School of Chinese Medicine
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).
Justicia gendarussa, Acanthaceae, Plant natural products, Arylnaphthalide lignans glycosides, Justiprocumins, Antiviral activity, Anti-HIV, NRTI- and NNRTI-resistant HIV-1 variants
Source Publication Title
© 2017 Elsevier Ltd. All rights reserved.
This project was supported by the Research Grants Council of the Hong Kong Special Administrative Region, China (Project No. HKBU 262912), the Health and Medical Research Fund (12132161) of the Food and Health Bureau, Hong Kong SAR, Faculty Research Grants, Hong Kong Baptist University (FRG2/11-12/134 and FRG2/14-15/047), NIH Grants 3U01TW001015-10S1 and 2U01TW001015-11A1, administered by the Fogarty International Center as part of an International Cooperative Biodiversity Groups (ICBG) program, through funds from NIH, NSF, and Foreign Agricultural Service of the USDA, and Mr. Kwok Yat Wai and Madam Kwok Chung Bo Fun Graduate School Development Fund.
Link to Publisher's Edition
Zhang, H., Rumschlag-Booms, E., Guan, Y., Liu, K., Wang, D., Li, W., Nguyen, V., Cuong, N., Soejarto, D., Fong, H., & Rong, L. (2017). Anti-HIV diphyllin glycosides from Justicia gendarussa. Phytochemistry, 136, 94-100. https://doi.org/10.1016/j.phytochem.2017.01.005
Additional FilesJA-5193-29186_suppl.pdf (1977 kB)