Anti-HIV diphyllin glycosides from Justicia gendarussa

Hong Jie Zhang*, Emily Rumschlag-Booms, Yi Fu Guan, Kang Lun Liu, Dong Ying Wang, Wan Fei Li, Van Hung Nguyen, Nguyen Manh Cuong, Djaja Doel Soejarto, Harry H.S. Fong, Lijun Rong

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

49 Citations (Scopus)
49 Downloads (Pure)

Abstract

In a search for new anti-HIV active leads from over several thousands of plant extracts, we have identified a potent plant lead. The active plant is determined as Justicia gendarussa (Acanthaceae), a medicinal plant that has been used for the treatment of injury, arthritis and rheumatism in Asia including China. Our bioassay-guided fractionation of the methanol extract of the stems and barks of the plant led to the isolation of two anti-HIV compounds, justiprocumins A and B. The compounds are identified as new arylnaphthalide lignans (ANL) glycosides. We further determined that the ANL glycosides are the chemical constituents that contribute to the anti-HIV activity of this plant. Justiprocumin B displayed potent activity against a broad spectrum of HIV strains with IC50 values in the range of 15–21 nM (AZT, IC50 77–95 nM). The compound also displayed potent inhibitory activity against the NRTI (nucleoside reverse transcriptase inhibitor)-resistant isolate (HIV-11617-1) of the analogue (AZT) as well as the NNRTI (non-nucleoside reverse transcriptase inhibitor)-resistant isolate (HIV-1N119) of the analogue (nevaripine).

Original languageEnglish
Pages (from-to)94-100
Number of pages7
JournalPhytochemistry
Volume136
DOIs
Publication statusPublished - 1 Apr 2017

Scopus Subject Areas

  • Biochemistry
  • Molecular Biology
  • Plant Science
  • Horticulture

User-Defined Keywords

  • Acanthaceae
  • Anti-HIV
  • Antiviral activity
  • Arylnaphthalide lignans glycosides
  • Justicia gendarussa
  • Justiprocumins
  • NRTI- and NNRTI-resistant HIV-1 variants
  • Plant natural products

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