Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Zhunan, Taiwan, Republic of China.
J Nat Prod. 2011 Apr 25;74(4):580-4. doi: 10.1021/np100578u. Epub 2011 Mar 10.
Diosgenin (3β-hydroxy-5-spirostene, 1), a plant-derived sapogenin, is used as a dietary supplement. However, the biological effects of 1 related to viral replication remain unexplored. In this study, the effects of 1 on hepatitis C virus (HCV) replication were evaluated. Based on a reporter-based HCV subgenomic replicon system, 1 was found to inhibit HCV replication at low micromolar concentrations. The EC(50) (concentration at which 50% of HCV replication is inhibited) of 1 was 3.8 μM. No cellular toxicity was observed at this concentration. Diosgenin (1) also significantly reduced the levels of viral RNA and viral proteins as evaluated by quantitative real-time reverse transcriptase PCR and Western blot analysis, respectively. In addition, in an alternative HCV antiviral system more closely aligned to all steps involved in the HCV infection and life cycle, 1 totally abolished HCV replication at 20 μM. Moreover, 1 reduced the phosphorylation of signal transducer and activator of transcription 3. A combination of 1 and interferon-α exerted an additive effect on the resultant anti-HCV activity.
薯蓣皂苷元（3β-羟基-5-螺甾烯，1），一种植物来源的甾体皂苷元，被用作膳食补充剂。然而，1 与病毒复制相关的生物学效应仍未被探索。在这项研究中，评估了 1 对丙型肝炎病毒（HCV）复制的影响。基于基于报告基因的 HCV 亚基因组复制子系统，发现 1 在低微摩尔浓度下抑制 HCV 复制。1 的 EC50（抑制 50% HCV 复制的浓度）为 3.8 μM。在该浓度下未观察到细胞毒性。薯蓣皂苷元（1）也显著降低了病毒 RNA 和病毒蛋白的水平，分别通过定量实时逆转录聚合酶链反应和 Western blot 分析评估。此外，在更接近 HCV 感染和生命周期中涉及的所有步骤的替代 HCV 抗病毒系统中，1 在 20 μM 时完全抑制了 HCV 复制。此外，1 降低了信号转导和转录激活因子 3 的磷酸化。1 和干扰素-α的联合使用对最终的抗 HCV 活性具有相加作用。
