Bacterial neuraminidase (NA) are important enzymes in the control of pathological process, including microbe binding that lead to infection. The methanol extract from Petasites japonicas (PJ) showed potent inhibition against NA. The bioactivity-guided fractionation of this methanol extract results in the isolated of four compound. The chemical structures of the isolated compounds were determined as bakkenolide B (1), bakkenolide D (2), 1,5-dicaffeoylquinic acid (3), and 3-O-caffeoylquinic acid (4) by 1D and 2D NMR analysis and its NA activity and kinetic were further investigated. Of the isolated 1,5-dicaffeoylquinic acid exhibited the most potent NA inhibitory activity with IC50 values of 1.2 ug/ml. Kinetic studies using Lineweaver-Burk and Dixon-plots revealed that two caffoylquinic acid were competitive inhibitors, whereas bakkenolide exhibited non-competitive inhibitory characteristics. In conclusion, this study is the first to demonstrate that the phytochemicals of PJ display potent inhibitory activities against NA.

Bakkenolides and caffeoylquinic acids from the aerial portion of Pestasites japonicas and their bacterial neuraminidase inhibition

2019 Fall National Meeting

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