Polyphenolic glycosides isolated from Pogostemon cablin (Blanco) Benth. as novel influenza neuraminidase inhibitors

Abstract

BackgroundInfluenza is historically an ancient disease that causes annual epidemics and, at irregular intervals, pandemics. At present, the first-line drugs (oseltamivir and zanamivir) don’t seem to be optimistic due to the spontaneously arising and spreading of oseltamivir resistance among influenza virus. Pogostemon cablin (Blanco) Benth. (P. cablin) is an important traditional Chinese medicine herb that has been widely used for treatment on common cold, nausea and fever. In our previous study, we have identified an extract derived from P. cablin as a novel selective neuraminidase (NA) inhibitor.ResultsA series of polyphenolic compounds were isolated from P. cablin for their potential ability to inhibit neuraminidase of influenza A virus. Two new octaketides (1, 2), together with other twenty compounds were isolated from P. cablin. These compounds showed better inhibitory activity against NA. The significant potent compounds of this series were compounds 2 (IC50 = 3.87 ± 0.19 μ mol/ml), 11, 12, 14, 15, 19 and 20 (IC50 was in 2.12 to 3.87 μ mol/ml), which were about fourfold to doubled less potent than zanamivir and could be used to design novel influenza NA inhibitors, especially compound 2, that exhibit increased activity based on these compounds. With the help of molecular docking, we had a preliminary understanding of the mechanism of the two new compounds (1–2)’ NA inhibitory activity.ConclusionsFractions 6 and polyphenolic compounds isolated from fractions 6 showed higher NA inhibition than that of the initial plant exacts. The findings of this study indicate that polyphenolic compounds and fractions 6 derived from P. cablin are potential NA inhibitors. This work is one of the evidence that P. cablin has better inhibitory activity against influenza, which not only enriches the compound library of P. cablin, but also facilitates further development and promises its therapeutic potential for the rising challenge of influenza diseases.Electronic supplementary materialThe online version of this article (doi:10.1186/s13065-016-0192-x) contains supplementary material, which is available to authorized users.

Inhibition of sialidase activity as a therapeutic approach

“… 16 The first step in the search for novel potential drugs is often a simple screening of some promising sources, such as traditional medicinal plants. 17 , 18 The identified compounds that often possess only limited neuraminidase-blocking activity can be further used as base molecules for design of novel potent inhibitors. 19 , 20 However, the occurrence of naturally present neuraminidase inhibitors is not limited to plants.…”

Integrated Chinese herbal medicine and Western medicine successfully resolves spontaneous subcutaneous emphysema and pneumomediastinum in a patient with severe COVID-19 in Taiwan: A case report

“…P. cablin, S. baicalensis and A. capillaris in the Ganlu Xiaodu Decoction are widely used herbal medicines for their antiviral effects. 30 , 31 , 32 S. baicalensis is commonly used for upper respiratory tract infections and in particular for its anti-influenza viral activities in H1N1 and H3N2 infections. Moreover, the derivative S. barbata D. Don inhibits the main proteases of SARS-CoV-2 infection (Mpro and TMPRSS2) and replication protease activity.…”

Efficacy and safety of Qinxiang Qingjie oral solution for the treatment of influenza in children: a randomized, double-blind, multicenter clinical trial

“…Similarly, Wu et al reported that patchouli downregulates the expression of inflammatory cytokines such as interferon-γ (IFN-γ) and interleukin-4 (IL4) (30). According to Liu et al, polyphenolic compounds isolated from patchouli may have potential as novel anti-influenza agents due to their neuraminidase inhibitory activity (31). Radix scutellariae, another component of the QXQJ oral solution, has been confirmed to protect influenza A virusinfected mice by inhibiting neuraminidase activities and remarkably decreasing lung virus titers (32).…”