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Differential in vitro anti-HIV activity of natural lignans.


Z Naturforsch [C]. 1990 Nov-Dec;45(11-12):1215-21. Unique Identifier :

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.

Animal Antiviral Agents/*PHARMACOLOGY Cell Division/DRUG EFFECTS Cell Line Comparative Study DNA Topoisomerase (ATP-Hydrolysing)/METABOLISM Human HIV/*DRUG EFFECTS/PHYSIOLOGY HIV-1/*DRUG EFFECTS/PHYSIOLOGY Leukemia L5178 Lignin/*PHARMACOLOGY Mice Plasmids Structure-Activity Relationship Support, Non-U.S. Gov't Viral Proteins/BIOSYNTHESIS JOURNAL ARTICLE


Information in this article was accurate in September 30, 1991. The state of the art may have changed since the publication date. This material is designed to support, not replace, the relationship that exists between you and your doctor. Always discuss treatment options with a doctor who specializes in treating HIV.