Lee Sung-Jin, Lee Hak-Kyo, Jung Min-Kyung, Mar Woongchon
Gyeonggi Regional Research Center, Hankyong National University, Gyeonggi, Korea.
Biol Pharm Bull. 2006 Oct;29(10):2131-4. doi: 10.1248/bpb.29.2131.
This study examined the antiviral activity of the root of Paeonia lactiflora PALL. Among the solvent fractions of the crude drug, the ethyl acetate fraction showed anti-hepatitis B virus (HBV) activity (IC50, 8.1 microg/ml) in an HBV-producing HepG2.2.15 cell culture system. The active anti-HBV principle was isolated and identified as 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) from the crude drug by activity-guided fractionation. PGG isolated from P. lactiflora was examined for the inhibition of HBV multiplication by measurement of HBV DNA and hepatitis B surface antigen (HBsAg) levels in the extracellular medium of HepG2.2.15 cells after 8-d treatment. PGG decreased the level of extracellular HBV (IC50, 1.0 microg/ml) in a dose-dependent manner. PGG also reduced the HBsAg level by 25% at a concentration of 4 microg/ml. The gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity. These results suggest that PGG could be a candidate for developing an anti-HBV agent.
本研究考察了芍药根的抗病毒活性。在该生药的溶剂提取物中，乙酸乙酯提取物在产生乙肝病毒（HBV）的HepG2.2.15细胞培养系统中显示出抗乙肝病毒活性（IC50，8.1微克/毫升）。通过活性导向分级分离法从该生药中分离并鉴定出具有抗HBV活性的主要成分是1,2,3,4,6 - 五 - O - 没食子酰 - β - D - 葡萄糖（PGG）。对从芍药中分离得到的PGG进行检测，通过测定经8天处理后HepG2.2.15细胞外培养基中的HBV DNA和乙肝表面抗原（HBsAg）水平，来考察其对HBV增殖的抑制作用。PGG以剂量依赖方式降低细胞外HBV水平（IC50，1.0微克/毫升）。在浓度为4微克/毫升时，PGG还可使HBsAg水平降低25%。PGG的没食子酸结构可能在抗HBV活性抑制中起关键作用。这些结果表明，PGG可能是开发抗HBV药物的候选物质。
