Amide alkaloids and neolignans from Piper hongkongense and their inhibitory activities of PCSK9 expression

Abstract

Four undescribed amide alkaloids hongkongensines A-C and 1-(1-oxo-6-hydroxy-2E,4E-dodecadienyl)-piperidine, five known amide alkaloids, and three known neolignans were isolated from the aerial part of Piper hongkongense. The planar structures of these compounds were determined by detailed analyses of HR-ESI-MS and NMR data. The absolute configurations of hongkongensines A-C were elucidated by single-crystal X-ray diffraction analysis and ECD calculations. Moreover, the inhibitory activities of PCSK9 expression in vitro for all compounds were assessed by PCSK9 AlphaLISA screening. Kadsurenone (10) displayed a significant inhibitory activity at 5 μM with an inhibition rate of 51.98%, compared with 55.55% of berberine (BBR 5 μM).

Keywords: Amide alkaloids; Inhibitory activities of PCSK9 expression; Neolignans; Piper hongkongense; piper.