title: Anti-HIV diphyllin glycosides from Justicia gendarussa.
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 IC50values in the range of 15-21 nM (AZT, IC5077-95 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).
authors.affiliation: School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong Special Administrative Region. Electronic address: zhanghj@hkbu.edu.hk.
authors.forename: Hong-Jie
authors.initials: HJ
authors.lastname: Zhang
authors.affiliation: Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, 835 South Wolcott Avenue, Chicago, IL 60612, USA.
authors.forename: Emily
authors.initials: E
authors.lastname: Rumschlag-Booms
authors.affiliation: School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong Special Administrative Region.
authors.forename: Yi-Fu
authors.initials: YF
authors.lastname: Guan
authors.affiliation: School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong Special Administrative Region.
authors.forename: Kang-Lun
authors.initials: KL
authors.lastname: Liu
authors.affiliation: School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong Special Administrative Region.
authors.forename: Dong-Ying
authors.initials: DY
authors.lastname: Wang
authors.affiliation: School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong Special Administrative Region.
authors.forename: Wan-Fei
authors.initials: WF
authors.lastname: Li
authors.affiliation: Institute of Marine Biochemistry of the Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet road, Cau Giay, Hanoi, Viet Nam.
authors.forename: Van Hung
authors.initials: VH
authors.lastname: Nguyen
authors.affiliation: Cuc Phuong National Park, Nho Quan, Ninh Binh, Viet Nam.
authors.forename: Nguyen Manh
authors.initials: NM
authors.lastname: Cuong
authors.affiliation: Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.
authors.forename: Djaja Doel
authors.initials: DD
authors.lastname: Soejarto
authors.affiliation: Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.
authors.forename: Harry H S
authors.initials: HHS
authors.lastname: Fong
authors.affiliation: Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, 835 South Wolcott Avenue, Chicago, IL 60612, USA. Electronic address: lijun@uic.edu.
authors.forename: Lijun
authors.initials: L
authors.lastname: Rong
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D052117:Benzodioxoles / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D020128:Inhibitory Concentration 50; D027902:Justicia / Q000737:chemistry*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular
chemical_list: D019380:Anti-HIV Agents; D052117:Benzodioxoles; D004365:Drugs, Chinese Herbal; D006027:Glycosides; D017705:Lignans; C000615627:justiprocumin B; C010130:diphyllin
keywords: Acanthaceae; Anti-HIV; Antiviral activity; Arylnaphthalide lignans glycosides; Justicia gendarussa; Justiprocumins; NRTI- and NNRTI-resistant HIV-1 variants; Plant natural products