A stilbene dimer and flavonoids from the aerial parts of Chromolaena odorata with proprotein convertase subtilisin/kexin type 9 expression inhibitory activity

Pisey Pel, Hee Sung Chae, Piseth Nhoek, Young Mi Kim, Piseth Khiev, Geum Jin Kim, Joo Won Nam, Hyukjae Choi, Young Hee Choi, Young Won Chin

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19 Scopus citations

Abstract

Investigation of components of the chloroform-soluble and ethyl acetate-soluble extracts of the aerial parts of Chromolaena odorata L. selected by PCSK9 mRNA expression monitoring assay in HepG2 cells led to the isolation of a new stilbene dimer, (+)-8b-epi-ampelopsin A (1), and 30 known compounds (2–31). The structures of the isolates were established by interpretation of NMR spectroscopic data and the stereochemistry of the new stilbene (1) was proposed based on ECD and NMR calculations. Among the isolates, 1, 5,6,7,4′-tetramethoxyflavanone (6), 5,6,7,3′,4′-pentamethoxyflavanone (7), acacetin (18), and uridine (21) were found to inhibit PCSK9 mRNA expression with IC50 values of 20.6, 21.4, 31.7, 15.0, and 13.7 µM, respectively. Furthermore, the most abundant isolate among the selected compounds, 6, suppressed PCSK9 and low-density lipoprotein receptor protein expression in addition to downregulating the mRNA expression of HNF-1α.

Original languageEnglish
Article number103869
JournalBioorganic Chemistry
Volume99
DOIs
StatePublished - Jun 2020

Keywords

  • (+)-8b-epi-ampelopsin A
  • 5,6,7,4′- tetramethoxyflavanone
  • Chromolaena odorata
  • Flavonoid
  • HNF-1α
  • LDLR
  • PCSK9
  • Stilbene dimer

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