Division of Clinical and Molecular Hepatology, Department of Human Pathology, University Hospital of Messina, Via Consolare Valeria, 98125, Messina, Italy.
Department of Clinical and Experimental Medicine, Section of Pharmacology, University of Messina, Via Consolare Valeria, Torre Biologica 5th floor, c/o AOU Policlinico G. Martino, Via C. Valeria Gazzi, 98125, Messina, Italy.
Inflamm Res. 2018 Jan;67(1):89-103. doi: 10.1007/s00011-017-1099-2. Epub 2017 Oct 10.
Flavocoxid is a proprietary blend of two flavonoids, baicalin and catechin, and recent evidence has shown that bioflavonoids may exert antiviral activities. The potential antiviral activity of Flavocoxid against hepatitis B virus (HBV) was evaluated. Additionally, it was investigated if Flavocoxid used in combination with Entecavir could potentiate its anti-HBV activity.
Hepatoma cells replicating HBV were treated with Flavocoxid, or Entecavir alone or in combination for up to 5 days. Viral replicative intermediates, transcripts, and cccDNA levels were evaluated in HBV-replicating cells by real-time PCR, Southern and Northern blotting. Expression profiling was performed using TaqMan low-density arrays.
Flavocoxid treatment induced a reduction of HBV replicative intermediates, the amount of transcripts, and HBsAg levels. Flavocoxid and Entecavir combination therapy further decreased the amount of HBV replicative intermediates, compared to Flavocoxid alone. Importantly, Flavocoxid alone or in combination with Entecavir also induced a reduction of cccDNA. Gene-expression analysis showed that Flavocoxid activates type I IFNs-signaling and dampens the HBV-induced inflammatory response.
Flavocoxid inhibits HBV replication by targeting multiple steps of viral life cycle. These results indicate that the antiviral activity of Entecavir is potentiated by Flavocoxid, suggesting that this medical food might be considered as an adjuvant for anti-HBV therapy.
Flavocoxid 是两种类黄酮(黄芩苷和儿茶素)的专利混合物,最近的证据表明生物类黄酮可能具有抗病毒活性。评估了 Flavocoxid 对乙型肝炎病毒(HBV)的潜在抗病毒活性。此外,还研究了 Flavocoxid 与恩替卡韦联合使用是否能增强其抗 HBV 活性。
用 Flavocoxid、恩替卡韦或两者联合处理复制 HBV 的肝癌细胞,时间长达 5 天。通过实时 PCR、Southern 和 Northern 印迹法评估 HBV 复制细胞中病毒复制中间体、转录物和cccDNA 水平。使用 TaqMan 低密度阵列进行表达谱分析。
Flavocoxid 处理诱导 HBV 复制中间体、转录物数量和 HBsAg 水平降低。Flavocoxid 和恩替卡韦联合治疗与 Flavocoxid 单药治疗相比,进一步降低了 HBV 复制中间体的数量。重要的是,Flavocoxid 单独或与恩替卡韦联合使用也可降低 cccDNA 的含量。基因表达分析表明,Flavocoxid 通过靶向病毒生命周期的多个步骤来抑制 HBV 复制。这些结果表明,Flavocoxid 增强了恩替卡韦的抗病毒活性,表明这种医疗食品可能被考虑作为抗 HBV 治疗的辅助药物。