Anti-HIV-1 activity of phlorotannin derivative 8,4‴-dieckol from Korean brown alga Ecklonia cava

Biosci Biotechnol Biochem. 2014;78(7):1151-8. doi: 10.1080/09168451.2014.923282. Epub 2014 Jun 12.

Abstract

8,4‴-dieckol is a natural product which has been isolated from brown alga, Ecklonia cava. This polyphenolic compound is a phlorotannin derivative with a broad range of bioactivities. Its inhibitory activity on human immunodeficiency virus type-1 (HIV-1) was tested and the results indicated that 8,4‴-dieckol inhibited HIV-1 induced syncytia formation, lytic effects, and viral p24 antigen production at noncytotoxic concentrations. Furthermore, it was found that 8,4‴-dieckol selectively inhibited the activity of HIV-1 reverse trancriptase (RT) enzyme with 91% inhibition ratio at the concentration of 50 μM. HIV-1 entry was also inhibited by 8,4‴-dieckol. According to data from this study, 8,4‴-dieckol is an effective compound against HIV-1 with high potential for further studies. These results suggest that it might be used as a drug candidate for the development of new generation therapeutic agents, although further studies on the mechanism of inhibition should be addressed.

Keywords: 8,4‴-dieckol; Ecklonia cava; HIV-1 RT inhibition; phlorotannin; syncytia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology*
  • Benzofurans / chemistry*
  • Benzofurans / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Cytopathogenic Effect, Viral / drug effects
  • Giant Cells / drug effects
  • HIV Core Protein p24 / biosynthesis
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • HIV-1 / metabolism
  • HIV-1 / physiology
  • Humans
  • Phaeophyta / chemistry*
  • T-Lymphocytes / cytology
  • T-Lymphocytes / drug effects
  • Tannins / chemistry*
  • Virus Internalization / drug effects

Substances

  • Anti-HIV Agents
  • Benzofurans
  • HIV Core Protein p24
  • Tannins
  • dieckol
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase