Department of Pharmacy, Zhejiang Provincial Key Laboratory of Biometrology and Inspection & Quarantine, College of Life Sciences, China Jiliang University, Hangzhou 310018, China.
J Ethnopharmacol. 2012 Oct 31;144(1):190-4. doi: 10.1016/j.jep.2012.09.003. Epub 2012 Sep 11.
The aim of this study was to determine the anti-hepatitis B effect of isochlorogenic acid A isolated from Laggera alata (Asteraceae), a traditional Chinese herbal medicine.
The anti-hepatitis B activity of isochlorogenic acid A was evaluated by the D-galactosamine (D-GalN)-induced HL-7702 hepatocyte damage model and the HBV-transfected HepG2.2.15 cells.
Isochlorogenic acid A significantly improved HL-7702 hepatocyte viability and markedly inhibited the productions of HBsAg and HBeAg. The inhibitory rates of isochlorogenic acid A on the HBsAg and HBeAg expressions were 86.9% and 72.9%, respectively. In addition, isochlorogenic acid A declined markedly the content of hepatitis B virus covalently closed circular DNA (HBV cccDNA) and induced significantly the heme oxygenase-1 (HO-1) expression in HepG2.2.15 cells.
Isochlorogenic acid A was verified to possess the potent anti-hepatitis B activity. The anti-HBV target of isochlorogenic acid A is probably associated with blocking the translation step of the HBV replication. Overexpression of HO-1 may contribute to the anti-HBV activity of isochlorogenic acid A by reducing the stability of the HBV core protein and thus blocking the refill of nuclear HBV cccDNA. Additionally, the hepatoprotective effect of isochlorogenic acid A could be achieved by its antioxidative property and induction of HO-1.
本研究旨在确定从传统中药 laggera alata（菊科）中分离出的绿原酸 A 对乙肝的抗病毒作用。
通过 D-半乳糖胺（D-GalN）诱导的 HL-7702 肝细胞损伤模型和 HBV 转染 HepG2.2.15 细胞评估绿原酸 A 的抗乙肝病毒活性。
绿原酸 A 显著提高 HL-7702 肝细胞活力，并显著抑制 HBsAg 和 HBeAg 的产生。绿原酸 A 对 HBsAg 和 HBeAg 表达的抑制率分别为 86.9%和 72.9%。此外，绿原酸 A 显著降低乙型肝炎病毒共价闭合环状 DNA（HBV cccDNA）的含量，并诱导 HepG2.2.15 细胞中血红素加氧酶-1（HO-1）的显著表达。
绿原酸 A 被证实具有较强的抗乙肝病毒活性。绿原酸 A 的抗 HBV 作用靶点可能与阻断 HBV 复制的翻译步骤有关。HO-1 的过表达可能通过降低 HBV 核心蛋白的稳定性从而阻断核 HBV cccDNA 的再填充，从而有助于绿原酸 A 的抗 HBV 活性。此外，绿原酸 A 的保肝作用可能是通过其抗氧化特性和诱导 HO-1 实现的。
