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 IC values in the range of 15-21 nM (AZT, IC 77-95 nM). The compound also displayed potent inhibitory activity against the NRTI (nucleoside reverse transcriptase inhibitor)-resistant isolate (HIV-1) of the analogue (AZT) as well as the NNRTI (non-nucleoside reverse transcriptase inhibitor)-resistant isolate (HIV-1) of the analogue (nevaripine).

A Review on the Phytochemistry, Medicinal Properties and Pharmacological Activities of 15 Selected Myanmar Medicinal Plants

“…Two diphyllin glycosides were obtained from the stems and the barks of J. gendarussa ; justiprocumins A–B ( 110 , 111 ) [80] (Figure 10). Souza et al isolated four alkaloids, brazoides A–D ( 112 – 115 ), squalene, β-sitosterol and lupeol from the ethanol extract of leaves of J. gendarussa [81].…”

Revisiting the linkage between ethnomedical use and development of new medicines: A novel plant collection strategy towards the discovery of anticancer agents

“…Although no bio-prospecting and isolation work from the Lao PDR has thus far proceeded to the stage of patent filing thereby meriting additional studies (unlike for Vietnam; Zhang et al, 2014Zhang et al, , 2017, through the VietnamLaos ICBG, six medicinal plant taxa from around the country have been evaluated through the compound isolation stage and have been found to contain mostly novel phytochemicals bearing anti-tuberculosis , anti-malarial (He et al, 2005(He et al, , 2006Libman et al, 2008;Ma et al, 2008); and cancer cell cytotoxicity activities (Zhang et al, 2004). With respect to anticancer bio-prospecting from the ICBG field work conducted from 1998 to 2012 in the Lao PDR, at least 34 species yielded 50 extracts with significant activity (IC 50 < 20 μg/ml) in one or more cancer cell lines of a six cell line panel, which notably led to the isolated compounds asparacoside and 3''-methoxy-nyasol (IC 50 > 4 μg/ml, < 10 μg/ml) from Asparagus cochinchinensis (Lour.)…”

Lignans and Their Derivatives from Plants as Antivirals

“…MOA showed that DGP inhibits ZIKV fusion with cellular membranes and infection by preventing the acidification of endosomal/lysosomal compartments in the target cells [51]. Besides, it also displays potent activity against a broad spectrum of HIV strains with IC 50 values in the range of 15-21 nM [54]; MOA showed that it acts as a potential inhibitor of HIV-1 reverse transcription [55].…”