Background: Influenza is historically an ancient disease that causes annual epidemics and, at irregular intervals,\npandemics. At present, the first-line drugs (oseltamivir and zanamivir) donââ?¬â?¢t seem to be optimistic due to the spontaneously\narising and spreading of oseltamivir resistance among influenza virus. Pogostemon cablin (Blanco) Benth.\n(P. cablin) is an important traditional Chinese medicine herb that has been widely used for treatment on common\ncold, nausea and fever. In our previous study, we have identified an extract derived from P. cablin as a novel selective\nneuraminidase (NA) inhibitor.\nResults: A series of polyphenolic compounds were isolated from P. cablin for their potential ability to inhibit neuraminidase\nof influenza A virus. Two new octaketides (1, 2), together with other twenty compounds were isolated from\nP. cablin. These compounds showed better inhibitory activity against NA. The significant potent compounds of this\nseries were compounds 2 (IC50 = 3.87 Ã?± 0.19 Ã?¼ mol/ml), 11, 12, 14, 15, 19 and 20 (IC50 was in 2.12 to 3.87 Ã?¼ mol/\nml), which were about fourfold to doubled less potent than zanamivir and could be used to design novel influenza\nNA inhibitors, especially compound 2, that exhibit increased activity based on these compounds. With the help of\nmolecular docking, we had a preliminary understanding of the mechanism of the two new compounds (1ââ?¬â??2)ââ?¬â?¢ NA\ninhibitory activity.\nConclusions: Fractions 6 and polyphenolic compounds isolated from fractions 6 showed higher NA inhibition\nthan that of the initial plant exacts. The findings of this study indicate that polyphenolic compounds and fractions 6\nderived from P. cablin are potential NA inhibitors. This work is one of the evidence that P. cablin has better inhibitory\nactivity against influenza, which not only enriches the compound library of P. cablin, but also facilitates further development\nand promises its therapeutic potential for the rising challenge of influenza diseases.
Loading....