Differential in vitro anti-HIV activity of natural lignans

Z Naturforsch C J Biosci. Nov-Dec 1990;45(11-12):1215-21. doi: 10.1515/znc-1990-11-1222.


Two naturally occurring lignanolides, isolated from the tropical climbing shrub Ipomoea cairica, (-)-arctigenin and (-)-trachelogenin, were found to inhibit strongly replication of human immunodeficiency virus type 1 (HIV-1; strain HTLV-III B) in vitro. At a concentration of 0.5 microM, (-)-arctigenin and (-)-trachelogenin inhibited the expression of HIV-1 proteins p17 and p24 by 80-90% and 60-70%, respectively. The reverse transcriptase activity in the culture fluids was reduced by 80-90% when the cells (HTLV-III B/H9) were cultivated in the presence of 0.5 microM (-)-arctigenin or 1 microM (-)-trachelogenin. At the same concentrations, the formation of syncytia in the HTLV-III B/H9-Jurkat cell system was inhibited by the compounds by more than 80%. A series of other lignan type compounds displayed no anti-HIV activity. Studying the molecular mechanism of action of (-)-arctigenin and (-)-trachelogenin we found that both compounds are efficient inhibitors of the nuclear matrix-associated DNA topoisomerase II activity, particularly of the enzyme from HIV-1-infected cells. Our results suggest that both compounds prevent the increase of topoisomerase II activity, involved in virus replication, after infection of cells with HIV-1.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • Cell Division / drug effects
  • Cell Line
  • DNA Topoisomerases, Type II / metabolism
  • HIV / drug effects*
  • HIV / physiology
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • Humans
  • Leukemia L5178
  • Lignans
  • Lignin / pharmacology*
  • Mice
  • Plasmids
  • Structure-Activity Relationship
  • Viral Proteins / biosynthesis


  • Antiviral Agents
  • Lignans
  • Viral Proteins
  • Lignin
  • DNA Topoisomerases, Type II