Wu Ming-Jiuan, Weng Ching-Yi, Ding Hsiou-Yu, Wu Pei-Jong
Department of Biotechnology, Chia-Nan University of Pharmacy and Science, Tainan 717, Taiwan.
Life Sci. 2005 Jan 21;76(10):1135-46. doi: 10.1016/j.lfs.2004.08.017.
Glossogyne tenuifolia (Hsiang-Ju) is a traditional antipyretic and hepatoprotective herb used in Chinese medicine. The aim of this research is to investigate the pharmacological activities and potent components of the ethanol extract of Glossogyne tenuifolia (GT) in human primary cells and cell line. We found that GT (0.1 approximately 0.25 mg/ml) exerted dose-dependent inhibitions on the release of TNF-alpha and IL-6 in LPS-activated human whole blood and peripheral blood mononuclear cells (PBMC), and IFN-gamma in PHA-stimulated human whole blood. The lack of cytotoxicity indicated that the inhibitory effects of GT on cytokine production were not due to cell death. Luteolin, the deglycosylated derivative of one of the major compositions, luteolin-7-glucoside, exerted inhibitory effects on TNF-alpha, IL-6 and IFN-gamma production in activated human whole blood with estimated IC(50)s of 42.73 microM, 44.86 microM and 3.34 microM, respectively. Furthermore, GT had potent anti-hepatitis B virus (HBV) effects on the human hepatocellular carcinoma cell line, PLC/PRF/5. GT exhibited a dose-dependent inhibition on the release of hepatitis B surface antigen (HBsAg) by repressing the expression of HBsAg with IC(50) of 0.093 mg/ml. We concluded that GT exerted combinatorial anti-inflammatory and antiviral effects, and the multiple actions may underlie its traditional hepatoprotective function.
卤地菊是一种用于中药的传统退烧药和保肝草药。本研究旨在探讨卤地菊乙醇提取物(GT)在人原代细胞和细胞系中的药理活性及有效成分。我们发现,GT(0.1至约0.25mg/ml)对脂多糖激活的人全血和外周血单核细胞(PBMC)中肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)的释放以及对PHA刺激的人全血中干扰素-γ(IFN-γ)的释放具有剂量依赖性抑制作用。缺乏细胞毒性表明GT对细胞因子产生的抑制作用并非由于细胞死亡。木犀草素是主要成分之一木犀草素-7-葡萄糖苷的去糖基化衍生物,对激活的人全血中TNF-α、IL-6和IFN-γ的产生具有抑制作用,估计半数抑制浓度(IC50)分别为42.73μM、44.86μM和3.34μM。此外,GT对人肝癌细胞系PLC/PRF/5具有强大的抗乙型肝炎病毒(HBV)作用。GT通过抑制乙肝表面抗原(HBsAg)的表达对其释放表现出剂量依赖性抑制作用,IC50为0.093mg/ml。我们得出结论,GT发挥了抗炎和抗病毒的联合作用,这些多种作用可能是其传统保肝功能的基础。