Inhibitory effects of caffeic acid phenethyl ester derivatives on replication of hepatitis C virus

PLoS One. 2013 Dec 17;8(12):e82299. doi: 10.1371/journal.pone.0082299. eCollection 2013.

Abstract

Caffeic acid phenethyl ester (CAPE) has been reported as a multifunctional compound. In this report, we tested the effect of CAPE and its derivatives on hepatitis C virus (HCV) replication in order to develop an effective anti-HCV compound. CAPE and CAPE derivatives exhibited anti-HCV activity against an HCV replicon cell line of genotype 1b with EC50 values in a range from 1.0 to 109.6 µM. Analyses of chemical structure and antiviral activity suggested that the length of the n-alkyl side chain and catechol moiety are responsible for the anti-HCV activity of these compounds. Caffeic acid n-octyl ester exhibited the highest anti-HCV activity among the tested derivatives with an EC50 value of 1.0 µM and an SI value of 63.1 by using the replicon cell line derived from genotype 1b strain Con1. Treatment with caffeic acid n-octyl ester inhibited HCV replication of genotype 2a at a similar level to that of genotype 1b irrespectively of interferon signaling. Caffeic acid n-octyl ester could synergistically enhance the anti-HCV activities of interferon-alpha 2b, daclatasvir, and VX-222, but neither telaprevir nor danoprevir. These results suggest that caffeic acid n-octyl ester is a potential candidate for novel anti-HCV chemotherapy drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / pharmacology*
  • Caffeic Acids / pharmacology*
  • Hepacivirus / genetics
  • Hepacivirus / physiology*
  • Phenylethyl Alcohol / analogs & derivatives*
  • Phenylethyl Alcohol / pharmacology
  • RNA, Viral / genetics
  • Structure-Activity Relationship
  • Virus Replication / drug effects*

Substances

  • Antiviral Agents
  • Caffeic Acids
  • RNA, Viral
  • caffeic acid phenethyl ester
  • Phenylethyl Alcohol

Grants and funding

This work was supported in part by grants-in-aid from the Ministry of Health, Labor, and Welfare and from the Ministry of Education, Culture, Sports, Science, and Technology of Japan. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.