌的抑制作用分别高于阳性对照拉米夫定，分别为33.5%和32.2%。由于HBeAg参与了HBV感染过程中的免疫耐受，新发现的抗HBV复方天竺葵蛋白可能是克服HBV感染个体免疫耐受的候选药物。本文首次报道了从天竺葵中提取的活性物质天竺葵苷和金丝桃苷抗乙肝病毒的作用。
The ethanol extract of Geranium carolinianum L., a domestic plant grown in China, was subjected to sequential extractions with different organic solvents. The extracts were assayed for anti-hepatitis B virus (HBV) activities. The ethyl acetate fraction was found to contain the highest level of anti-HBV activity. In order to identify the active ingredients, the ethyl acetate fraction was further fractionated by column chromatography. Seven compounds were identified including ellagic acid, geraniin, quercitrin, hyperin, hirsutrin, quercetin, and kaempferol, whose structures were determined by NMR. The presence of the anti-HBV compounds geraniin, ellagic acid and hyperin in G. carolinianum L. may account for the effectiveness of this folk medicine in the treatment of HBV infections. Geraniin inhibited hepatitis B surface antigen (HBsAg) and hepatitis B e antigen (HBeAg) secretion by more than 85.8% and 63.7%, respectively, at the non-cytotoxic concentration of 200 mu g/ml. The inhibitions of HBsAg and HBeAg secretion by geraniin were higher than the inhibition by the positive control Lamivudine, 33.5% and 32.2% respectively, at the same concentration. Since HBeAg is involved in immune tolerance during HBV infection, the newly identified anti-HBV compound geraniin might be a candidate agent to overcome the immune tolerance in HBV-infected individuals. This is the first report of the anti-HBV effects of geraniin and hyperin, the active substances derived from G. carolinianum L.